RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00660G, Review Article

Shutang Li, Jinfei Yang
As research on AD has progressed, TCM and its active ingredients have increasingly played a crucial role in clinical treatment. This article summarizes extracts from TCM and briefly elucidates their pharmacological mechanisms against AD.
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RSC Med. Chem., 2024, 15,3395-3417
DOI: 10.1039/D4MD00334A, Research Article

Vu Ngoc Toan, Do Son Hai, Hoang Thi Kim Van, Nguyen Minh Tri, Duong Ngoc Toan, Nguyen Thi Thanh Mai, Nguyen Dinh Thanh
D-Glucose-conjugated thioureas from 2-aminopyrimidines had inhibitory activity against α-amylase, α-glucosidase, DPP-4, PTP1B. The cytotoxicity, inhibitory kinetics, and molecular simulations of the most potent inhibitors 8k, 8j, 8f, and 8h were studied.
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RSC Med. Chem., 2024, 15,3286-3344
DOI: 10.1039/D4MD00169A, Review Article

Open Access

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

Jenny-Lee Panayides, Darren Lyall Riley, Felix Hasenmaile, Willem A. L. van Otterlo
This review aims to highlight the role of silicon in drug discovery.
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RSC Med. Chem., 2024, 15,3495-3506
DOI: 10.1039/D4MD00275J, Research Article

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Thomas J. Cogswell, Laia Josa-Culleré, David Zimmer, Sébastien R. G. Galan, Morgan Jay-Smith, Kate S. Harris, Carole J. R. Bataille, Thomas R. Jackson, Douzi Zhang, Stephen G. Davies, Paresh Vyas, Thomas A. Milne, Graham M. Wynne, Angela J. Russell
The optimisation of a class of AML differentiation agents is described to show improved potency, solubility and stability, reduced off target toxicity, and tumour regression in a murine model in vivo.
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RSC Med. Chem., 2024, 15,3507-3528
DOI: 10.1039/D4MD00417E, Research Article

Yuying Liu, Zeyu Yang, Jie Zhang, Na Guo, Nanxin Liu, Qingqing Zhang, Xintao Dang, Yanchen Li, Jie Zhang, Xiaoyan Pan
In continuation of our previous research, a series of novel Bcr-Abl^T315I inhibitors with tert-leucine or serine as a flexible linker were developed and biological evaluation was performed in vitro.
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RSC Med. Chem., 2024, 15,3576-3596
DOI: 10.1039/D4MD00438H, Research Article

Ruolin Cao, Fangyu Du, Zhiqiang Liu, Pengcheng Cai, Minggang Qi, Wei Xiao, Xuefei Bao, Guoliang Chen
Rho-associated coiled-coil containing kinase (ROCK) plays an important role in inflammation.
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RSC Med. Chem., 2024, 15,3469-3476
DOI: 10.1039/D4MD00422A, Research Article

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Hugo Kocek, Dominika Chalupská, Milan Dejmek, Alexandra Dvořáková, Michala Zgarbová, Michal Šála, Karel Chalupský, Petra Krafčíková, Tomáš Otava, Matúš Drexler, Eliška Procházková, Blanka Klepetářová, Milan Štefek, Ján Kozic, Helena Mertlíková-Kaiserová, Evzen Boura, Jan Weber, Radim Nencka
SARS-CoV-2 nsp14 methyltransferase inhibitors based on adenosine 5'-carboxamides.
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RSC Med. Chem., 2024, 15,3418-3432
DOI: 10.1039/D4MD00170B, Research Article

Open Access

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Chien Van Tran, Thao Thi Phuong Tran, Anh The Nguyen, Loc Van Tran, Ninh Thi Pham, Luu Thi Nguyen, Dung Thi Nguyen, Michelle D. Garrett, Nga Thi Nguyen, Thao Thi Do, Christopher J. Serpell, Sung Van Tran
Madecassic acid and silybin have been conjoined to produce hybrid compounds with improved and different activity against liver cancer cells.
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RSC Med. Chem., 2024, 15,3345-3370
DOI: 10.1039/D4MD00317A, Review Article

Meghna Arora, Ankit Kumar Singh, Adarsh Kumar, Harshwardhan Singh, Prateek Pathak, Maria Grishina, Jagat Pal Yadav, Amita Verma, Pradeep Kumar
Semisynthetic phytochemicals in cancer treatment.
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RSC Med. Chem., 2024, 15,3444-3459
DOI: 10.1039/D4MD00318G, Research Article

Anuja Gracy Joseph, Mohanan Biji, Vishnu Priya Murali, Daisy R. Sherin, Alisha Valsan, Vimalkumar P. Sukumaran, Kokkuvayil Vasu Radhakrishnan, Kaustabh Kumar Maiti
Niloticin, a triterpenoid from Aphanamixis polystachya, induces apoptosis in HeLa cells which is primarily validated through in silico analysis and subsequently in vitro apoptotic evaluation by modulating the apoptotic proteins.
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RSC Med. Chem., 2024, 15,3433-3443
DOI: 10.1039/D4MD00468J, Research Article

Meijuan Liu, Na Li, Zhaoxue Wang, Shuo Wang, Shaoda Ren, Xiaojing Li
A synthetic celastrol derivative (Cel-N) attenuates cancer cell stemness, inhibits the STAT3 pathway, and exerts anti-ovarian cancer effects in cell and mouse models.
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RSC Med. Chem., 2024, 15,3529-3557
DOI: 10.1039/D4MD00481G, Research Article

Mohamed K. S. El-Nagar, Mai I. Shahin, Mohammed F. El-Behairy, Ehab S. Taher, Mohamed F. El-Badawy, Marwa Sharaky, Dalal A. Abou El Ella, Khaled A. M. Abouzid, Mai Adel
Discovery of novel pyridazinone derivatives with dual antimicrobial and anticancer activities.
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RSC Med. Chem., 2024, 15,3460-3468
DOI: 10.1039/D4MD00405A, Research Article

Xiaoqin Luo, Jin Wang, Ruichang Wang, Jiabing Lian, Mengnan Guo, Hongrui Zhou, Mengxue Zhang, Zhe Yang, Xiaolong Li, Xianran He, Xiuli Bi
Schematic of proposed mechanism for the treatment of the SLL-1A-16 inhibiting the proliferation in NSCLC.
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RSC Med. Chem., 2024, 15,3485-3494
DOI: 10.1039/D4MD00246F, Research Article

Shouguo Peng, Haixia Li, Weilu Cui, Tianning Xiong, Jiaqi Hu, Haixiang Qi, Songwen Lin, Deyu Wu, Ming Ji, Heng Xu
A novel PSMA–PI3K small molecule drug conjugate has been prepared, highlighting its potential in targeted cancer therapy.
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RSC Med. Chem., 2024, 15,3477-3484
DOI: 10.1039/D4MD00266K, Research Article

Raitis Bobrovs, Svetlana Terentjeva, Ninni Elise Olafsen, Zilvinas Dambrauskas, Antanas Gulbinas, Toivo Maimets, Indrek Teino, Aigars Jirgensons, Jason Matthews, Kristaps Jaudzems
The aryl hydrocarbon receptor (AHR) is a versatile ligand-dependent transcription factor involved in diverse biological processes, from metabolic adaptations to immune system regulation.
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RSC Med. Chem., 2024, 15,3371-3394
DOI: 10.1039/D4MD00384E, Review Article

Debasis Das, Lingzhi Xie, Jian Hong
Prospects of novel fourth-generation EGFR-TKIs overcoming C797S-mediated resistance in non-small cell lung cancer.
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RSC Med. Chem., 2024, 15,3609-3615
DOI: 10.1039/D4MD00501E, Research Article

Open Access

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Gciniwe S. Mathenjwa, Abir Chakraborty, Abantika Chakraborty, Ronel Muller, Mathew P. Akerman, Moira L. Bode, Adrienne L. Edkins, Clinton G. L. Veale
Rationally modified Hsp90 inhibitors which retained of on-target activity but showed no engagement of intracellular Hsp90, or stimulation of the heat shock response, were found to significantly alter the extracellular fibronectin network.
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RSC Med. Chem., 2024, 15,3558-3575
DOI: 10.1039/D4MD00391H, Research Article

Pothiyil S. Vimalkumar, Neethu Sivadas, Vishnu Priya Murali, Daisy R. Sherin, Madhukrishnan Murali, Anuja Gracy Joseph, Kokkuvayil Vasu Radhakrishnan, Kaustabh Kumar Maiti
Malabaricone A isolated from Myristica malabarica induces apoptosis in triple-negative breast cancer cells through intrinsic and extrinsic pathways, which is validated through in vitro and in silico studies and resembles a potent phyto-entity.
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RSC Med. Chem., 2024, 15,3597-3608
DOI: 10.1039/D4MD00378K, Research Article

Open Access

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Rachel A. Heylen, Nicola Cusick, Tom White, Emily J. Owen, Bethany L. Patenall, Martin Alm, Peter Thomsen, Maisem Laabei, A. Toby A. Jenkins
In silico identification of urease inhibitors based on thiourea, tested to determine IC₅₀ and tested on a catheterised in vitro bladder model, showing efficacy in reducing catheter blockage.
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RSC Med. Chem., 2024, 15,3616-3624
DOI: 10.1039/D4MD00306C, Research Article

Open Access

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Adam Throup, Manar Saleh Zraikat, Andrew Gordon, Shohreh Jafarinejad Soumehsaraei, Kathrin D. Haase, Laurence H. Patterson, Patricia A. Cooper, Katherine Hanlon, Paul M. Loadman, Mark Sutherland, Steven D. Shnyder, Helen M. Sheldrake
Cyclobutanes provide a versatile scaffold for the synthesis of small molecule integrin antagonists with good metabolic stability and in vivo tolerability.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00257A, Research Article

Shahabuddin, Uzma, Mohammad Azam, Mehtab Parveen, Nurul Huda Abd Kadir, Kim Min, Mahboob Alam
In light of the ongoing pandemic caused by SARS-CoV-2, effective and clinically translatable treatments are desperately needed for COVID-19 and its emerging variants.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00517A, Research Article

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Arianna Amenta, Susanna Comi, Marcelo Kravicz, Silvia Sesana, Antonia Antoniou, Daniele Passarella, Pierfausto Seneci, Sara Pellegrino, Francesca Re
A novel, glutathione-activated prodrug of pimasertib (PROPIMA) has been developed. PROPIMA showed ability to inhibit tumour cell migration and proliferation controlled over time, while also achieving a high incorporation rate into liposomes.
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RSC Med. Chem., 2024, 15,3284-3285
DOI: 10.1039/D4MD90035A, Editorial

Jian Zhang, Ola Engkvist, Gerhard Hessler
Jian Zhang, Ola Engkvist and Gerhard Hessler introduce the RSC Medicinal Chemistry themed collection on ‘AI in Medicinal Chemistry’.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00537F, Research Article

Open Access

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Abdelfattah Faouzi, Alexandre Arnaud, François Hallé, Jean Roussel, Mandy Aymard, Vincent Denavit, Cong Viet Do, Angélique Mularoni, Mohamed Salah, Ahmed ElHady, Thanh-Nhat Pham, Alexandre Bancet, Marc Le Borgne, Raphaël Terreux, Roland Barret, Matthias Engel, Thierry Lomberget
A series of sulfur-containing tetracycles was designed and evaluated for their ability to inhibit protein kinase DYRK1A, a target known to have several potential therapeutic applications including cancers, Down syndrome or Alzheimer's disease.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00471J, Research Article

Poorvi Saraf, Bhagwati Bhardwaj, Akash Verma, Mohammad Aquib Siddiqui, Himanshu Verma, Pradeep Kumar, Samridhi Srivastava, Sairam Krishnamurthy, Saripella Srikrishna, Sushant Kumar Shrivastava
Screening piperazine derivatives via ChEMBL database led to the design and synthesis of novel dual COX-2/5-LOX inhibitors with strong anti-inflammatory, analgesic, and anti-cancer activity.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00608A, Research Article

Sunil Kumar, Bishnu Prasad Pandey, Mohamed A. Abdelgawad, Mohammed M. Ghoneim, Rania B. Bakr, Hoon Kim, Bijo Mathew
A total of 18 heterocyclic derived conjugated dienones (CD1–CD18) were evaluated for their potential monoamine oxidase (MAO)-A/-B inhibitory activity.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00673A, Review Article

Juhyung Song, Cheoljun Park, Francis E. B. Cabanting, Yong Woong Jun
Potential therapeutic target proteins for upregulating DNA repair system are reviewed, along with reported small-molecule activators.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00297K, Research Article

Branislava Tenjović, Sofija Bekić, Andjelka Ćelić, Edward Petri, Julia Scholda, Florian Kopp, Marija Sakač, Andrea Nikolić
In this study, a series of 13 new D-ring fused steroidal N(2)-substituted-1,2,3-triazoles were synthesized, characterized and evaluated for their biological activities.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD90039A, Editorial

Marcel Hollenstein, Eugen Stulz
Marcel Hollenstein and Eugen Stulz introduce the cross-journal themed collection celebrating Christian Leumann’s retirement.
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RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00721B, Research Article

Qun Tang, Haiyang Zhang, Kasemsiri Chandarajoti, Zirui Jiao, Lianhua Nie, Sai Lv, Jiakun Zuo, Wen Zhou, Xiangan Han
Bacterial infections pose a threat to the health of animals and human being, and the biofilm formation exacerbates the microbial threat. New antimicrobial agents to address this challenge are much...
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00662C, Research Article

Rajat Arora, Ayan Mukherjee, Gilbert Arthur, Mark W. Nachtigal, Frank Schweizer
We describe the multi-step synthesis of different dibasic and tribasic galactosamine-based glycosylated antitumor ether lipids (GAELs) and their cytotoxic response in comparison to doxorubicin and cisplatin.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00541D, Research Article

Mikhail N. Anisimov, Maksim A. Boichenko, Vitaly V. Shorokhov, Julia N. Borzunova, Marina Janibekova, Vadim V. Mustyatsa, Ilya A. Lifshits, Andrey Yu. Plodukhin, Ivan A. Andreev, Nina K. Ratmanova, Sergey S. Zhokhov, Elena A. Tarasenko, Daria A. Ipatova, Alexander R. Pisarev, Ivan A. Vorobjev, Igor V. Trushkov, Olga A. Ivanova, Nikita B. Gudimchuk
New 1,5-disubstituted pyrrolidin-2-ones 1, 2 and 5-aryl-3,3a,4,5-tetrahydropyrrolo[1,2-a]quinoline-1(2H)-ones 3 were explored as inhibitors of tubulin polymerization.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00594E, Research Article

Nagat Ghareb, Khaled M. Darwish, Mohamed S. Nafie, Ranwa Elrayess, Noha M. Abourobe, Shaimaa A. Fattah, Reem M. Hazem, Eman T. Mehanna, Ranza Elrayess
One benzene-sulfonamide derivative exhibited potent protein tyrosine phosphatase-1B inhibition for managing diabetes mellitus and associated metabolic disorders.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00494A, Research Article

Shekhar, Shefali Chowdhary, Joel Mosnier, Isabelle Fonta, Bruno Pradines, Vipan Kumar
In pursuit of novel anti-plasmodial agents, a library of triclosan-based dimers both with and without a 1H-1,2,3 triazole core were designed, synthesized and evaluated in order to achieve a multitargeted approach.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD90044H, Correction

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Kennosuke Itoh, Hiroki Nakahara, Atsushi Takashino, Aya Hara, Akiho Katsuno, Yuriko Abe, Takaaki Mizuguchi, Fumika Karaki, Shigeto Hirayama, Kenichiro Nagai, Reiko Seki, Noriko Sato, Kazuki Okuyama, Masashi Hashimoto, Ken Tokunaga, Hitoshi Ishida, Fusako Mikami, Kofi Dadzie Kwofie, Hayato Kawada, Bangzhong Lin, Kazuto Nunomura, Toshio Kanai, Takeshi Hatta, Naotoshi Tsuji, Junichi Haruta, Hideaki Fujii
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00645C, Research Article

Geetmani Singh Nongthombam, Semim Akhtar Ahmed, Kangkon Saikia, Sanjib Gogoi, Jagat Chandra Borah
Virtual screening and synthetic modification of natural product-derived steroidal precursors as potential SGLT2 inhibitors for the treatment of diabetic nephropathy.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00383G, Research Article

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Walaa K. Mousa, Ashif Y. Shaikh, Rose Ghemrawi, Mohammed Aldulaimi, Aya Al Ali, Nour Sammani, Mostafa Khair, Mohamed I. Helal, Farah Al-Marzooq, Emilia Oueis
An AMP-derived short 15-mer peptide and its cyclic derivatives have low micromolar broad spectrum antibacterial activity, with rapid onset of bactericidal effect and a membrane-targeting mode of action.
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RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00742E, Research Article

Open Access

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Uladzimir Bildziukevich, Lucie Cerna, Jana Trylčová, Marie Kvasnicova, Lucie Rárová, David Šaman, Petra Lovecká, Jan Weber, Zdenek Wimmer
A series of amides of the selected plant triterpenoids, moronic acid and morolic acid, with the tripeptides MAG and GAM was designed and synthesized. Two required tripeptides 5 and 10...
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00617H, Research Article

Aida Buza, Cüneyt Türkeş, Mustafa Arslan, Yeliz Demir, Busra Dincer, Arleta Rifati Nixha, Şükrü Beydemir
In this research, a series of sulfonamides incorporating a 1,2,3-triazolyloxime substituted 1,2,3-triazolyl moiety was conceptualized, synthesized, and investigated as carbonic anhydrase inhibitors.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00562G, Research Article

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Andreas Simoens, Andreas Dejaegere, Marthe Vandevelde, Christian V. Stevens
Flow chemistry allows for the rapid and clean synthesis of therapeutically relevant tryptamines in good yields, including the large scale drug rizatriptan.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00511B, Research Article

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Francesco Melfi, Marialuigia Fantacuzzi, Simone Carradori, Ilaria D'Agostino, Alessandra Ammazzalorso, Noemi Mencarelli, Marialucia Gallorini, Mattia Spano, Paolo Guglielmi, Mariangela Agamennone, Sazan Haji Ali, Ali Al-Samydai, Francesca Sisto
Monoterpene-derived azo benzenes showed selective antibacterial activity against Helicobacter pylori with a safe profile. An in silico investigation highlighted the inosine 5'-monophosphate dehydrogenase enzyme as the putative target.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00522H, Review Article

Keran Wang, Yanwen Huang, Yan Wang, Qidong You, Lei Wang
CADD and AIDD contribute to the drug discovery.
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RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00450G, Review Article

Shikha Thakur, Devendra Kumar, shivani jaiswal, Kapil Kumar Goel, Pramod Rawat, Vivek Srivastava, Sonia Dhiman, Hemant R Jadhav, Ashish Ranjan Dwivedi
Thiophene is a privileged pharmacophore in medicinal chemistry owing to its diversified biological attributes. The thiophene moiety has been ranked 4th in US FDA drug approval of small drug molecules,...
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00632A, Review Article

Ashish Ranjan Dwivedi, Shivani Jaiswal, Deepak Kukkar, Roshan Kumar, Thakur Gurjeet Singh, Mahendra Pratap Singh, Abhay M. Gaidhane, Sorabh Lakhanpal, K. Nagendra Prasad, Bhupinder Kumar
The present review is a concerted effort to cover drugs bearing pyridine rings approved in the last decade, and it provides thorough discussion and commentary on their pharmacokinetics and pharmacodynamics together with in-depth structural analysis.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00579A, Research Article

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Cecilia C. Ayala-Aguilera, Yang Ge, Álvaro Lorente-Macías, Benjamin N. Jones, Catherine Adam, Neil O. Carragher, Asier Unciti-Broceta
A ligand-centred strategy combined with phenotypic screening was used to develop novel antiproliferative inhibitors against oesophageal cancer and identified a lead compound that induces potent anticancer activity and inhibits Aurora kinase A.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00621F, Research Article

Chunfei Zhang, Yixin Liu, Xiao Zhang, Chunping Wan, Zewei Mao
A series of novel benzofuran-based chalcone derivatives could be considered as potent VEGFR-2 inhibitors.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00619D, Research Article

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Marina Perieteanu, Tayner Rodriguez Garzon, Leah M. C. McGee, Abedawn I. Khalaf, Colin J. Suckling, Rebecca Beveridge, Vicky M. Avery, Fraser J. Scott
25 S-MGBs, including those bearing an amidine tail group, were investigated for their antiplasmodial, in vitro activity against 3D7 and Dd2 strains of P. falciparum. Several potent, and selective, hit compounds were identified.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00555D, Research Article

Shenghua Gao, Letian Song, Bing Ye, Mianling Yang, Junyi Li, Manyu Gu, Ann E. Tollefson, Karoly Toth, Peng Zhan, Xinyong Liu
The continuous mutational nature of SARS-CoV-2 and its inter-species' similarities emphasize the urgent need to design and develop more direct-acting antiviral agents against highly infectious variants.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00508B, Review Article

Carlos Roberto Tavolari Jortieke, Angélica Rocha Joaquim, Fernando Fumagalli
This review presents the recent findings on antibacterial agents against Mycobacterium fortuitum and reveals the most promising and effective chemical frameworks to inspire the development of new drugs.
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