el

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




el

Azo derivatives of monoterpenes as anti-Helicobacter pylori agents: from synthesis to structure-based target investigation

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00511B, Research Article
Open Access
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.
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




el

Recent advances from computer-aided drug design to artificial intelligence drug design

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.
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




el

Ligand-centred phenotype-driven development of potent kinase inhibitors against oesophageal cancer

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00579A, Research Article
Open Access
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.
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




el

S-MGBs bearing amidine tail groups are potent, selective antiplasmodial agents

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00619D, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
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.
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




el

A novel approach for the synthesis of the cyclic lipopeptide globomycin

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00685B, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Samantha J. Bann, Stephen A. Cochrane
Lipid swapping: a new approach for the synthesis of globomycin that allows for facile lipid diversification.
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




el

Novel quinoxaline-derived derivatives: design, synthesis, bioactive evaluation, SARs and preliminary antibacterial mechanism

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




el

Metal-free synthesis of N-fused quinazolino-quinazoline-diones as a MALAT1 RNA triple helix intercalator

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.
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




el

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




el

Synthesis, in silico and bio-evaluation studies of new isothiocyanate derivatives with respect to COX inhibition and H2S release profiles

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.
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




el

meso-Substituted AB3-type phenothiazinyl porphyrins and their indium and zinc complexes photosensitising properties, cytotoxicity and phototoxicity on ovarian cancer cells

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00601A, Research Article
Open Access
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.
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




el

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




el

Discovery of N-substituted-2-oxoindolin benzoylhydrazines as c-MET/SMO modulators in EGFRi-resistant non-small cell lung cancer

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.
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




el

Technical, preclinical, and clinical developments of Fc-glycan-specific antibody–drug conjugates

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00637B, Review Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Qiang Yang, Yunpeng Liu
Fc-glycan-specific ADC is a significant advance in site-specific ADCs for cancer therapy. Notably, JSKN003 and IBI343 have demonstrated promising results in phase 1 clinical trials and are advancing into phase 3 studies.
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




el

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




el

SIGMAP: an explainable artificial intelligence tool for SIGMA-1 receptor affinity Prediction

RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00722K, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
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...
The content of this RSS Feed (c) The Royal Society of Chemistry




el

Water level in Mettur Dam stands at 107.04 feet




el

Water level in Mettur dam stands at 106.89 feet




el

Ensure time-bound implementation of development schemes, says Thirumavalavan




el

Case filed against actor Kasthuri over remarks on Telugu community




el

Deputy CM releases commemorative flag of Bharat Scouts and Guides




el

Udhayanidhi lays foundation stone for infrastructure development projects in Thanjavur district

Buildings at the Government Arts and Science College, Thirukkattupalli, construction of compound wall and an indoor stadium at the Government Rajah Serfoji College, Thanjavur, are among the projects




el

High-level committee formed to facilitate clearances for companies that signed MoU, says Minister

Constant monitoring was being done now from the time of signing of MoUs to providing employment in new industrial units, says Industries Minister T.R.B. Rajaa




el

Uppiliyapuram, gateway to scenic Pachamalai, lacks bus stand with passengers left to fight the elements

Buses stop at a busy junction making it difficult for commuters as well as local businessmen; a site is yet to be identified for the bus stand




el

Guidelines issued for fertilizer distribution in Karaikal for samba, thaladi paddy cultivation




el

EPS’s dream of AIADMK staging a comeback in 2026 election will not materialise: Law Minister Regupathy




el

Library to hold Group II-A Mains, Group IV TNPSC model test




el

Water level in Mettur Dam stands at 106.58 feet




el

Tiruchi Corporation office expansion plan witnesses more delay




el

Association holds protest against delay in Anna University’s staff absorption, promotions




el

543: Zach Leatherman on Eleventy, Mastodon, Twitter, and is-land

Zach Leatherman talks with us about what's new with Eleventy, setting up on Mastodon, what's happened with Twitter, and is-land.




el

559: Fidget Apps, Coding with AI, Dialog Element Navs, Getting Rid of CSS

Is there still any value in specializing in front-of-the-frontend dev? Would you ever use the dialog element for a mobile navigation? Why did CodePen decide to use Go for its GraphQL server?




el

561: Web Perf News, Web Sommelier, Data Analytics, and Passkeys

Topics for this one include how do you learn about web performance news? Do you need a web components sommelier? Our thoughts on Syntax going to Sentry, and being able to focus on the things you want to focus on. Passkeys, Arc split screen, and vibe driven development.




el

567: Full Stack Dev, Load Bearing Developer, and Being Zod Curious

What do you do if your computer dies? Chris applies to work at Luro, Dave applies at CodePen, Dave's Zod curious, TypeScript, sorting out a 10MB blog post, and how much do you miss jQuery?




el

568: Display Contents, Passkeys Follow Up, Yellow Fade Technique, and TOTK Talk

Macho Man Randy Standards stops by for a quick chat, Passkeys follow up, discussing the safety of Display: contents, the yellow fade technique, how hot CSS is right now (so hot), and a check in on how everyone's doing with Tears of the Kingdom.




el

570: Haircut Maintenance, Dave’s Bookshelf, Lazy Loading, and APIs

We're talking Dave's new haircut, playing Hondo, what Dave uses for images on his bookshelf page, lazy-loading thoughts, vh vw follow up, eyeball tracking updates, loading website with js, Vue transitions, charging for API access, and do you cross post, one post, or no post on social media in 2023?




el

572: Text Sqwunch Property, Figma Developer Mode, Stripe Elements

Show DescriptionDave reports back from the Figma Conference, how to build a better developer to designer bridge, do clients really want to update their website, using Stripe in 2023, permissions and sharing, and are you feeling overwhelmed by CSS in 2023? Listen on Website →Links Config 2023 | Figma’s Annual Conference Figma Visual Studio Code […]




el

574: Estelle & Eric on CSS The Definitive Guide, 5th Edition

Estelle Weyl and Eric Meyer join us to talk about the 5th edition of their book, CSS: The Definitive Guide. We talk about some of CSS' biggest blunders, custom scroll bars, single line comments, shorthand in CSS, useless CSS trivia, and how to get started learning CSS in 2023.




el

581: DevRel, Musical Mics, Social Sharing, and 100 Years of WordPress

Dave calls a quick Luro branding meeting, some thoughts on DevRel, Chris tries to figure out musical instrument mics, follow up on WordPress from a previous episode, Chris' journey through the social graph options, 100 year hosting with WordPress, and the introduction of a new segment: Happy Project Share Time.




el

583: Language Models, AI, and Digital Gardens with Maggie Appleton

Maggie Appleton talks with us about her work at Elicit, working with large and small language models, how humans vet the responses from AI, the discussion around the Soggoth meme in AI, using Discord as UI, what to do if your boss wants AI in your app, and why does she call her blog a digital garden?




el

588: Elliott Marquez on Web Components and Lit

Elliot Marquez talks with us about the history of Polymer and Lit, why you should pick Lit, working with web components, the shadow dom, managing state, and how Material design is built with web components.




el

598: Jen Simmons on Interop, WebKit Releases, and New CSS Features in Safari

Jen Simmons, Apple Evangelist on the Web Developer Experience team for Safari & Webkit, stops by to talk about what Interop is, and a look ahead at new CSS features in Webkit and Safari such as JPEG XL, masks, a round function, JavaScript improvements, styling form controls, content unblocks, masonry, and more!




el

605: Jim Nielsen on Subversive URLs, Blogging + AI, and Design Engineers

Jim Nielsen joins us to about URLs and linking as the new subversive way to maintain the web, paying for news in Canada, should content creators be worried about AI, the case for design engineers, RSS in HTML, and the state of state and UI.




el

606: Web Sustainability with Michelle Barker

Show DescriptionWe're talking with Michelle Barker about the idea of paying to support bloggers (and podcasters!) via services like Patreon, drumming as a fun side gig from CSS, how big of an issue digital sustainability is, trying to understand the environmental impact of our websites and digital life, wondering why YouTube embeds are still so […]




el

614: CSS Grid Level 3 aka Masonry with Adam Argyle

Adam Argyle stops by to chat about the conversation that's happening around CSS Grid / Masonry. What do we want? What might Apple's response to Google be? And nitpicking the spec just for fun.




el

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?




el

632: Adam Coster on Game Development and Crashlands 2

Adam Coster talks with us about working with his family in game development, how they get started making games, what all is involved with publishing games, deciding to go Steam and Netflix only for Crashlands 2, how web tech is involved in game development, and the fun of testing and doing Q&A for games.




el

Reuse greywater wisely

Treating greywater rather than transferring it to an STP has numerous benefits, says Indukanth Ragade




el

Webcams & borewells

A groundwater expert uses a webcam to find out the yield from borewells and identify problems. By




el

Earth as shelter

Traditionally, people built walls by placing mud mixed with jaggery, grass and such local additives, but today we have scientifically evolved mix with cement and quarry dust.