vi

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




vi

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




vi

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




vi

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




vi

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




vi

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




vi

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




vi

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




vi

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




vi

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




vi

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.
To cite this article before page numbers are assigned, use the DOI form of citation above.
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vi

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.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




vi

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.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




vi

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.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




vi

Correction: Anti-schistosomal activity and ADMET properties of 1,2,5-oxadiazinane-containing compound synthesized by visible-light photoredox catalysis

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD90044H, Correction
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
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
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




vi

Human microbiome derived synthetic antimicrobial peptides with activity against Gram-negative, Gram-positive, and antibiotic resistant bacteria

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00383G, Research Article
Open Access
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.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




vi

Amides of moronic acid and morolic acid with the tripeptides MAG and GAM targeting antimicrobial, antiviral and cytotoxic effects

RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00742E, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
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...
The content of this RSS Feed (c) The Royal Society of Chemistry




vi

Novel benzenesulfonamides containing a dual triazole moiety with selective carbonic anhydrase inhibition and anticancer activity

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.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




vi

Synthesis and anti-tumor activity of new benzofuran-based chalcone derivatives as potent VEGFR-2 inhibitors

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.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




vi

Enhancing the antimycobacterial efficacy of pyridine-4-carbohydrazide: linkage to additional antimicrobial agents via oxocarboxylic acids

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00663A, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Václav Pflégr, Klára Konečná, Jiřina Stolaříková, Jan Ősterreicher, Ondřej Janďourek, Martin Krátký
Linking pyridine-4-carbohydrazide to other antimicrobial agents via oxocarboxylic acids significantly enhances efficacy against mycobacteria with promising selectivity and safety profiles.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




vi

Synthesis of cationic N-acylated thiazolidine for selective activity against Gram-positive bacteria and evaluation of N-acylation's role in membrane-disrupting activity

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.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




vi

Generation and capture of naphthoquinonynes: a new frontier in the development of trypanocidal quinones via aryne chemistry

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00558A, Research Article
Laura P. R. Figueroa, Renato L. de Carvalho, Renata G. Almeida, Esther R. S. Paz, Emilay B. T. Diogo, Maria H. Araujo, Warley S. Borges, Victor F. S. Ramos, Rubem F. S. Menna-Barreto, James M. Wood, John F. Bower, Eufrânio N. da Silva Júnior
This article presents A-ring functionalized quinones via a modern and efficient new strategy involving the generation and capture of benzyne quinones and their evaluation against Trypanosoma cruzi.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




vi

3-Thio-3,4,5-Trisubstituted-1,2,4-Triazoles: High Affinity Somatostatin Receptor-4 Agonist Synthesis and Structure-Activity Relationships

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




vi

U.S. Presidential polls: Thulasendrapuram residents pray for Kamala Harris ‘victory




vi

Changes in train services notified due to demolition of old bridge near Tiruchi junction




vi

Will decide on sharing stage with actor Vijay in consultation with VCK leaders: Thirumavalavan

Mr. Thirumavalavan told reporters in Tiruchi that the book release event was not something that was planned recently, and that he had consented to take part in it almost a year ago




vi

Heavy weed growth at Kasi Viswanathar Temple tank prevents replenishing of underground water table, say Tiruchi residents




vi

TNSTC Kumbakonam Division mops up ₹17.13 crore in four days




vi

Bids invited for setting up International Dugong Conservation Centre at Manora

The proposed centre, to be set up at an estimate of ₹41 crore, is being established to conserve endangered Dugong species and its habitat in the Palk Bay




vi

‘State should retain primary agricultural cooperative societies under its purview’




vi

566: View Transitions and Passkeys

How should a podcast start? Talking View transitions, Google's Baseline, Passkeys, how to start a company, and ordering a spicy chicken combo at Wendy's.




vi

569: Apple’s Web Apps, Meta Quest and Vision Pro, and Missing Sticky Headers

How do you point out things in a UI? Are Arc Boosts the end of the web? What do you think of VR and AR / Vision Pro and Meta Quest? And what do you do when the sticky header goes missing?




vi

578: Customer Support, P3 Color, Dave on Productivity, and Mobile vs Desktop

Is Apple's Numbers amazing or the worst? Customer support at various levels of software, Figma and P3 color, imagining a colorspace property in CSS, what's Dave doing for productivity, how has offloading CSS Tricks affected Chris, and should we build different websites for mobile vs desktop?




vi

610: TypeScript in 2024, Signals, Productivity Sniped, and Follow Up

Dave's about to be eclipsed, the state of TypeScript in 2024, signals stage zero proposal, corrections on accessibility in frameworks (thanks!), web apps for better collaborative writing, getting productivity sniped, the problem with email may be you, indieweb follow up, and ultimate guitar tab apps.




vi

617: Economic & AI Vibes with Jason Grigsby

We're chatting with Jason Grigsby about what a white-collar recession means, how the sources and methods of consuming news shape our perspectives, whether the current economic conditions represent a market correction and if a rebound is imminent. We explore the critical decision of whether to embrace AI advancements or risk being left behind. We also talk about AI-generated voices, large language models and ethics, and the impact of social media signals in an AI world.




vi

618: Matt Visiwig on SVGBackgrounds

Matt Visiwig stops by to chat with us about his site, SVGBackgrounds.com, a membership site for copy-and-paste website graphics built around SVG. We talk about why he built the site, how he decided to monetize it, competing with AI garbage on the web, pricing membership options, and how he's running the site.




vi

627: Getting Comfortable with the Struggle and Vibe Driven Development

Chris brings some blog posts to talk about including being comfortable with the struggle of developer life, Cloudflare Workers + monorepos, vibe driven development, and questions about database migrations, and whether we think AI free blogs are going to be a rarity in the future?




vi

629: The Great Divide, Global Design + Web Components, and Job Titles

A bit of follow-up on vibe driven development and JavaScript not causing The Great Divide, writing testing automation, global design systems and web components, could PHP be used for web components, what if view transitions are going to be everywhere, and frontend engineer vs design systems engineer job titles and descriptions.




vi

635: Jeff Robbins and Visibox as an Instrument for Video

Jeff Robbins stops by to talk about his software, Visibox, that was used at Frostapalooza for presenting video at the concert, what it's like building an app with Electron, how it's distributed, how files are used and managed, and how he supports hardware devices inside Electron.




vi

640: Navigating the Pros and Cons of Web Components

Riffing off a Dave Rupert blog post, Chris and Dave talk through the pros and cons of web components, when to use them, when it's a bad idea to use them, what would it take to make the Next.js of web components, and how long until we don't need anymore frameworks?




vi

Saving six rivers

Unless an institution is created and armed with powers to manage the Nandi Hills range we will see the gradual demise of a culture centered around water and the death of six rivers.




vi

Are freeways viable?

Barring very few functionally useful ones, many elevated concrete structures with suboptimal utility have ripped the city apart, defiled and marred it.




vi

Towards healthier living

Invest in a green home for long-term benefits, says Arvind Jain




vi

Bikes for last mile connectivity

The Japanese are increasingly shunning cars to help the urban environment get greener.




vi

Visit a wetland, please

Wetlands harbour a tremendous biodiversity of plants and animals, and are also called the “kidneys of the world” because they clean up water as a natural function.




vi

Saving on time, money

Experts feel pre-cast technology could solve housing problems for the economically weaker sections, despite limitations in additions, alterations and repairs.




vi

The four Rs of urban living

Each one of us has a role to play in combating drought and we should adopt the mantra of reject, reduce, reuse and recycle, says S. Vishwanath




vi

Carbon credits to boost incomes of Jharkhand village farmers 

The Birsa Harit Gram project serves as a potential model for agro-forestry, which is gaining ground because the buyers of carbon credits prefer — pay a premium — for credits based on Nature Based Solution, as opposed to offsetting projects like renewable energy or projects like carbon capture.




vi

How Ratan Tata pushed for evidence-led ayurveda 

Ratan Tata sought to promote research that could validate ayurveda through contemporary science




vi

Spotlight on ways to end violence against children