RSC - RSC Med. Chem. latest articles

Recent Advances in the Development of Acridine-Based Hybrids with Antiproliferative Activity

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

Mahdi Gallala, Najeh Tka, Sonia Aroui
Cancer remains a leading cause of mortality worldwide, with the limitations of conventional singletarget therapies, such as severe side effects and drug resistance, driving the need for innovative treatment strategies....
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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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Beyond Acrylamide: A Structure-Guided Investigation of Covalent Warheads in the Development of CDK7 Inhibitors

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

Jiaan Shao, Yu Cao, Yiqing Huang, Yunlong Pan, Jialuo Mao, Lixin Gao, Jiankang Zhang, Huajian Zhu, Shourong Liu, Rangxiao Zhuang, Yang Liu, Yu-Bo Zhou
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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Recent advances towards BACE1 drug discovery and therapeutics design

RSC Med. Chem., 2026, Accepted Manuscript
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
Alzheimer's disease (AD) is a progressive neurodegenerative disorder characterized by cognitive decline and memory loss. A key feature of AD is the accumulation of amyloid beta (Aβ) peptides in the...
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Bicyclic Monoterpenoid-Based Orthopoxvirus Inhibitors: Design, Synthesis, and Biological Assessment of a Novel Amide Series

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

Serafim A Tishchenko, Anastasiya Sokolova, Valeriya V Samsonova, Julia G Pushkareva, Daria E Solomina, Olga I Yarovaya, Nikolay I. Bormotov, Ivan A. Moskalev, Artem Rogachev, Alina Fatyanova, Sophia Borisevich, Olga Serova, Alena Ovchinnikova, Larisa Shishkina, Alexander Agafonov, Artemiy Sergeev, Nariman Salakhutdinov, Alexander Sergeev
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. A...
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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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Quinoline/Thiazole Compounds as Selective Acetylcholinesterase Inhibitors: Synthesis and Biological Assessment

RSC Med. Chem., 2026, Accepted Manuscript
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 Ozkay, Zafer Asim Kaplancikli
Acetylcholine (ACh), acetylcholinesterase enzyme (AChE), and AChE inhibition are of great importance in the treatment of neurodegenerative diseases. When it comes to AChE inhibition, FDA-approved AChE inhibitors such as Donepezil...
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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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Rational discovery of novel phenylindole-bisamide derivatives as potent P-glycoprotein inhibitors for cancer multidrug resistance

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00030D, Research Article

Zhikun Yang, Jiajia Han, Yanhong Yang, Xue Yang, Yijing Du, Zimeng Huang, Leyi Ying, Xin Yu, Yi Hua, Qihao Wu, Xiaozhou Mou, Hong Wang
P-gp-mediated MDR hinders cancer chemotherapy. Our phenylindole-bisamide l1 shows potent MDR reversal, low cytotoxicity, broad chemosensitization. It inhibits P-gp efflux and suppresses 3D tumor growth with doxorubicin, a promising P-gp inhibitor.
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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, Accepted Manuscript
DOI: 10.1039/D5MD01001B, Research Article

Nan Wang, Lige Liu, Tao Liu, Hong Luo, Yan Long, Xinglong Yang, Youli Zhang, Qinggang Ji
Two series of compounds were designed and synthesized based on a glycine methyl ester-quinoline core scaffold combined with a fragment containing nitrogen using either an isoxazole or a piperidine carboxamide...
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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, Accepted Manuscript
DOI: 10.1039/D6MD00148C, Research Article

Chinh The Pham, Thi Tham Pham, Lien Thi Vu, Nhung Thi Dao, Loan Thi Thuy Le, Khieu Thi Tam, Vu Tuan Kien, Cao Thanh Hải, Thanh Phuong Phan, T. T. Thao, Truong Xuan Vuong, 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. The cytotoxicity of these derivatives was evaluated against...
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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, Advance Article
DOI: 10.1039/D5MD01027F, Review Article

Open Access

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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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D-Galactose-conjugated pyrimidine thioureas as potent antimicrobial agents: rapid green synthesis, structure-activity relationships and molecular modelling

RSC Med. Chem., 2026, Accepted Manuscript
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
A series of D-galactose-conjugated pyrimidine-based thioureas 8a-l was efficiently synthesized using an environmentally benign ionic liquid-microwave protocol. Optimal conditions employing [BMIM][BF4] under microwave irradiation (100 W) afforded excellent yields (up...
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Exploration of a benzothiophene scaffold for use as adjuvants with β-lactam antibiotics against methicillin-resistant Staphylococcus aureus

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D5MD01109D, Research Article

Open Access

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

Monica A. Stefaniak, Vijay S. Gondil, Emily P. Gillis, Ansley M. Nemeth, Allen G. Oliver, Roberta J. Melander, Paul M. Dunman, Christian Melander
Rising antibiotic resistance coupled with diminishing investment in antibiotic development has led to limited treatment options for multi drug-resistant bacterial infections.
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The dual functions of a nor-sesquiterpene-triazole derivative against influenza A viruses through the activation of the Nrf2/HO-1 signaling pathway and interaction with hemagglutinin

RSC Med. Chem., 2026, 17,1735-1748
DOI: 10.1039/D5MD00841G, Research Article

Shaofen Zhou, Jingyan Wei, Shixin Li, Jingnan Qiu, Shuaiqi Ma, Jian He
SF-4 inhibits influenza virus infection and the excessive inflammatory response resulting from viral infection by inhibiting NF-κB activation and activating the Nrf2/HO-1 pathway.
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A halogenated pregnenolone analogue suppresses HepG2 proliferation and induces apoptosis via PPARγ regulation

RSC Med. Chem., 2026, 17,1493-1512
DOI: 10.1039/D5MD01142F, Research Article

Shi-Ying Xu, Quan-Xing Liu, Yan Luo, Wu-He Wu, Qing Li, Shang-Gao Liao, Jun-Li Ao, Guo-Bo Xu
Halogenated pregnenolone derivative 20 exerts potent anti-HepG2 effects by inhibiting proliferation and inducing apoptosis through PPARγ modulation.
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Empowering molecular complexity via biocatalysis: emerging blueprints in the total synthesis of medicinally relevant natural products

RSC Med. Chem., 2026, 17,1397-1444
DOI: 10.1039/D5MD01011J, Review Article

Ram N. Yadav, Sovan Dey, Md. Firoj Hossain, Devalina Ray, Bimal K. Banik, Luciana C. Schmidt, Vandana Singh
Biocatalysis has ascended as a defining force in contemporary total synthesis, furnishing catalytic modalities that deliver molecular complexity with unparalleled chemo-, regio-, and stereo-control.
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Integrating green synthesis and liquid–liquid extraction of lidocaine in deep eutectic solvents

RSC Med. Chem., 2026, 17,1474-1482
DOI: 10.1039/D5MD00922G, Research Article

Open Access

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

Assunta Perri, Leonardo C. Parrotta, Stefania Gencarelli, Roberta Sole, Oana M. Dragostin, Gabriela Guillena, Maria L. Di Gioia
A DES-to-DES process enables one-pot lidocaine synthesis with solvent-free isolation, while eutectic media serve as reaction solvents, extraction agents and formulation platforms, enabling reduced PMI and greener pharmaceutical processing.
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A medicinal chemistry perspective on SIRT3 modulators in disease treatment

RSC Med. Chem., 2026, 17,1347-1368
DOI: 10.1039/D5MD01007A, Review Article

Yaoliang Li, Yuqi Bao, Yunxia Cui, Jian Zhang, Mingliang Wang
This review analyzes the structure–activity relationships, mechanisms, and activity of SIRT3 modulators, and discusses future directions like selective design, targeted delivery, and protease-mediated degradation for treating SIRT3-related diseases.
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Synthesis and biological evaluation of carabrol derivatives

RSC Med. Chem., 2026, 17,1619-1635
DOI: 10.1039/D5MD00940E, Research Article

Haidi Wu, Mengshi Zhao, Shifeng Ren, Xiaodong Mu, Yanqin Lu, Yuji Liang, Jingyong Sun
A carabrol derivative reduces the production of the inflammatory mediator NO in macrophages by inhibiting the expression of iNOS and COX-2.
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Medicinal attributes of nitrogen heterocycles directing aldose reductase selectivity and potency

RSC Med. Chem., 2026, 17,1445-1473
DOI: 10.1039/D5MD01038A, Review Article

Anita Kumari, Shyamal Kumar Manna, Kajal Rani, Rupali Kohal, Ghanshyam Das Gupta, Sant Kumar Verma
This review describes the medicinal attributes of nitrogen heterocycles, including SAR and target-interaction studies that guide their selectivity and potency for aldose reductase.
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Design, synthesis, and molecular modeling of novel thiazolopyridine-based inhibitors of enoyl acyl carrier protein reductase (InhA) as anti-Mycobacterium tuberculosis agents

RSC Med. Chem., 2026, 17,1586-1599
DOI: 10.1039/D5MD00997A, Research Article

Ahmed Sabt, Małgorzata Korycka-Machała, Asmaa F. Kassem, Abdulrahman M. Saleh, Hanaa Farag, Moataz A. Shaldam, Mohamed G. Thabit, Anna Brzostek, Magdalena Kuzioła, Bożena Dziadek, Hoda Atef Abdelsattar Ibrahim, Xinsheng Lei, Jarosław Dziadek, Mohamed A. Abdelrahman
The updated guidelines from the World Health Organization highlight that treatment options for multidrug-resistant tuberculosis (MDR-TB) remain limited due to the scarcity of effective drugs.
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3-(Pyridine-3-ylmethylene)chroman-4-one and tetralone derivatives: synthesis, Mycobacterium tuberculosis CYP121A1 enzyme inhibition and antimycobacterial activity vs drug-sensitive and drug-resistant strains

RSC Med. Chem., 2026, 17,1672-1686
DOI: 10.1039/D5MD00738K, Research Article

Open Access

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

Lama A. Alshabani, Jabril M. Abdali, Alistair K. Brown, Damião Pergentino de Sousa, Sam Willcocks, Amit Kumar, Ahmed Y. G. Alhejaili, D. Fernando Estrada, Claire Simons
Chromanone derivatives displayed strong CYP121A1 binding affinity while the tetralone derivatives were very effective antimycobacterial activity against multidrug resistant Mtb.
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Structure–activity landscape of Nurr1 (NR4A2) modulators: medicinal chemistry strategies for neurodegenerative disease intervention

RSC Med. Chem., 2026, 17,1369-1396
DOI: 10.1039/D5MD01177A, Review Article

Sahil Jaidka, Ankush Kumar, Thakur Gurjeet Singh, Rohit Bhatia, Rajesh Kumar Singh
Nurr1 modulators show promise for neurodegenerative diseases by improving neuroprotection and suppressing neuroinflammation. This review summarizes scaffold-based SAR and highlights challenges in NR4A selectivity and CNS translation.
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Leveraging fragment-based drug discovery to advance 3D scaffolds into potent ligands: application to the histamine H1 receptor

RSC Med. Chem., 2026, 17,1483-1492
DOI: 10.1039/D5MD01081K, Research Article

Open Access

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

Tom Dekker, Oscar P. J. van Linden, Herman D. Lim, Mabel E. Dekker, Henry F. Vischer, Rob Leurs, Tiffany van der Meer, Maurice C. M. L. Buzink, David J. Hamilton, Barbara Zarzycka, Elwin Janssen, Maikel Wijtmans, Iwan J. P. de Esch
Fragment-based drug discovery enables translation of novel (3D) chemistries into biologically relevant hit matter, as demonstrated by the identification and optimization of a cyclobutane-based 3D fragment into a potent histamine H₁ receptor ligand.
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Novel glycine amides, semicarbazides and fluoroallylamines as inhibitors of the amine oxidase vascular adhesion protein-1 (VAP-1)

RSC Med. Chem., 2026, 17,1709-1728
DOI: 10.1039/D5MD01008J, Research Article

Open Access

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

Timo Pöstges, Jan Kampschulze, Walburga Hanekamp, Marcel Bermúdez, Matthias Lehr
Vascular adhesion protein-1 (VAP-1), also known as copper-containing amine oxidase 3 (AOC3), is an enzyme implicated in the pathogenesis of various diseases.
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Structure–activity optimization of N-arylindole GPR52 agonists for enhanced antipsychotic efficacy: design, synthesis, and pharmacological evaluation

RSC Med. Chem., 2026, 17,1749-1757
DOI: 10.1039/D5MD00944H, Research Article

Xiaojie Hu, Qingshan Gu, Qiuyu Xiong, Donglei Chen, Qingkun Wu, Lu Zheng
A series of N-arylindole GPR52 agonists were developed via linker, head, and tail optimization, showing moderate to good activity and antipsychotic potential. SAR highlights the importance of balanced flexibility and hydroxyl groups.
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Synthesis of new trans-ferulic acid derivatives as potential anticancer agents and VEGFR-2 inhibitors

RSC Med. Chem., 2026, 17,1636-1650
DOI: 10.1039/D5MD00980D, Research Article

Asmaa N. Mohie, Mahmoud A. Doheim, Ragab A. El Masry, Ayman M. Gomaa, Rofaida Salem, Haytham O. Tawfik, Wagdy M. Eldehna
By using –OH blocking, seven TFA derivatives were created. Compound 4e regulated AFP, BCL-2, caspase-3, and P53, inhibited VEGFR-2 in docking, and exhibited the maximum cytotoxicity against HepG2, Hep3B, and Huh7 with a safe profile.
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Endoperoxide delivered singlet oxygen: the future of PDT, without light or oxygen

RSC Med. Chem., 2026, 17,1729-1734
DOI: 10.1039/D5MD00887E, Research Article

Open Access

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

Wanwan Wang, Lei Wang, Rensong Sun, Xiao Qian, Ziang Liu, Engin U. Akkaya
Chemically generated singlet oxygen via cycloreversion reaction of aromatic endoperoxides is poised to evolve into a highly promising therapeutic protocol.
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2,5-Diazabicyclo[2.2.1]heptane in medicinal chemistry: a treasure trove of therapeutic opportunities

RSC Med. Chem., 2026, 17,1299-1346
DOI: 10.1039/D5MD00992H, Review Article

Pranav Kumar Ambast, Saumya Kapoor, Rudradip Das, Deep Rohan Chatterjee, Amit Shard
2,5-Diazabicyclo[2.2.1]heptane (2,5-DBH) is a conformationally rigid bicyclic diamine and a privileged scaffold in medicinal chemistry, enabling diverse synthetic modifications and broad therapeutic applications across multiple disease areas.
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Discovery of RP-37 analogues as potent, selective irreversible inhibitors targeting DNA polymerase theta (POLθ)

RSC Med. Chem., 2026, 17,1694-1708
DOI: 10.1039/D5MD00830A, Research Article

Zhenwei Wang, Mengyuan Qiu, Deming Liu, Yanzhen Yu, Dongyan Gu, FengMin Zhang, Rong Sheng
Enzymatic IC₅₀ = 1.54 nM (POLθ polymerase domain). Cellular IC₅₀ = 1.16 μM (DLD-1 BRCA2^−/−; ∼5-fold enhancement). Sustained target engagement via irreversible inhibition.
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Exploring pyrazoline-thiophene hybrids as CDK2 inhibitors: synthesis, mechanism, biological studies, and computational insights

RSC Med. Chem., 2026, 17,1651-1671
DOI: 10.1039/D5MD00910C, Research Article

Heba M. Abosalim, Tarek F. El-Moselhy, Nabaweya Sharafeldin, Mohamed S. Nafie, Mohamed K. Diab, Mervat H. El-Hamamsy, Haytham O. Tawfik
Novel pyrazoline-linked thiophenes were synthesized as anticancer agents. Lead compound 4p showed sub-micromolar cytotoxicity, induced CDK2-mediated apoptosis and cell-cycle arrest, and reduced tumor burden in vivo with low toxicity.
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Investigating the role of cytochrome bd oxidases in the antibacterial activity of madecassic acid and derivatives thereof

RSC Med. Chem., 2026, 17,1513-1520
DOI: 10.1039/D5MD01116G, Research Article

Open Access

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

Samantha A. Henry, Geraud N. Sansom, Thao Thi Phuong Tran, Ryan A. Boughton, Guy Joiner, Calum M. Webster, H. Ireshika C. de Silva, Michelle D. Garrett, Christopher J. Serpell, Gary K. Robinson, Mark Shepherd
Madecassic acid is found to have activity against cytochrome proteins found only in bacteria, offering a new route to antibiotics.
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Oxyprenyl–chalcones as antibacterial hits: design of experiments-optimized synthesis, antibacterial evaluation, early drug-like profiling and biodegradability prediction

RSC Med. Chem., 2026, 17,1573-1585
DOI: 10.1039/D5MD00839E, Research Article

Ludovica Marotta, Francesca Maria Pia Rita Giammarino, Brondon Brandly Senenou Tambou, Valeria Tudino, Stefania Butini, Lorenza Broccardo, Sacha Michèle Idriss Cancade, Jean-Denis Docquier, Federica Perego, Nicoletta Basilico, Lorenzo Raffellini, Sheraz Gul, Gabriele Carullo, Sandra Gemma, Giuseppe Campiani
The escalating threat of antimicrobial resistance (AMR) compels the development of novel antibiotics with broad spectrum activity and environmentally responsible degradation profiles.
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Efficient log P determination by automated, spatially encoded 19F NMR spectroscopy

RSC Med. Chem., 2026, 17,1550-1558
DOI: 10.1039/D5MD00678C, Research Article

Open Access

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

Susanna H. Wood, Fiona Gordon, Robin S. Stein, Mark J. Howard, John A. Parkinson
A method for measuring log P of fluorinated molecules by ¹⁹F NMR under full instrument automation. Placing an advanced NMR technique in the hands of synthetic chemists for simple, efficient data acquisition.
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Design and optimization of simplified inhibitors targeting Escherichia coli and Klebsiella pneumoniae IspE

RSC Med. Chem., 2026, 17,1687-1693
DOI: 10.1039/D5MD00874C, Research Article

Open Access

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

Danica J. Walsh, Rawia Hamid, Tim Giele, Norbert Reiling, Matthias Rottmann, Mostafa M. Hamed, Anna K. H. Hirsch
Simplified amide IspE inhibitors restore potency against Klebsiella pneumoniae and Escherichia coli, offering synthetically accessible antibacterial hits.
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A dialogue on innovation in anticancer drug discovery

RSC Med. Chem., 2026, 17,1246-1251
DOI: 10.1039/D5MD01040C, Opinion

Susanta Samajdar
From cytotoxic agents to proximity-inducing modalities and advanced drug conjugates.
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CNS penetrant TEAD1,2,4 inhibitor MSC-4070 derived from phenotypic screening hit optimization

RSC Med. Chem., 2026, 17,1559-1572
DOI: 10.1039/D5MD00928F, Research Article

Timo Heinrich, Carl Petersson, Jakub Gunera, Alessia Gambardella, Daniel Schwarz, Sakshi Garg, Heike Schilke, Thomas Weitzel, Christian Kolb, Uwe Anlauf, Vivian Reither, Corinna Rettig, Beate Opelt, Andrea Delp, Nicole Wildner, Pedro M. F. Sousa, Filipe Freire, Tiago M. Bandeiras, Dirk Wienke
N-Methylation decreased efflux in the Caco-2 assay without compromising activity, yielding the brain-penetrant TEAD inhibitor MSC-4070.
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Inhibitors of type II NADH-dehydrogenase, cytochrome bd oxidase, and ATP synthase for anti-tubercular response

RSC Med. Chem., 2026, 17,1271-1288
DOI: 10.1039/D5MD00950B, Review Article

Pallavi Saha, Mohit Kumar, Deepak K. Sharma
The identification of novel anti-tubercular agents capable of eliciting lethal responses against drug-resistant tuberculosis is critically needed to address the escalating mortality from tuberculosis.
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Recent progress of METTL3 inhibitors for cancer therapeutics: design, optimization and potential applications

RSC Med. Chem., 2026, 17,1289-1298
DOI: 10.1039/D5MD00867K, Review Article

Yun Zhang, Mengxiang Quan, Qinlan Chen, Hongdi Han, Xianling Zhang, Xiangwei Xu, Zunyuan Wang
METTL3 plays an important role in AML and other cancers. This review summarized the strategies for discovering and optimizing METTL3 inhibitors, and looked forward to the potential application prospects of METTL3 inhibitors in clinical practice.
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Novel isoxazolone derivatives as acetylcholinesterase inhibitors: design, synthesis, in silico and in vitro evaluation

RSC Med. Chem., 2026, 17,1600-1618
DOI: 10.1039/D5MD00890E, Research Article

Nitasha Gohar, Adil Saeed, Muzaffar Abbas, Sana Ayaz, Iqra Zulfiqar, Syed Muzzammil Masaud, Humaira Nadeem
Acetylcholinesterase (AChE) plays a pivotal role in Alzheimer's disease by accelerating acetylcholine breakdown, leading to cognitive decline.
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Targeted degradation of Pin1 by an antagonistic peptide enhances gemcitabine therapy in pancreatic cancer

RSC Med. Chem., 2026, 17,1537-1549
DOI: 10.1039/D5MD00970G, Research Article

Mengting Chen, Xiangyu Chu, Haipeng Zhao, Lilusi Ma, Jie Meng, Yanlian Yang, Qiaojun Fang, Xiaocui Fang, Chen Wang
PIPWF peptide binds to the Pin1 protein through multi-site interactions, thereby inducing its conformational change and leading to subsequent degradation.
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Ferrocenyl ferroptosis inducers as an emerging class of anticancer agents: a mini review

RSC Med. Chem., 2026, 17,1252-1270
DOI: 10.1039/D5MD00935A, Review Article

Mateusz Klarek, Aryan Gautam, Konrad Kowalski
Ferroptosis is one of the regulated cell death pathways. Molecular mechanisms underlying ferroptosis involve iron-dependent lipid peroxidation, which results in cell-deleterious membrane damage.
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Kupffer cell M2-like polarization increases liver metastatic burden via the uptake of exosomal KRAS mutant protein from hypoxic colorectal carcinoma cells

RSC Med. Chem., 2026, 17,1521-1536
DOI: 10.1039/D5MD00897B, Research Article

Yu You, Zhihao Feng, Jiao Lu, Jie Xu, Ke You, Fuyao Liu, Tianzhu Wu, Hua Song, Zuojin Liu
Kupffer cell M2-like polarization driven by exosomal mutant KRAS via AKT signaling is a key factor in colorectal cancer liver metastasis.
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From bolinaquinone, a marine hydroxyquinone sesquiterpene, to naphthoquinones with clathrin inhibitory effects

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D5MD00900F, Research Article

Nicholas S. O'Brien, Azadeh Ghods, Jing Xue, Mary J. Garson, Ken W. L. Yong, Jennette A. Sakoff, Jayne Glibert, Megan Chircop, Uwe Fink, Volker Haucke, Phillip J. Robinson, Adam McCluskey
Bolinaquinone (1) is cited as a clathrin inhibitor; applying a DFT approach, naphthoquinones with similar electronic properties were designed and shown to be potent inhibitors of the clathrin N-terminal domain–amphiphysin interaction, e.g. 23.
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Design, synthesis and biological evaluation of benzoyl hydrazone derivatives as anticancer agents inducing ROS-associated mitochondrial apoptosis

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D5MD01046B, Research Article

Rongbin Wei, Xin Wang, Yamin Ding, Suting Zhu, Richmond Kwame Frimpong Asiedu, Muzi Li, Haitao Qian, Yifei Gu, Bailing Jiang
Compound Q-11 shows potent nanomolar antiproliferative activity in gastric cancer cells and induces ROS accumulation, mitochondrial dysfunction and cytoskeletal disruption.
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The effects of bioisostere substitution on the antimicrobial and physicochemical properties of supramolecular self-associating amphiphiles

RSC Med. Chem., 2026, Advance Article
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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Extending the architecture of bolaamphiphilic disinfectants: an investigation of octenidine and isooctenidine analogs

RSC Med. Chem., 2026, Advance Article
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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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, Advance Article
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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Verbenone-based selenophene derivatives as potential anti-cancer agents: synthesis and biological evaluation in 2D and 3D A549 cell models

RSC Med. Chem., 2026, Advance Article
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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Design and biological evaluation of triagonist GLP-1R/GCGR/GIPR peptides as potential therapeutic agents for diabetes and obesity

RSC Med. Chem., 2026, Advance Article
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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Pharmacological landscape of carbolines: a holistic view

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00057F, Review Article

Yao Zhang, Fule Wu, Muneeb Ur Rehman, Sihui Long
This review comprehensively explores the design, synthesis, and pharmacological activities of carboline isomers reported between 2000 and 2025, with a particular emphasis on their key bioactivities, encompassing anticancer, neuroprotective, antiparasitic, and antimicrobial.
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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, Advance Article
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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