RSC - RSC Med. Chem. latest articles

Light-Controlled Inhibition of Gram-Positive Bacteria by Photoswitchable Amphiphilic Lipids (PALs)

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00096G, Research Article

Open Access

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.

Guilherme Fernandes, Seong Heun Kim, Charlotte K Hind, Jessica Furner-Pardoe , Janis Romanopulos, Christian D. Lorenz, James Mason, J. Mark Sutton, Daniele Castagnolo
Amphiphilic lipids are potent membrane-disrupting antibacterials, but their activity cannot normally be modulated after administration. Here we report photoswitchable amphiphilic lipids (PALs) that enable reversible, light-controlled modulation of antibacterial potency...
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Development of novel chalcone-based quinazoline derivatives as dual VEGFR-2 and EGFR inhibitors

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00179C, Research Article

Zainab Elsayed, Haytham O. Tawfik, Loah R Hemeda, Mohamed S. Nafie, Hadia Almahli, Rehan Monir, Ikhlas A Sindi, Eslam Elkaeed, Mostafa M Elbadawi, Mahmoud A. El Hassab, Wagdy M. Eldehna
As possible dual VEGFR-2/EGFR inhibitors, a new set of quinazoline-chalcone hybrid compounds (8a-h and 11a-h) was logically developed and synthesized. The synthesized compounds' chemical structures were verified by high-resolution mass...
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Small-Molecule Therapeutics for Diabetic Retinopathy: From VEGFR Inhibitors to Emerging Non-VEGF Targets

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00069J, Review Article

Yan Li, Wenfang Zhang, Yin-Liang Bai, Honghua Zhang
Diabetic retinopathy (DR) remains a leading cause of vision loss worldwide and is driven largely by chronic microvascular dysfunction dominated by vascular endothelial growth factor (VEGF) signaling. Although biologics have...
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Recent advances in the development of acridine-based hybrids with antiproliferative activity

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00023A, Review Article

Mahdi Gallala, Najeh Tka, Sonia Aroui
Exploring the evolution of acridine hybrids as multi-targeted anticancer agents, this review synthesizes key SAR insights and design principles. It evaluates the impact of hybridization on potency, selectivity, and preclinical development.
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Beyond acrylamide: a structure-guided investigation of covalent warheads in the development of CDK7 inhibitors

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00088F, Research Article

Yu Cao, Yiqing Huang, Yunlong Pan, Jialuo Mao, Lixin Gao, Jiankang Zhang, Huajian Zhu, Shourong Liu, Rangxiao Zhuang, Yang Liu, Yubo Zhou, Jiaan Shao
To achieve covalent CDK7 inhibitors with superior antiproliferative activity and enhanced selectivity, we designed and synthesized a series of covalent CDK7 inhibitors bearing diverse warheads based on the THZ1 scaffold.
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Histone Deacetylases-Based Dual Inhibitors: Research Progress Focusing on Non-Small Cell Lung Cancer Therapy

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00063K, Review Article

Zhiguang Yang, Zihao Liu
Epigenetic regulation plays a pivotal role in the initiation, progression and drug resistance mechanisms of non-small cell lung cancer (NSCLC). As important epigenetic regulatory enzymes, histone deacetylases (HDACs) are aberrantly...
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The effects of bioisostere substitution on the antimicrobial and physicochemical properties of supramolecular self-associating amphiphiles

RSC Med. Chem., 2026, 17,2151-2156
DOI: 10.1039/D6MD00091F, Research Article

Open Access

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.

Pinky K. Naicker, Mariam Yacoub, Lisa J. White, Dominick E. Balderston, Perry A. Hailey, J. Mark Sutton, Charlotte K. Hind, Jennifer R. Hiscock
The use of bioisosteres enhances the antimicrobial activity for a range of supramolecular self-associating amphiphiles.
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Design and biological evaluation of triagonist GLP-1R/GCGR/GIPR peptides as potential therapeutic agents for diabetes and obesity

RSC Med. Chem., 2026, 17,2113-2129
DOI: 10.1039/D5MD01086A, Research Article

Iwona Kalinowska, Alicja Gawalska, Paulina Kasprzycka, Michał Stępniewski, Piotr Rózga, Aneta Pałka, Andrii Shubin, Katarzyna Bukato, Marlena Gałązka, Ewa Burchard, Paulina Zielińska-Świder, Albert Jaworski, Marcin Feder
Rational design and molecular modelling enabled the development of potent GLP-1/GIP/GCGR triagonists with robust in vitro activity and efficacy comparable to established incretin agonists.
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Discovery of dihydrospiro[cyclopropane-1,7′-pyrrolo[3,4-d]pyrimidine] derivatives as novel ATR inhibitors

RSC Med. Chem., 2026, 17,2067-2080
DOI: 10.1039/D5MD01127B, Research Article

Xiaozhen Chen, Yunbo Qian, Yitong Guo, Junfei Li, Lei Xu, Xingxing Zeng, Kailong Jiang, Yubo Zhou, Jia Li, Tao Liu
Novel ATR inhibitors were developed using a scaffold hopping strategy, with compound 10h exhibiting favorable activity.
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Design, synthesis and biological assessment of erlotinib-1,2,3-triazole derivatives for anticancer applications

RSC Med. Chem., 2026, 17,2053-2066
DOI: 10.1039/D5MD01149C, Research Article

Qiyan Yao, Kexin Qu, Lan Wang, Mengmeng Huang, Longfei Mao, Sanqiang Li
A series of novel erlotinib derivatives incorporating 1,2,3-triazole moieties were synthesized and evaluated for their anti-hepatocellular carcinoma activity both in vitro and in vivo.
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Peptides as multifunctional linchpins in targeted drug conjugates

RSC Med. Chem., 2026, 17,1794-1810
DOI: 10.1039/D6MD00049E, Review Article

Open Access

This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence.

Xue Li, Yuechen Qian, Jiongjia Cheng, Qian Chu
Multifunctional roles of peptides in peptide–drug conjugates.
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Design, synthesis, and biological evaluation of X19: a matrine pyrazole derivatives therapeutic candidate

RSC Med. Chem., 2026, 17,2002-2014
DOI: 10.1039/D5MD01118C, Research Article

Tingguo Xu, Suyi Dai, Zhouxing Hu, Anqi Ou, Xingdong Wang, Lisheng Wang
A series of novel matrine-pyrazole derivatives were designed and synthesized through structural modification of the natural alkaloid matrine to enhance its antitumor efficacy.
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Extending the architecture of bolaamphiphilic disinfectants: an investigation of octenidine and isooctenidine analogs

RSC Med. Chem., 2026, 17,2144-2150
DOI: 10.1039/D5MD01098E, Research Article

Danielle E. Talbot, Caroline M. Casey, Elise L. Bezold, Kelsi Membrino, Alina Y. Muldagaliyeva, William M. Wuest, Kevin P. C. Minbiole
Octenidine and isooctenidine are equally potent disinfectant architectures, capitalizing on a bolaamphiphilic structure to confer significant activity to two dozen QACs tested against a panel of gram positive, gram negative, and resistant bacteria.
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Discovery of GBA-16-24 as a highly potent, selective ATR inhibitor for the treatment of FLT3-mutated acute myeloid leukemia

RSC Med. Chem., 2026, 17,2081-2095
DOI: 10.1039/D5MD01005E, Research Article

Ping Li, Haiyan Ren, Xinyan Lan, Junfei Li, Zhi Liu, Huashuo Liu, Zhijie Zheng, Tianyan Zeng, Peili Wang, Mingyang Sun, Lei Xu, Yanyan Zhang, Yubo Zhou, Jia Li, Mingliang Wang, Kailong Jiang
A novel and selective ATR inhibitor, GBA-16-24, was developed. It exhibits potent synthetic lethality in FLT3-mutated AML and synergizes with clinical FLT3 inhibitors, proposing a promising combination therapy.
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Design, synthesis and biological evaluation of novel 3,4-dihydro-2(1H)-quinoline-O-carbamate derivatives as AChE/MAO-B dual inhibitors for the treatment of Alzheimer's disease

RSC Med. Chem., 2026, 17,2096-2112
DOI: 10.1039/D5MD01138H, Research Article

Wenling Fu, Keren Wang, Hongsong Chen, Taoyi Liu, Xiaojuan Liu, Qishun Jin, Zhenghuai Tan, Wu Dong, Wenmin Liu, Zhipei Sang
Based on the MTDL strategy, a dual AChE/MAO-B inhibitor 3c was obtained. 3c presented good BBB permeability and significant efficacy in vivo.
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New series of pentamidine-based 1,2,3-triazole-diaryl-hydrazones: design, synthesis, and evaluation of their leishmanicidal activity and mechanism of action against Leishmania (L.) amazonensis

RSC Med. Chem., 2026, 17,2157-2169
DOI: 10.1039/D5MD01174D, Research Article

Patrícia F. Espuri Sepini, Vanessa Silva Gontijo, Laiane Mota Tavares, Leonardo Maciel Souza, Thalles H. F. Souza, Dyecika S. Couto, Juliana B. Nunes, Catarina Azevedo Ribeiro, Sara M. Mendonça da Silva Cravo, Bruno Zavan, Marina A. Alves, Hygor M. R. Souza, Marisa Ionta, Maria Emília Sousa, Eduardo F. Peloso, Marcos J. Marques, Claudio Viegas Jr.
New series of pentamidine-based 1,2,3-triazole-diaryl-hydrazones was designed, synthesized, and evaluated against L. amazonensis, with PQM-150 as the most potent multifunctional compound.
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1,3,4-Oxadiazole derivatives: targeting multiple bacterial pathways

RSC Med. Chem., 2026, 17,1867-1887
DOI: 10.1039/D5MD01139F, Review Article

Pankaj Gupta, Sangeeta Verma, Rakesh Narang, Bhupesh Sharma, Vikramjeet Singh, Sukhbir Lal
1,3,4-oxadiazole-based compounds exhibited antibacterial activity through inhibition of various essential bacterial cell components or pathways.
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In vitro and in vivo studies of dehydroxylated-isoquines and -isotebuquines against trypanosomatids: a preclinical drug candidate for treatment of cutaneous leishmaniasis

RSC Med. Chem., 2026, 17,2015-2035
DOI: 10.1039/D6MD00006A, Research Article

Angel H. Romero, Elva Serna, Elena Aguilera, Belen Davila, Francisco Delgado, Gonzalo Scalese, Leticia Pérez-Díaz, Gloria Yaluff, Noris Rodríguez, Hugo Cerecetto
A promising candidate based on dehydroxylated isotebuquine against cutaneous leishmaniasis was identified, with high in vitro activity against intracellular forms, adequate ADME-properties and drug-likeness parameters and good in vivo efficacy.
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Adamantane-based inhibitors of the influenza A M2 proton channel: structure-based design, biological evaluation, and synthetic approaches

RSC Med. Chem., 2026, 17,1811-1846
DOI: 10.1039/D5MD01027F, Review Article

Open Access

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.

Marianna Stampolaki, Maria-Eleni Kouridaki, Kyriakos Georgiou, Antonios Kolocouris
Experimental structures and accurate simulations can guide the design and synthesis of adamantanamines that can block AM2 wild-type and mutant AM2-mediated proton conductance.
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ZRMQ-22, a novel DYRK1A inhibitor, attenuates neuroinflammation and cognitive impairments in LPS-induced mice: a potential strategy for Alzheimer's disease

RSC Med. Chem., 2026, 17,2036-2052
DOI: 10.1039/D6MD00007J, Research Article

Mengyu Ren, Huanhua Chen, Zhenshu Li, Jiacheng Zhuang, Aizhu Yang, Xiangdong Li, Xinyu Li, Xinpeng Wang, Zonghe Xu, Xianghuan Liu, Jiawen Song, Tianhao Jiang, Zihua Xu, Xudong Gao, Qingchun Zhao
Alzheimer's disease (AD) is a progressive neurodegenerative disorder characterized by irreversible cognitive decline and memory loss.
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PROTAC-mediated multi-target protein degradation in Alzheimer's disease: mechanistic insights, therapeutic applications, and translational challenges

RSC Med. Chem., 2026, 17,1847-1866
DOI: 10.1039/D5MD00963D, Review Article

Open Access

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.

Bin Wang, Yunan Li, Tingting Yao, Xinai Shen, Huan Li, Wei Jiang, Xinuo Li, Zheying Zhu
Clearing pathological proteins in Alzheimer's disease via PROTAC-induced degradation.
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PROTAC approaches against drug-resistant EGFRC797S/L858R/T790M mutants: biological evaluation and SAR studies (2020–2025)

RSC Med. Chem., 2026, 17,1888-1906
DOI: 10.1039/D5MD01113B, Review Article

Ankush Kumar, Vishakha Sharma, Pallvi Kumari, Rajwinder Kaur, Rohit Bhatia
The development of EGFR^{C797S/L858R/T790M} mutation has become a major barrier to tyrosine kinase inhibitors.
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Design, synthesis and exploration of cyclic imides as PDE4 inhibitors in psoriasis

RSC Med. Chem., 2026, 17,1968-1988
DOI: 10.1039/D5MD01165E, Research Article

Veena K. S., Pallabi Panja, Tirtha Nath, V. G. M. Naidu, Kalyan K. Sethi
Twenty cyclic imide derivatives were synthesized and tested for their PDE4B inhibition potential. The best molecule selected was further evaluated for its anti-inflammatory property in vitro and PDE4B selectivity in silico.
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Antibacterial peptidomimetics via fragment display on small-molecule scaffolds

RSC Med. Chem., 2026, 17,1989-2001
DOI: 10.1039/D5MD00916B, Research Article

Emma Dyhr, Lucía Cañete de Pinedo, Nicki Frederiksen, Martin Saxtorph Bojer, Hanne Ingmer, Ingvill Pedersen Sæbø, Synnøve Brandt Ræder, Magnar Bjørås, Emily Helgesen, James Alexander Booth, Henrik Franzyk
In response to the growing threat of antimicrobial resistance, scaffold-based peptidomimetics were explored as potential antibacterial agents.
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Synthesis and evaluation of 14β-acyl substituted 17-cyclopropylmethyl-7,8-dihydromorphinone derivatives: mixed partial agonists at mu opioid and nociception/orphanin FQ peptide receptors

RSC Med. Chem., 2026, 17,1950-1960
DOI: 10.1039/D5MD00685F, Research Article

Open Access

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.

Mehrnoosh Ostovar, Keith Olsen, Gerta Cami-Kobeci, John R. Traynor, Luka Jeramaz, Stewart B. Kirton, Stephen M. Husbands
The development of a new series of mixed mu/nociceptin opioid partial agonists as analgesics with a greatly improved safety profile.
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Biocompatible de novo indolylchalcones as platelet aggregation inhibition and diabetic wound healing agents

RSC Med. Chem., 2026, 17,1916-1937
DOI: 10.1039/D5MD00984G, Research Article

Sumit Kumar, Radhika Chaurasia, Gaurav Kumar, Arun K. Sharma, Ijaz Ahmed, Alam Nur-E-Kamal, Monalisa Mukherjee, Brajendra K. Singh, Virinder S. Parmar
Biocompatible de novo indolylchalcones exhibit anti-platelet aggregation and nitric oxide-mediated effects. They show antiplatelet activity and accelerated diabetic wound healing, indicating promise for diabetic wounds and cardiovascular therapy.
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Verbenone-based selenophene derivatives as potential anti-cancer agents: synthesis and biological evaluation in 2D and 3D A549 cell models

RSC Med. Chem., 2026, 17,2130-2143
DOI: 10.1039/D5MD01140J, Research Article

Jiale Han, Wei Shi, Min Hu, Wei Liu, Hongmei Wu, Biao Xiong, Xiaodong Qiu, Yunyun Wang
Compound 2R, a verbenone–selenophene hybrid, selectively inhibits A549 cells via ROS-mediated mitochondrial dysfunction, apoptosis and G0/G1 arrest, with efficacy confirmed in a 3D tumor spheroid model.
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Emerging strategies for Alzheimer's disease: leveraging flavonoid derivatives for early diagnosis and neuroprotection

RSC Med. Chem., 2026, 17,1771-1793
DOI: 10.1039/D5MD01026H, Review Article

Zhe Han, Wenling Fu, Mingjuan Dai, Roujun Lu, Jianhua Yu, Wu Dong, Zhipei Sang
Alzheimer's disease (AD) is a prevalent chronic and progressive neurodegenerative disorder predominantly affecting the elderly population.
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Harnessing oligonucleotide architecture for potent multivalent inhibition of human carbonic anhydrases

RSC Med. Chem., 2026, 17,1961-1967
DOI: 10.1039/D5MD01167A, Research Article

Open Access

This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence.

Eslam M. Abbass, Federico Ladu, Justine Mansot, Mathieu Noël, Alessio Nocentini, Mario Sechi, Claudiu T. Supuran, Michael Smietana, Jean-Yves Winum
This study introduces oligonucleotides as spatially defined multivalent platforms for carbonic anhydrase inhibitor design.
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Discovery of novel coumarin amphiphiles: dual-action antimicrobials with bacteria-mediated biofilm disruption and host-directed immunomodulation

RSC Med. Chem., 2026, 17,1938-1949
DOI: 10.1039/D6MD00004E, Research Article

Haiyang Zhang, Qun Tang, Qian Zhu, Weiwei Xu, Zhihao Wang, Zirui Jiao, Jiakun Zuo, Wei Jiang, Cuiqin Huang, Huifang Yin, Xiangan Han, Wen Zhou
Coumarin-derived amphipathic compounds were synthesised. Compound 15 shows potent anti-S. aureus, anti-biofilm and in vivo activities as a potential candidate.
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Discovery of a CHI3L1-targeted small molecule modulating neuroinflammation in Alzheimer's disease via DNA-encoded library (DEL) screening

RSC Med. Chem., 2026, 17,1907-1915
DOI: 10.1039/D5MD00943J, Research Article

Baljit Kaur, Longfei Zhang, Hossam Nada, Laura Calvo-Barreiro, Moustafa T. Gabr
Chitinase-3-like protein 1 (CHI3L1, also known as YKL-40) has emerged as a central effector of astrocyte-mediated neuroinflammation and a promising biomarker for Alzheimer's disease (AD).
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Structure-guided optimisation of fenofibrate-derived oxidative phosphorylation inhibitors to modify tumour hypoxia

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D5MD00742A, Research Article

Open Access

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.

James P. Holt-Martyn, Nicole Machado, James T. T. Coates, Rathi Puliyadi, Thomas Ashton, Elysia Traynor, Samina Aslam, Thomas K. Wise, Gonzalo Rodriguez-Berriguete, Christopher J. Schofield, Geoff S. Higgins
Hypoxia, or low levels of oxygen, is a common feature of solid tumours that makes them resistant to cancer therapies. Electron transport chain inhibitors are a promising strategy for O₂ redistribution to target tumour hypoxia during radiotherapy.
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Sulfone and Sulfoxide-containing Pharmaceuticals: Targets, Pharmacological Properties and SAR Studies

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D5MD01089F, Review Article

Yunfei Du, Yiyang Zhou, Jinqu Li, Yiou Mei, Yuzhu Chen, Fengxia Sun
Sulfone/sulfoxide functional groups are extremely important functional groups widely utilized in the design of biologically active drugs. Pharmaceuticals incorporating sulfone/sulfoxide have shown a broad spectrum of pharmacological properties, including anti-inflammatory,...
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Design, synthesis, and anticancer evaluation of novel pyrrole–pyrazoline/chalcone hybrids: in vitro and computational insights into EGFR inhibition

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D5MD00800J, Research Article

Open Access

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.

Mansour S. Alturki, Marwa F. Ahmed, Abdulaziz H. Al Khzem, Mohamed S. Gomaa, Mohammad Sarafroz, Nada Tawfeeq, Mashael M. Alharbi, Abdulaziz K. Al Mouslem, Mohammed F. Aldawsari, Wajin R. Alruwili, Shah Alam Khan, Radwan El-Haggar, Atiah H. Almalki
Design, synthesis, and biological evaluation of pyrazoline–pyrrole hybrids led to the identification of compound 6b as a potent EGFR inhibitor with significant antiproliferative activity against MCF-7 cells.
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New Terpenyl-Cinnamoyl-Hydrazone Analogues of Cannabidiol with Potent Antinociceptive Effect

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00185H, Research Article

João Pedro Barros de Paiva, Anna Carolina Pereira Lontra, Rachel Marins Campos, Eduardo Araújo, Thaís Biondino Sardella Giorno, Mikaela Lucinda de Souza, Graziella Dos Reis Rosa Franco, Claudio Viegas, Jr., Patricia Dias Fernandes
In this study, novel terpenyl-cinnamoyl-hydrazone analogs were synthesized and evaluated for antinociceptive potential in preclinical nociception models. The compounds were tested in chemical (formalin-induced licking) and thermal (hot plate) assays...
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Addressing Multidrug-resistant Bacterial Infections with Iridium-based Theragnostic Agents

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00120C, Research Article

Rama Karn, Mahesmita Sahoo, Sayantani Biswas, Suravi Chauhan, Ajay Kumar Nag, Soham Basu, Srikanta Patra, Debasis Manna
Effective strategies are essential for addressing bacterial infections caused by antimicrobial resistance (AMR). The increasing interest in transition-metal complexes stems from their fluorescence properties and diverse mechanisms of action against...
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Design, synthesis and pharmacological evaluation of 3H-spiro[benzofuran-2,4′-piperidine] IRAK4 inhibitors for the treatment of diffuse large B-cell lymphoma

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00025H, Research Article

Zhiwei Chen, Qi Zhang, Yun Chen, Yi Ning, Q-i Zhang, Mengxiao Zhang, Qiupei Liu, Yi Xue, Linjiang Tong, Jian Ding, Hua Xie, Wenhu Duan
We report the discovery of a new series of 3H-spiro[benzofuran-2,4′-piperidine] IRAK4 inhibitors as potential anti-DLBCL agents.
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Lead optimization of 5jc21 (CG13250), a quinolin-2(1H)-one-based inhibitor of the BRD4 member of the bromodomain and extraterminal (BET) family of proteins

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D5MD01082A, Research Article

Jay Chauhan, Sarah Pogash, Makoto Yoshioka, Mithun Raje, Daniel Van Eker, Jeffrey W. Strovel, Steven Fletcher
4,6-Disubstituted quinolinones are potent BRD4 inhibitors.
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Diverse ring architectures of cyclic peptidomimetics targeting melanocortin receptors

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00115G, Review Article

Wenxiao K. Yue, Nicholas Barlow, Philip E. Thompson
A review of the many types of macrocyclic melanocortin peptides. We show that there is a historical gap in the evaluation of these architectures in terms of their influence upon potency, selectivity and pharmacokinetics.
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Quinoline/thiazole compounds as selective acetylcholinesterase inhibitors: synthesis and biological assessment

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00165C, Research Article

Open Access

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.

Berkant Kurban, Derya Osmaniye, Serkan Levent, Yusuf Özkay, Zafer Asım Kaplancıklı
Acetylcholine (ACh), acetylcholinesterase enzyme (AChE), and AChE inhibition are of great importance in the treatment of neurodegenerative diseases.
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D-Galactose-conjugated pyrimidine thioureas as potent antimicrobial agents: rapid green synthesis, structure–activity relationships and molecular modelling

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00026F, Research Article

Nguyen Dinh Thanh, Vu Ngoc Toan, Ngo Hong Anh Thu, Nguyen Minh Tri, Duong Ngoc Toan, Hoang Thi Kim Van
D-Galactose–pyrimidine thioureas were synthesized via a recyclable ionic liquid–microwave method in high yields. Several derivatives showed broad-spectrum antimicrobial activity, and docking with ADMET predicted strong binding and drug-like properties.
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Emerging Cellular Uptake Mechanisms of bRo5 PROTACs

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00243A, Review Article

Toshihiko Tashima
Proteolysis-targeting chimeras (PROTACs) predominantly occupy beyond-Rule-of-5 (bRo5) chemical space, where the mechanisms governing their cellular uptake remain incompletely understood and are not captured by classical models of passive membrane diffusion....
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Bicyclic monoterpenoid-based orthopoxvirus inhibitors: design, synthesis, and biological assessment of a novel amide series

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00217J, Research Article

Serafim A. Tishchenko, Anastasiya S. Sokolova, Valeriya V. Samsonova, Julia G. Pushkareva, Nikolay I. Bormotov, Ivan A. Moskalev, Daria. E. Solomina, Artem D. Rogachev, Alina V. Fatyanova, Sophia S. Borisevich, Olga I. Yarovaya, Olga A. Serova, Alena S. Ovchinnikova, Alexander A. Sergeev, Larisa N. Shishkina, Artemiy A. Sergeev, Alexander P. Agafonov, Nariman F. Salakhutdinov
This study reports the design, synthesis, and comprehensive biological evaluation of a new class of orthopoxvirus inhibitors utilizing natural bicyclic monoterpenoid scaffolds as strategic replacements for synthetic polycyclic cores.
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Regioselective Triclocarban-Catalyzed Synthesis of Spiroindeno- and Spirooxindolo-Pyrrolizidines with Apoptosis Induction in MCF-7 Cells

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00132G, Research Article

V Rukyanaik, Samata Pradhan, Chandraiah Godugu, Srinu Tothadi, Kadiyam Rama Krishna, Ravinder Pawar, Srinivas Basavoju
Design of new molecules from known structural motifs via [3+2] cycloaddition is a widely used strategy in modern drug discovery. Herein, an efficient, eco-friendly synthesis of spiroindeno- and spirooxindolo-pyrrolizidine derivatives...
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Pyrazole–triazole hybrids as kinase-triad inhibitors: a triple-target strategy for synergistic anticancer therapy

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00022C, Research Article

Mahmoud S. Elkotamy, Mohamed K. Elgohary, Mariam M. Fakhry, Mohamed E. Albakri, Abdelrahman A. Naglah, Abdulrahman A. Almehizia, Ahmed M. Naglah, Mohamed Fares, Haytham O. Tawfik, Wagdy M. Eldehna, Hatem A. Abdel-Aziz
The ongoing issue of drug resistance and the lack of specificity in existing cancer treatments highlight the necessity for innovative multi-target agents.
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A new class of Indole-based HDAC8 inhibitors as potential anti-lung cancer agents: In silico design, synthesis, biological assessment and binding interaction analysis

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00194G, Research Article

SAMIMA KHATUN, Venkatesh Muthukumar, Ambati Himaja, Indrasis Dasgupta, Kalpataru Das, Balaram Ghosh, Shovanlal Gayen
A novel series of indole-based hydroxamic acids was designed, synthesized, and evaluated as promising HDAC8 inhibitors for lung cancer therapy. In silico analyses, including classification-based QSAR, chemical space networks, and...
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Design, synthesis, and biological evaluation of quinoline derivatives as dual-target inhibitors of chitin synthase and glucosamine-6-phosphate synthase

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D5MD01001B, Research Article

Nan Wang, Lige Liu, Tao Liu, Hong Luo, Yan Long, Xinlong Yang, Youli Zhang, Qinggang Ji
This study designed and synthesized a series of glycine methyl ester quinoline derivatives as dual-target inhibitors of CHS and GlmS, followed by biological evaluation including enzyme inhibition assays and in vitro antifungal activity testing.
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Novel zerumbone-amide-triazole hybrids as potential NF-κB pathway inhibitors: design, synthesis, cytotoxicity evaluation, computational studies, and mechanistic insights

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00148C, Research Article

Pham The Chinh, Pham Thi Tham, Vu Thi Lien, Dao Thi Nhung, Le Thi Thuy Loan, Khieu Thi Tam, Vu Tuan Kien, Cao Thanh Hai, Phan Thanh Phuong, Truong Thi Thao, Vuong Truong Xuan, Le Thi Lien
A series of fifteen novel zerumbone-amide-triazole hybrids 12a–i and 15a–f were successfully designed and synthesized from azazerumbone II (2) via click reaction.
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Synthesis-guided design and discovery of alkylated indoles with antibacterial activity against MRSA

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00221H, Research Article

Auqib Rashid, Vishwani Jamwal, Bilal A Bhat, KULJIT SINGH, Showkat Rashid
Substantially high morbidity and mortality rates are associated with antimicrobial resistance (AMR), which poses an alarming challenge to global healthcare. The causative, drug-resistant superbugs (headed by Staphylococcus aureus) adopt multiple...
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Structure-based design of potent pyrazolo[1,5-a]pyrimidine CDK4/6 inhibitors: biological evaluation and computational validation

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D5MD01147G, Research Article

Faizah A. Binjubair, Mahmoud S. Elkotamy, Amr A. Mattar, Bjad K. Almutairy, Sara T. Al-Rashood, Mohamed M. Eldesouki, Jalloul Bouajila, Hatem A. Abdel-Aziz, Mariam M. Fakhry
Structure-based design yielded potent CDK4/6 inhibitor 19i, inducing G1 cell-cycle arrest and apoptosis in HCT-116 cells, supported by enzymatic inhibition and molecular docking/dynamics studies.
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Discovery of novel BCAT2 inhibitors: design, synthesis, in vitro evaluation, and molecular modeling studies

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00019C, Research Article

Dong Xu, Wenxiu Weng, Huining Cao, Chao Zhang, Yudi Zhang, Yan Li, Junhai Xiao, Hua Xie, Jialin Guo, Guoliang Chen
Structure-based rational design yielded novel potent BCAT2 inhibitors C10 (IC₅₀ = 44 nM) and C11 (IC₅₀ = 54 nM), which exhibit 8–10-fold selectivity over BCAT1 and form stable, key interactions within the BCAT2 active pocket.
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Recent advances towards BACE1 drug discovery and therapeutics design

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D5MD01095K, Review Article

Open Access

This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence.

Saim Imran, Meera Patel, Meissam Noroozifar, Kagan Kerman
We explored the latest developments in modulators, antibody therapy, and gene therapy targeting β-site amyloid precursor protein cleaving enzyme 1 (BACE1) to combat Alzheimer's disease.
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Hypoxia-triggered dichloroacetate delivery with effective reversal of cancer cell reprogramming

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D5MD00911A, Research Article

Rensong Sun, Lei Wang, Ziang Liu, Hao Wu, Wanwan Wang, Yang Wang, Xiao Qian, Engin U. Akkaya
The 3-methyl-2-nitroimidazole dichloroacetate derivative studied in this work is a prodrug version of dichloroacetate, and it is active at lower concentrations in hypoxic cell cultures and suppresses tumor progression significantly in vivo.
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Decoding the association of polycystic ovary syndrome with metabolic-associated fatty liver: insights into CK18 and LC3II/ATG7/P62 autophagy axis and adjunct therapeutics of metformin and levothyroxine

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D5MD00819K, Research Article

Sameeah Mejbel Hamad Algenabi, Anwar Nather Seiwan, Maha Hussein Hashem Sabra, Doaa I. Mohamed, Lobna Fouad Abd ElAziz Bassyouni, Dalia Alaa El-Din Aly El-Waseef, Samar F. Ezzat, Omnyah A. El-Kharashi, Hanaa F. Abd El-Kareem, Hyfa A. Alzahrani, Fawzyah Obeedallah Albaldi, Ahmed Shokry Elharoun, Mansour Altayyar, Amal Fahmy Dawood, Hebatallah H. Abo Nahas, Ahmed Abdel-Salam M. Elmelegy
Metformin–levothyroxine synergistically treats PCOS-MAFLD. Reduced body/liver weight, ALT/AST/TSH/lipids, testosterone/LH/HOMA-IR. Increased estradiol. Suppressed autophagy (LC3II/ATG7/p62/CK18) and improved histology.
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Beyond infection control: exploring the therapeutic potential of antimicrobials in oncology and their synthetic perspectives

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00084C, Review Article

Rahul Kumar, Mohd Yeshab Ansari
This review explores the burgeoning potential of antimicrobial agents in oncology, highlighting their roles in reducing infection-related mortality, enhancing therapeutic effectiveness, and improving the overall quality of life in cancer patients.
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Phenoxyacetic acid scaffold as a platform for dual anticonvulsant and anti-inflammatory drug design

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00097E, Research Article

Mohamed K. Elgohary, Mahmoud Abdelrahman Alkabbani, Aya Mohamed Ahmed Ibrahim, Ahmed Elsonbaty, Mayada H. Mohamed, Abdulrahman A. Almehizia, Ahmed M. Naglah, Mohamed Fares, Hatem A. Abdel-Aziz
Neuroinflammation is increasingly recognized as a critical contributor to epileptogenesis and antiepileptic drug resistance, emphasizing the need for multi-target therapeutic strategies.
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A Comprehensive Study of Novel Pregnenolone-Isoxazole Hybrids as Selective Inducers of Mitochondrial Apoptosis in Breast Cancer Cells

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00076B, Research Article

Victoria Malakhova, Alexander Scherbakov, Diana I. Salnikova, Alvina Khamidullina, Danila Sorokin, Dmitry A. Vasilenko, Elena Chernoburova, Elena Averina, Igor V. Zavarzin, Yulia Volkova
Heterocyclic derivatives of steroids have emerged as promising anticancer agents by concurrently targeting multiple pathways, including apoptosis induction, cell cycle arrest, and mitochondrial dysfunction. Here, we report novel pregnenolone-isoxazole hybrids...
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Triclosan–isatin hybrids as potent anti-proliferative agents inducing S-phase arrest via DNA gyrase inhibition in triple-negative breast cancer

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00013D, Research Article

Shekhar, Asif Raza, Sukhmanpreet kaur, Amit Anand, Arun K. Sharma, Vipan Kumar
A series of 1H-1,2,3-triazole-tethered TCS–isatin hybrid compounds were synthesized and evaluated for their antiproliferative activity against triple-negative breast cancer (TNBC).
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Redefining the role of the thiol-based agent N-acetylcysteine in human health and disease and elucidating potential advantages of its amide derivative

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D5MD01173F, Review Article

Open Access

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.

Hui-Qi Qu, Charlly Kao, Hakon Hakonarson
N-Acetylcysteine amide (NACA) reduces polarity and ionization relative to NAC, improving membrane permeability and intracellular exposure while preserving thiol-mediated redox activity and glutathione support.
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