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

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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, 15,3444-3459
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, 15,3371-3394
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, 15,3597-3608
DOI: 10.1039/D4MD00378K, Research Article

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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

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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/D4MD00537F, Research Article

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

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

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, 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/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/D4MD00685B, Research Article

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Samantha J. Bann, Stephen A. Cochrane
Lipid swapping: a new approach for the synthesis of globomycin that allows for facile lipid diversification.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00623B, Research Article

Ojaswitha Ommi, Priyanka Sudhir Dhopat, Shashikanta Sau, Madhu Rekha Estharla, Srinivas Nanduri, Nitin Pal Kalia, Venkata Madhavi Yaddanapudi
A series of pyrazole–ciprofloxacin hybrids were designed, synthesized, and tested for antibacterial activity against Staphylococcus aureus, Pseudomonas aeruginosa, and Mycobacterium tuberculosis, aiming to combat antibiotic resistance.
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RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00670D, Research Article

Yuting Liu, Pengju Yang, Yunyun Zhou, Zhiwen Zhou
In the current study, we have designed and prepared a series of quinoxaline-based compounds, which were derived from o-phenylenediamine. Among which, compounds 5m-p displayed good to moderate antibacterial activity with...
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RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00373J, Research Article

YongLai Jiao, Jie Zhong, Jin-Fang Xu, Shaobo Ning, Taigang Liang, Mingzhu Zhao, Jian Zhang
The mitotic kinase Aurora A, a pivotal regulator of cell cycle, is overexpressed in various cancers and has emerged as one of the most promising targets for anticancer drug discovery....
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00614C, Research Article

Vijay Babu Pathi, Pranotosh Das, Abhyuday Guin, Manish Debnath, Biswadip Banerji
The development of chemical scaffolds that target highly conserved MALAT1 RNA received attention due to its significance in splicing, nuclear organization, and gene expression in disease progression pathways.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00626G, Research Article

Aleena Pious, Vignesh Venkatasubramanian, Dharshini Karnan Singaravelu, Subburethinam Ramesh, Fuad Ameen, Anbazhagan Veerappan
Lipidation modulates the Gram-selective antibacterial activity of QPyNATh.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00495G, Research Article

Yakup Berkay Yilmaz, Tuğba Güngör, Serhat Dönmez, Hazal Nazlıcan Atalay, Pınar Siyah, Serdar Durdağı, Mehmet Ay, Tugba Boyunegmez Tumer
New isothiocyanate derivatives (I1–3 and I1a–e) were synthesized and screened for their anti-inflammatory activities and H₂S-releasing capacities. Compounds I1 and I1c demonstrated the most potent and selective COX-2 inhibition.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00601A, Research Article

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Brém Balázs, Bianca Stoean (Vasile), Éva Molnár, Eva Fischer-Fodor, Ovidiu Bălăcescu, Raluca Borlan, Monica Focsan, Adriana Grozav, Patriciu Achimaş-Cadariu, Emese Gál, Luiza Gaina
New meso-substituted AB₃-type phenothiazinyl porphyrins and ferrocenylvinyl phenothiazinyl porphyrin were synthesised by Suzuki–Miyaura and Mizoroki–Heck cross-coupling reactions, respectively.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00553H, Research Article

Stefano Tomassi, Benito Natale, Michele Roggia, Luisa Amato, Caterina De Rosa, Carminia Maria Della Corte, Emma Baglini, Giorgio Amendola, Anna Messere, Salvatore Di Maro, Elisabetta Barresi, Federico Da Settimo, Maria Letizia Trincavelli, Fortunato Ciardiello, Sabrina Taliani, Floriana Morgillo, Sandro Cosconati
Non-small cell lung cancer (NSCLC), the leading cause of cancer-related mortality worldwide, poses a formidable challenge due to its heterogeneity and the emergence of resistance to targeted therapies.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00600C, Research Article

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Gennaro Sanità, Maria Laura Alfieri, Barbara Carrese, Serena Damian, Vincenza Mele, Gaetano Calì, Brigida Silvestri, Sebastiano Marra, Susan Mohammadi, Giuseppina Luciani, Paola Manini, Annalisa Lamberti
Biological assays carried out on melanoma and breast cancer cells highlighted the role of light in boosting the cytotoxic effect of a ruthenium complex featuring a dihydroisoquinoline ligand suggesting applications in photodynamic therapy.
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RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00597J, Research Article

Albert Michael Crider, Audrey Hospital, Karin Sandoval, William Neumann, Stephen Kukielski, Lejla Garic, Kristen Ingold, Matthew Dunahoo, Khush Srabony, Rafael Frare, Olivia Slater, Nathan Peel, Maria Kontoyianni, Ken Witt
Somatostatin receptor-4 (SST4) is a therapeutic target for several conditions, including Alzheimer’s disease, seizures, neuropsychiatric disorders, and pain. Our previous work on 1,2,4-triazole derivatives led to enhanced SST4 binding affinity,...
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00707G, Review Article

Lavleen K. Mader, Jessica E. Borean, Jeffrey W. Keillor
Kinetic evaluations for assay dependent characterization of irreversible inhibitors.
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RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00722K, Research Article

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Maria Cristina Lomuscio, Nicola Corriero, Vittoria Nanna, Antonio Piccinno, Michele Saviano, Rosa Lanzilotti, Carmen Abate, Domenico Alberga, Giuseppe Felice Mangiatordi
Developing sigma-1 receptor (S1R) modulators is considered a valuable therapeutic strategy to counteract neurodegeneration, cancer progression, and viral infections, including COVID-19. In this context, in-silico tools capable of accurately predicting...
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00724G, Research Article

Zhengxiao Huang, Hongjie Chen, Xiao Zhang, Ruirui Wang, Chunyan Hu, Zewei Mao
A series of novel azole derivatives containing 1,2,3-triazole have been synthesized with good antifungal effects on sensitive and drug-resistant C. albicans.
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RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00654B, Review Article

Madison R. Nuske, Junlang Zhong, Renjie Huang, Vijayalekshmi Sarojini, Jack L. Y. Chen, Christopher J. Squire, Mark A. T. Blaskovich, Ivanhoe K. H. Leung
The emergence of the mobile colistin resistance (mcr) gene is a significant threat contributing to the worldwide antibiotic resistance crisis. This review discusses adjuvant strategies to restore polymyxin sensitivity in these resistant bacteria.
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