RSC - RSC Med. Chem. latest articles

Inhibition effects and binding behavior of alginate oligosaccharides on tyrosinase and elastase: multi-spectroscopic approaches and zebrafish evaluation

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00183A, Research Article

Hangen Li, Shuyi Liang, Yuanyi Cen, Yan Liang, Xuetao Xu
(1) AOSs were inhibitors on tyrosinase and elastase. Multi-spectroscopic and docking approaches revealed inhibition interaction of AOSs on tyrosinase and elastase. (2) AOSs displayed the ability of melanin inhibition and ROS clearance.
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Design, synthesis, and X-ray structural studies of potent SARS-CoV-2 Mpro inhibitors containing tetrahydroisoquinoline-3-carboxamides as P2 ligands

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00312E, Research Article

Open Access

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

Arun K. Ghosh, Ashish Sharma, Satyanarayana Iddum, Sydney N. Bogan, Uttara Jayashankar, Emma K. Lendy, Shin-ichiro Hattori, Nobuyo Higashi-Kuwata, Hiroaki Mitsuya, Andrew D. Mesecar
A series of potent SARS-CoV-2 Mpro inhibitors is designed, synthesized and evaluated. Inhibitor 5j and the X-ray structure of the SARS-CoV-2 Mpro–5j complex are represented.
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Synthesis, molecular modelling and evaluation of (−)-isopulegol-based 2,4-diaminopyrimidines as promising aurora kinase inhibitors

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00278A, Research Article

Open Access

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

Tam Minh Le, Nikoletta Szemerédi, Gabriella Spengler, Minh Canh Nguyen, Huynh Nguyen Khanh Tran, Khac-Minh Thai, Zsolt Szakonyi
(−)-Isopulegol-based 2,4-diaminopyrimidines were prepared and evaluated for cytotoxicity against human colon adenocarcinoma cell lines. Molecular docking analysis indicated their interaction with the aurora kinase A receptor.
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Ring-Opening Simplification of Thiazolyl-Pyrazoline-Triazole Hybrids: Synthesis, SAR and Antifolate Mechanism Against Leishmania major

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00382F, Research Article

Esraa A Abdelsalam, Wagdy M. Eldehna, Radwan El-Haggar, Sherif Hammad, Nicolas MASURIER, Tamer M Ibrahim, Kikuko Amagase, Sherry N Nasralla, Hatem A. Abdel-Aziz, Adnan Bekhit
Leishmaniasis, a neglected tropical disease with a severely limited and toxicity-prone therapeutic arsenal, urgently demands structurally innovative drug candidates. Capitalizing on the well-established antileishmanial potential of thiazole, triazole, and pyrazole...
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Drug Repurposing of Fluvastatin as a DP2 Antagonist: An Ensemble Learning Strategy with In Vitro Cellular Functional Validation

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00403B, Research Article

GuoHui Wei, Zhuo Sun, Yuanxu Gao, Jia Heng, Wenyang Lu, Zixing Zou
We present a framework to repurpose FDA-approved drugs as DP2 antagonists for asthma, using a two-stage strategy. First, we train and evaluate eight models—five machine learning algorithms and three graph...
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From dual norepinephrine-dopamine reuptake inhibition to selective dopamine reuptake inhibitors: a case of aromatically substituted N,2-cyclopentylamines

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00112B, Research Article

Open Access

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Majlen A. Dilweg, Willem Jespers, Ameya S Kasture, Rongfang Liu, Tamara A. M. Mocking, Jelle G Van Der Ploeg, M M Baselier, Gerard Van Westen, Thomas Hummel, Sonja Sucic, Adriaan P. IJzerman, Laura H. Heitman, Daan van der Es
Dopamine (DA) is essential for motor control, mood, motivation, and reward in the central nervous system. It functions through receptor activation and is regulated by the dopamine transporter (DAT, SLC6A3),...
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Combining β2-AR agonism with butyrylcholinesterase inhibition, a synergistic neuroprotective action against Alzheimer's disease

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00250A, Research Article

Alice Wang, Thomas Curel, Sylvie Claeysen, Valentin Travers-Lesage, Marie Elodie Hélène Cadot, Audrey Davis, Jana Sopkova de Oliveira Santos, Fabrice Modeste, Xavier Brazzolotto, Florian Nachon, Patrick Dallemagne, Marc Since, Christophe Rochais
Alzheimer’s disease (AD) is a multifactorial neurodegenerative disorder for which the current treatments remain largely symptomatic. Pleiotropic prodrug strategies offer a promising approach to address this complexity, combining complementary pharmacological...
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Exploring the Antimycobacterial Profile of N-Alkyl Imidazoles

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00418K, Research Article

Alejandro I. Recio-Balsells, Gabriel Di Gresia, Marcelo Luciano Merli, Julia Alejandra Cricco, Hector R. Morbidoni, Guillermo R Labadie
The emergence of drug-resistant Mycobacterium tuberculosis strains and non-tuberculous mycobacteria (NTM) species such as Mycobacterium abscessus, highlights the urgent need for new chemotypes with broad-spectrum antimycobacterial activity. In this study,...
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Discovery of Novel Indazole Derivatives with Antineuroinflammatory Activity

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00270F, Research Article

Qing qing Zhang, Xixi Hou, Xuanwei Zhang, Yimian Wang, Yaquan Cao, Lan Wang, Longfei Mao
This study focuses on the critical role of microglia-mediated neuroinflammation in various neurological disorders. Utilizing the indazole heterocycle-a scaffold known for its structural plasticity and multi-target potential-as the core structure,...
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Discovery of Novel SIRT3 Inhibitors with MLLr Leukemia Inhibitory Potency

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00249H, Research Article

Shaopeng Chen, Xinyang Wei, Honggang Li, Jiangying Cao, lei zhang
SIRT3 has emerged as a therapeutic target for the treatment of leukemia. Based on our previously identified lead compound, structural modification was performed in the current study. A total of...
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Synthesis and Bioevaluation of Substituted 2,11-dihydroimidazo[1′,5′:1,2]pyrido-[3,4-b]indoles as antiplasmodial and antiproliferative agents

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00085A, Research Article

Adilakshmi Vutla, Akash Pandey, Amanullah Sayeed, Richa Shukla, Ashan Manhas, Niti Kumar, Sanjeev Meena, Dipak Datta, Sanjay Batra
The synthesis and bioevaluation of a new series of substituted 2,11-dihydroimidazo[1’,5’:1,2]pyrido-[3.4-b]indoles as antiplasmodial and antiproliferative agents are described. Several compounds (16aaf, 16abf, 16acf, 16adq, 16aeo, and 16afe ) exhibited significant...
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1,8-Naphthalimide Heterocycles as Skeleton Structures Targeting Cancer: Insights into Synthesis, Bioactivity, SAR, and Future Directions

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00016A, Review Article

Jitendra Choudhary, Gurdeep Kaur, Iqubal Singh
1,8-Naphthalimide-based heterocyclic compounds have emerged as an important class of anticancer agents owing to their strong DNA-intercalating ability, topoisomerase inhibition, and capacity to modulate multiple cellular pathways. This review aims...
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Design, synthesis, and in silico and in vitro evaluation of novel complex naphthalimide–ciprofloxacin hybrids as next-generation antimicrobial agents

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00193A, Research Article

Dharmendra Singh, Ankita Singh, Harikesh Kumar Gupta, Sajida Banoo, Sumit Maurya, Vishwakarma Krishna Ramesh, Khushbu Khushbu, Ambrish Kumar, Jyoti Kumari, Avisek Mahapa, Shruti Trivedi, Rajnish Kumar, Shashikala Verma, Arunava Manna
A series of ciprofloxacin–naphthalimide hybrid drugs as novel antibacterial agents were synthesized and screened for their intriguing antibacterial properties.
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Triarylphosphonium-conjugated Sn(IV)-porphyrins for antimicrobial photodynamic therapy: impact of substituents on lipophilicity, aggregation, and photoantibacterial activity

RSC Med. Chem., 2026, 17,3115-3123
DOI: 10.1039/D6MD00300A, Research Article

Open Access

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

Gayathri MP, Nandhakumar Muruganandam, Sutharsan Govindarajan, Balaji Babu
Antimicrobial photodynamic therapy is an effective approach to counteract bacterial infections that are not possible to be treated through antibiotics.
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Identification and structure–activity relationship analysis of minimal fusion inhibitors targeting measles virus F protein

RSC Med. Chem., 2026, 17,3100-3114
DOI: 10.1039/D6MD00211K, Research Article

Open Access

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

Kazuya Kobayashi, Yuki Yamaguchi, Mizuki Itahara, Kazushige Hirata, Keisuke Aoki, Naoya Iwamoto, Hironori Hayashi, Eiichi Kodama, Shinya Oishi
Optimization of a measles virus HR2-derived fusion inhibitor yielded a short peptide with potent antiviral activity and revealed key residues governing interactions with HR1.
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Investigation of 2,3-diaryl-1,3-thiazolidin-4-ones as promising agents for reducing lipid accumulation in liver cells through AMPK activation: synthesis, in vitro, in silico and lipidomic studies

RSC Med. Chem., 2026, 17,3054-3073
DOI: 10.1039/D6MD00226A, Research Article

Arnatchai Maiuthed, Nichawadee Sandech, Meng Chieh Yang, Sucheewin Krobthong, Pattarawit Rukthong, Kittisak Sripha, Witcha Imaram, Chaiyawat Aonsri
A series of 2,3-diaryl-1,3-thiazolidin-4-ones was synthesized and identified as promising AMP-activated protein kinase (AMPK) activators with potential lipid-lowering activity.
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Ruthenium(II) polypyridyl complexes and the DNA damage response: mechanisms and therapeutic implications

RSC Med. Chem., 2026, 17,2726-2742
DOI: 10.1039/D6MD00154H, Review Article

Open Access

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Martin R. Gill
This review summarises the design of ruthenium(II) polypyridyl complexes (RPCs) as pharmacological DNA-targeting agents, linking binding mode, DDR pathway activation, and cancer cell fate.
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Design, synthesis, and biological evaluation of novel SN38–sulfonamide conjugates as Topo I/CA IX dual inhibitors inducing ferroptosis in colorectal cancer

RSC Med. Chem., 2026, 17,3012-3025
DOI: 10.1039/D6MD00290K, Research Article

Xinyu Zhao, Anna Ye, Yujie Wang, Yeying Qiu, Shiyan Liu, Liyu Wei, Feng Qin, Ye Zhang, Rizhen Huang
A series of novel SN38–sulfonamide conjugates were designed and synthesized as carbonic anhydrase IX (CA IX) and topoisomerase I (Topo I) dual inhibitors for colorectal cancer therapy.
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Light-controlled inhibition of Gram-positive bacteria by photoswitchable amphiphilic lipids (PALs)

RSC Med. Chem., 2026, 17,3042-3053
DOI: 10.1039/D6MD00096G, Research Article

Open Access

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Guilherme F. S. Fernandes, Seong-Heun Kim, Charlotte K. Hind, Jessica Furner-Pardoe, Janis Romanopulos, Christian D. Lorenz, A. James Mason, J. Mark Sutton, Daniele Castagnolo
Photoswitchable amphiphilic lipids (PALs) enable reversible light-controlled inhibition of Gram-positive bacteria. Azobenzene photoisomerization modulates membrane insertion, switching antibacterial activity on or off depending on alkyl chain length.
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Development of novel chalcone-based quinazoline derivatives as dual VEGFR-2 and EGFR inhibitors

RSC Med. Chem., 2026, 17,2984-3002
DOI: 10.1039/D6MD00179C, Research Article

Zainab M. Elsayed, Haytham O. Tawfik, Loah R. Hemeda, Mohamed S. Nafie, Hadia Almahli, Rehan Monir, Ikhlas A. Sindi, Eslam B. 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.
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Small-molecule therapeutics for diabetic retinopathy: from VEGFR inhibitors to emerging non-VEGF targets

RSC Med. Chem., 2026, 17,2860-2885
DOI: 10.1039/D6MD00069J, Review Article

Yan Li, Wenfang Zhang, Yinliang Bai, Honghua Zhang
Small-molecule therapy for diabetic retinopathy is advancing from VEGFR inhibitors to non-VEGF targets, with success increasingly determined by ocular PK/PD optimization, route-specific delivery, and scaffold design rather than potency alone.
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Structure-guided optimisation of fenofibrate-derived oxidative phosphorylation inhibitors to modify tumour hypoxia

RSC Med. Chem., 2026, 17,2925-2935
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, 17,2743-2767
DOI: 10.1039/D5MD01089F, Review Article

Yiran Zhou, Jinqu Li, Yiou Mei, Yuzhu Chen, Fengxia Sun, Yunfei Du
Numerous sulfone/sulfoxide-containing drugs are FDA-approved for clinical use, and these moieties remain of great interest. This review overviews these agents, focusing on their targets, activities, and SAR studies.
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New terpenyl–cinnamoyl–hydrazone analogues of cannabidiol with potent antinociceptive effect

RSC Med. Chem., 2026, 17,2936-2944
DOI: 10.1039/D6MD00185H, Research Article

João Pedro Barros de Paiva, Anna Carolina Pereira Lontra, Rachel Marins Campos, Eduardo Araújo, Thais Biondino Sardella Giorno, Mikaela Lucinda de Souza, Graziella dos Reis Rosa Franco, Claudio Viegas, Patrícia Dias Fernandes
In this study, novel terpenyl–cinnamoyl–hydrazone analogs were synthesized and evaluated for antinociceptive potential in preclinical nociception models.
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Addressing multidrug-resistant bacterial infections with iridium-based theragnostic agents

RSC Med. Chem., 2026, 17,3003-3011
DOI: 10.1039/D6MD00120C, Research Article

Rama Karn, Mahesmita Sahoo, Sayantani Biswas, Suravi Chauhan, Ajay Kumar Nag, Soham Basu, Srikanta Patra, Debasis Manna
An amphiphilic iridium(III) complex self-assembles into cationic nanoaggregates that disrupt bacterial membranes and facilitate selective fluorescence imaging, providing a promising theragnostic platform to combat antimicrobial resistance.
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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, 17,2907-2924
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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Emerging cellular uptake mechanisms of bRo5 PROTACs

RSC Med. Chem., 2026, 17,2850-2859
DOI: 10.1039/D6MD00243A, Review Article

Toshihiko Tashima
CD36-mediated endocytosis provides an alternative uptake pathway for bRo5 PROTACs beyond passive diffusion.
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Regioselective triclocarban-catalyzed synthesis of spiroindeno- and spirooxindolo-pyrrolizidines with apoptosis induction in MCF-7 cells

RSC Med. Chem., 2026, 17,3026-3041
DOI: 10.1039/D6MD00132G, Research Article

V. Rukyanaik, Samata Pradhan, Chandraiah Godugu, Srinu Tothadi, Kadiyam Rama Krishna, Ravinder Pawar, Srinivas Basavoju
The design of new molecules from known structural motifs via [3 + 2] cycloaddition is a widely used strategy in modern drug discovery.
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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, 17,2945-2962
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.
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Synthesis-guided design and discovery of alkylated indoles with antibacterial activity against MRSA

RSC Med. Chem., 2026, 17,3074-3099
DOI: 10.1039/D6MD00221H, Research Article

Auqib Rashid, Vishwani Jamwal, Bilal A. Bhat, Kuljit Singh, Showkat Rashid
This research work presents a framework for rational design, synthesis, and detailed biological evaluation of a series of C-3 alkylated indole derivatives as potential antibacterial agents against methicillin-resistant Staphylococcus aureus (MRSA).
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Recent advances in the development of acridine-based hybrids with antiproliferative activity

RSC Med. Chem., 2026, 17,2768-2849
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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A comprehensive study of novel pregnenolone-isoxazole hybrids as selective inducers of mitochondrial apoptosis in breast cancer cells

RSC Med. Chem., 2026, 17,2963-2983
DOI: 10.1039/D6MD00076B, Research Article

Victoria Malakhova, Alexander Scherbakov, Diana Salnikova, Alvina Khamidullina, Danila Sorokin, Dmitry Vasilenko, Elena Chernoburova, Elena Averina, Igor Zavarzin, Yulia Volkova
The lead compound induced mitochondria-dependent apoptosis and demonstrated IC₅₀ values of 2.6 μM or lower against MCF7, MCF7/HT2, MDA-MB-231, and HCC1954 breast cancer cell lines under both normoxic and hypoxic conditions.
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Bisarylthiourea comprising cycloalkyl-thiophene-3-carboxylate derivatives as potential human toll-like receptor (TLR2) agonists: design, synthesis, and structure–activity relationship enabling the switch from TLR2/1 to TLR2/6 activation

RSC Med. Chem., 2026, 17,2886-2906
DOI: 10.1039/D5MD01078K, Research Article

Munugala Chandrakanth, Yoshikazu Honda-Okubo, Arya C. G., Deepak B. Salunke, Nikolai Petrovsky, Janardhan Banothu
A series of bisarylthiourea (BAT) comprising cycloalkyl-thiophene-3-carboxylate derivatives was rationally designed, synthesized, and evaluated as potential human TLR2 agonists.
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Design and synthesis of N-3-substituted quinazolinone derivatives as anticancer agents targeting EGFR

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D5MD01148E, Research Article

Pritam Maity, Poonam Yadav, Joydeep Chatterjee, Madhurendra Kumar Katiyar, Umashanker Navik, Raj Kumar
A series of new N-3-substituted quinazolinones targeting epidermal growth factor receptor (EGFR) was designed and synthesized for anticancer evaluation.
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3-Hydroxypyrimidine-2,4-dione derivatives as monkeypox virus resolvase (Mpr) inhibitors

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00285D, Research Article

Muhammad Syafiq Bin Shahari, Jacob P. Mahoney, Ziyue Wang, Anil Pant, Ajit Jagtap, Roshan Katekar, Jiashu Xie, Zhilong Yang, Zhengqiang Wang
New HPD analogs potently inhibited purified Mpr in the low nM to sub μM range, but produced modest Gluc reduction due to poor permeability.
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Structure–activity relationship for calanthoside, a potential hair-growth stimulant with an indole 2-S-,3-O-bis-glucoside structure. Part 1: role of two glucoside moieties in promoting HFDPC proliferation

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00273K, Research Article

Open Access

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Riko Suzuki, Katsuki Takashima, Yoshiaki Manse, Haruto Nishikawa, Mina Ashidate, Shinsuke Marumoto, Fumihiro Ishikawa, Toshio Morikawa, Genzoh Tanabe
The development of new and effective drugs for treating androgenetic alopecia (AGA) remains challenging.
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Research process of iminosugars in glycosidase inhibition and hypoglycemic activity

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00293E, Review Article

Chao-Na An, Mei-Qi Yang, Xin-Ran Song, Hai-Shan Zhao, Fangqian Yin, Meng-Yue Li, Ke-Rang Wang
Multivalent effect or glycocluster effect is a natural phenomenon, especially for the carbohydrate-protein interactions.Multivalent glycoclusters have been widely studied, which show significantly stronger binding interactions with proteins compared with the...
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Polypharmacology in multi-drug-resistant tuberculosis: current scenario and future promise

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00029K, Review Article

Itibaw Farooq, Hadiya Amin Kantroo, Mohammad Iqbal Banday, Zahoor Ahmad
This review provides a consolidated overview of the polypharmacological strategies against MDR-TB, covering the design approaches, current progress, promising molecules, and unresolved gaps.
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Rational design of an environment-sensitive fluorescent probe for monitoring butyrylcholinesterase activity and its application in Alzheimer's disease

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00363J, Research Article

Ning Guo, Feng Wang, Yu Wang, Jiahao Du, Qingwen Zhang, Wenting Cao, Jiongtao Su, Fenqin Zhao, Junfeng Wang, Xiaobin Pang, Yuemin Zhou, Lin Yan
LY36 integrates selective BChE inhibition with environment-sensitive fluorescence for real-time visualization of Alzheimer's pathology in biological models.
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Bismuth drug as an antibiotic adjuvant to inhibit biofilm formation via a dual mechanism

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00204H, Research Article

Jingru Li, Peng Gao, Richard Yi-Tsun Kao, Hongyan Li, Hongzhe Sun
Bismuth targets terminal oxidases CyoC and CydA, impairing energy production and elevating NO. This triggers c-di-GMP degradation and upregulates rpoS via reduced cAMP–CRP, synergistically inhibiting B. cepacia biofilm formation.
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Novel hydroxytyrosol esters as potential anti-amyloid and neuroprotective agents for Alzheimer's disease

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00265J, Research Article

Open Access

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Ioanna Kalpaktsi, Anthi Panara, Barbara Mavroidi, Giorgos Garcia Niforos, Amalia D. Kalampaliki, Ioanna C. Vlachogianni, Eleftheria A. Georgiou, Elizabeth Fragopoulou, Anthony Tsarbopoulos, Alexios-Leandros Skaltsounis, Maria Pelecanou, Kontantinos Palikaras, Evagelos Gikas, Ioannis K. Kostakis
Hydroxytyrosol-derived esters emerge as stable oleuropein mimetics that inhibit Aβ aggregation and confer in vivo neuroprotection.
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From AlphaFold to site-selective inhibition of DNA methylation in glioblastoma multiforme

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D5MD00988J, Research Article

Jean-Maxime Besson, Alain Chavanieu, Arulraj Nadaradjane, Pierre-François Cartron, Marie Lopez
Targeting specific protein–protein interactions, particularly those involving DNA methyltransferases (DNMTs), offers a promising strategy to resensitise glioblastoma multiforme cells to temozolomide.
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New roxadustat amino acid drug conjugation derivatives: molecular docking, molecular dynamics simulation and in vitro assay

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00094K, Research Article

Marjan Samadi, Azizollah Habibi, Leila Karami, Soroush Sardari, Ramin Ebrahimi Kiasari, Ghazaleh Ghavami, Mohammad Shahcheragh
In this study, a series of novel amino acid drug conjugates (ADCs) of roxadustat were designed to inhibit the prolyl hydroxylase domain (PHD) enzyme.
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Targeting Hexokinase 2 for Cancer Therapy: Advances, Limitations, and Emerging Opportunities in Inhibitors and Degraders

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00103C, Review Article

Xianglong Wang, Baohu Li, Wei-Wei Yao, Jinfei Yang
Hexokinase 2 (HK2) is an important target in cancer metabolism because it supports both glycolytic flux and mitochondria-associated survival signaling. In recent years, multiple HK2-directed strategies have emerged, including active-site...
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Discovery of a Potent Dual Target CDK8 and Cyclic C PROTAC Degrader for Treatment of Colorectal Cancer

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00281A, Research Article

Xingxing Zhang, Qingsong Chen, Cencen Lei, Da Long Jin, Hao Dong Liu, Yumeng Wang, Chenyu zhao, Liping Zhi, Xinhua Liu
CDK8 exerts important physiological functions, particularly in CRC, by forming intermediate complexes with Cyclic C, MED12, and MED13. In this work, different from the design of traditional single CDK8 protac...
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Novel urea- and piperazine-functionalized alepterolic acid derivatives: synthesis, anticancer activity, and mechanism of action

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00275G, Research Article

Binbin Zhang, Yating Jia, Siyu Qiu, Yanchun Sun, Zixuan Tong, Peixin Wang, Lian Ma, Fengjiao Wang, Guozheng Huang, Jianguo Cao
Urea- and piperazine-functionalized alepterolic acid derivatives significantly inhibited the growth of A549 cancer cells.
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Targeting DNA-PK: medicinal chemistry insights into small-molecule inhibitor discovery and optimisation

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00119J, Review Article

Open Access

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

Elle Watson, Jack R. R. Hutchinson, Suzannah J. Harnor, Luke Gaughan, Celine Cano
Since Wortmannin's discovery, DNA-PK inhibitors have expanded to optimised scaffolds, including chromen-4-ones (e.g. NU5455) and purinones (e.g. AZD7648). This review covers their synthesis and pharmacology from early hits to clinical candidates.
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Recent advances in piperine and its derivatives as potential anticancer agents

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00223D, Review Article

Open Access

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

Qi-Hua Yu, Zhiyan Liu, Jiazheng Liu, Li-Ping Bai
This review identified piperine as a promising anticancer agent, demonstrating that the structural modification of its amide region can significantly improve the anticancer activity.
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Synthetic routes towards antiviral agents from the houttuynoid family: structure–activity relationships and antiviral efficacy against herpes simplex virus type 1

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00158K, Review Article

Adarsh Krishna T. P, Ajeesh Krishna T. P, Reshma Rajan, Laxman Kota, Prasobh K. Mohan
This review delineates the total synthesis of houttuynoids, highlighting a diverse chemical toolkit and their structure–activity relationships (SARs) and antiviral efficacy.
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A Bakuchiol-Linked Tetrazole Exhibits Narrow-spectrum Activity Against Streptococcus pneumoniae

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00230G, Research Article

Neha Sengar, Vidyadhar Pratap, Tuhin Sarkar, Vishnu Kriplani, Astha Gupta, Sanjay Mandal, Prasad V. Bharatam, Dulal Panda, Inder Pal Singh
Natural product-based amphiphilic phenolic terpenoid antimicrobial agents were rationally designed by integrating the meroterpenoid bakuchiol with a tetrazole moiety through a fragment-based drug design strategy. A library of 30 bakuchiol-linked...
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