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At a loss: On the New Zealand-India three-match series

India batters frittered away the home advantage against New Zealand 




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​Escalation ladder: On conflict between Israel and Iran

Iran should show strategic restraint; and the world should rein in Israel




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Western front: On the parties and their prospects in the Maharashtra polls

Granular factors can determine the outcome in Maharashtra 




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​Beautifully vague: On the Tamilaga Vettri Kazhagam’s inaugural conference  

Actor Vijay seems to be targeting both the BJP and the DMK 




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​Tough task: On the battle lines in the Jharkhand Assembly election

Coalitional incoherence could stymie the INDIA bloc’s effort to retain power in Jharkhand




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Sun signs: On extreme heat and Tamil Nadu’s policy decision

States should prepare to assist the vulnerable during extreme heat events




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Towards Europe: On the India visits by the leaders of Germany, Spain

India used visits by leaders of Germany and Spain to balance ties in Europe 




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Watch: When Jimmy Sheirgill Got Violent

'As a storyteller, one always looks to create something for the audience which is thrilling, engaging and entertaining and that is exactly what we have endeavoured with Sikandar Ka Muqaddar.'




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What Makes <I>Andaz Apna Apna</I> Such Fun Even Today

Andaz Apna Apna is practically the most quoted film since Sholay, observes Sukanya Verma, as she celebrates 30 years of this cult classic movie.




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Why Kriti Is So Grateful

Kriti Kharbanda took a trip down memory lane when her rom-com Shaadi Mein Zaroor Aana clocked seven years since its release.




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Alia-Ranbir's Daughter Raha Turns 2

Alia Bhatt and Ranbir Kapoor's little girl Raha turned two on November 6, and we were treated to the most adorable pictures on social media.




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The Raj & DK Line-Up You Cannot Miss

Sukanya Verma looks at their eclectic career of over two decades as their latest offering Citadel: Honey Bunny, the Indian leg of the Russo Brothers globetrotting spy universe series, drops on Amazon Prime Video on November 7.




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Why Abhishek Missed Aishwarya's Birthday

When Aishwarya celebrated her birthday in Dubai on November 1, the speculation regarding the Abhishek-Aishwarya marital rift ran even higher.




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The Woman Who Lost Everything

When the landslide hit, Sruthi's house was washed away, along with its inhabitants.




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'He Doesn't Have The Air He Is Raj Thackeray's Son'

'I love to meet people.'




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Ananya-Suhana Party Together

Ananya Panday celebrated her birthday with family and the media, but she really wasn't done yet.




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Look Who Just Met Tom Cruise!

Kartik wants to savour Litti Chokha in Patna... Amyra holidays in Phuket... Karishma in Italy...




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Pathogenesis of Alzheimer's disease and therapeutic strategies involving traditional Chinese medicine

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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Design, synthesis, inhibitory activity, and molecular simulations study for D-glucose-conjugated thioureas containing pyrimidine ring as multitarget inhibitors against α-amylase, α-glucosidase, DDP-4, and PTP1B in Type 2 diabetes mellitus

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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The role of silicon in drug discovery: a review

RSC Med. Chem., 2024, 15,3286-3344
DOI: 10.1039/D4MD00169A, Review Article
Open Access
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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Lead optimisation of OXS007417: in vivo PK profile and hERG liability modulation to optimise a small molecule differentiation agent for the potential treatment of acute myeloid leukaemia

RSC Med. Chem., 2024, 15,3495-3506
DOI: 10.1039/D4MD00275J, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
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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Integrating amino acids into Bcr-Abl inhibitors: design, synthesis, biological evaluation, and in silico studies

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-AblT315I inhibitors with tert-leucine or serine as a flexible linker were developed and biological evaluation was performed in vitro.
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The synthesis and bioactivities of ROCK2 inhibitors with 1,2-dithiolan-3-yl motif

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.
The content of this RSS Feed (c) The Royal Society of Chemistry




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Discovery of highly potent SARS-CoV-2 nsp14 methyltransferase inhibitors based on adenosine 5'-carboxamides

RSC Med. Chem., 2024, 15,3469-3476
DOI: 10.1039/D4MD00422A, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
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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Synthesis and cytotoxic activity of madecassic acid–silybin conjugate compounds in liver cancer cells

RSC Med. Chem., 2024, 15,3418-3432
DOI: 10.1039/D4MD00170B, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
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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Semisynthetic phytochemicals in cancer treatment: a medicinal chemistry perspective

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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A comprehensive apoptotic assessment of niloticin in cervical cancer cells: a tirucallane-type triterpenoid from Aphanamixis polystachya (Wall.) Parker

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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Synthesis of a celastrol derivative as a cancer stem cell inhibitor through regulation of the STAT3 pathway for treatment of ovarian cancer

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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Pyridazinone-based derivatives as anticancer agents endowed with anti-microbial activity: molecular design, synthesis, and biological investigation

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.
The content of this RSS Feed (c) The Royal Society of Chemistry




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SLL-1A-16 suppresses proliferation and induces autophagy in non-small-cell lung cancer cells via the AKT/mTOR signaling pathway

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.
The content of this RSS Feed (c) The Royal Society of Chemistry




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Design, synthesis and biological evaluation of a novel PSMA–PI3K small molecule drug conjugate

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.
The content of this RSS Feed (c) The Royal Society of Chemistry




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Discovery and optimisation of pyrazolo[1,5-a]pyrimidines as aryl hydrocarbon receptor antagonists

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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Next-generation EGFR tyrosine kinase inhibitors to overcome C797S mutation in non-small cell lung cancer (2019–2024)

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.
The content of this RSS Feed (c) The Royal Society of Chemistry




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Rationally modified SNX-class Hsp90 inhibitors disrupt extracellular fibronectin assembly without intracellular Hsp90 activity

RSC Med. Chem., 2024, 15,3609-3615
DOI: 10.1039/D4MD00501E, Research Article
Open Access
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.
The content of this RSS Feed (c) The Royal Society of Chemistry




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Exploring apoptotic induction of malabaricone A in triple-negative breast cancer cells: an acylphenol phyto-entity isolated from the fruit rind of Myristica malabarica Lam.

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.
The content of this RSS Feed (c) The Royal Society of Chemistry




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Rational design and in vitro testing of new urease inhibitors to prevent urinary catheter blockage

RSC Med. Chem., 2024, 15,3597-3608
DOI: 10.1039/D4MD00378K, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
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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Sidechain structure–activity relationships of cyclobutane-based small molecule αvβ3 antagonists

RSC Med. Chem., 2024, 15,3616-3624
DOI: 10.1039/D4MD00306C, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
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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Exploring 7β-amino-6-nitrocholestens as COVID-19 antivirals: in silico, synthesis, evaluation, and integration of artificial intelligence (AI) in drug design: assessing the cytotoxicity and antioxidant activity of 3β-acetoxynitrocholestane

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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A novel, glutathione-activated prodrug of pimasertib loaded in liposomes for targeted cancer therapy

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00517A, Research Article
Open Access
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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Introduction to the themed collection on ‘AI in Medicinal Chemistry’

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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Design, synthesis, and structure–activity relationship studies of 6H-benzo[b]indeno[1,2-d]thiophen-6-one derivatives as DYRK1A/CLK1/CLK4/haspin inhibitors

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00537F, Research Article
Open Access
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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Design, synthesis, and evaluation of benzhydrylpiperazine-based novel dual COX-2/5-LOX inhibitors with anti-inflammatory and anti-cancer activity

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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Inhibition of monoamine oxidases by heterocyclic derived conjugated dienones: synthesis and in vitro and in silico investigations

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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Therapeutic upregulation of DNA repair pathways: strategies and small molecule activators

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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Synthesis and biological evaluation of novel D-ring fused steroidal N(2)-substituted-1,2,3-triazoles

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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Introduction to the themed collection in honour of Professor Christian Leumann

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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Design and Synthesis of coumarin-based amphoteric antimicrobials with the biofilm interference and immunoregulation effects

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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Modulating polybasic character of galactose-based glycosylated antitumor ether lipids for enhanced cytotoxic response

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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Synthesis and evaluation of tetrahydropyrrolo[1,2-a]quinolin-1(2H)-ones as new tubulin polymerization inhibitors

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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Development, biological evaluation, and molecular modelling of some benzene-sulfonamide derivatives as protein tyrosine phosphatase-1B inhibitors for managing diabetes mellitus and associated metabolic disorders

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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