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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.
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Continuous flow synthesis of N,N-dimethyltryptamine (DMT) analogues with therapeutic potential

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00562G, Research Article
Open Access
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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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.
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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.
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Medicinal chemistry-based perspective on thiophene and its derivatives: Exploring the structural insights to discover plausible druggable leads

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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A decade of pyridine-containing heterocycles in US FDA approved drugs: a medicinal chemistry-based analysis

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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Miniaturized click chemistry and direct screening facilitate the discovery of triazole piperazine SARS-CoV-2 Mpro inhibitors with improved metabolic stability

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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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.
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Design, synthesis, and biological evaluation of pyrazole–ciprofloxacin hybrids as antibacterial and antibiofilm agents against Staphylococcus aureus

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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Design and synthesis of (E)-3-benzylideneindolin-2-one derivatives as potential allosteric inhibitors of Aurora A kinase

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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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.
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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.
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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.
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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.
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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.
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Light enhanced cytotoxicity and antitumoral effect of a ruthenium-based photosensitizer inspired from natural alkaloids

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00600C, Research Article
Open Access
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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A practical guide for the assay-dependent characterisation of irreversible inhibitors

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




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




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Frequent traffic snarls pose hardship to motorists in Tiruchi

It is common to see vehicles lining up for a long distance from the traffic signal near Cauvery bridge to Anna Statue.




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Agro-tourism push needs industry-specific policies, say farmers




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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




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Tiruchi district SHGs compete to prepare healthy millet-based recipes at food festival

Women entrepreneurs urged to take advantage of social media platforms to advertise and market their products to a wider customer base




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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




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Art and literary contests lined up for District Central Library’s National Library Week




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Tiruchi Corporation office expansion plan witnesses more delay




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




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Students and agriculture officials grapple with logistical, technical issues during digital crop survey




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Students cautioned against drug addiction




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Lack of signboards indicating bus timings at Chathiram Bus Stand in Tiruchi irks passengers

Passengers also say some buses leave earlier than scheduled or don’t pass certain rural areas, leading to schoolchildren not being able to board on time




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Live Cricket Scores, Cricket News, Analysis, Results & More | The Hindu




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555: React Documentary, Front of the Front End, Fast Fallacy, and Best Practices

Reacting to the React.js documentary, is there still jobs for front of the front end anymore? The fast fallacy in frameworks, best practices, dealing with too much or too little isolation, and AI test generation.




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558: Esoteric Weird Content Editable Problems with Kristin Valentine

Kristin Valentine from Vox joins the show to talk about text editor CMS fun across multiple sites, Vox's Chorus, The Verge redesign, sharing Design Systems, theming articles, and a fun new game called "Can Your Text Editor Do This??"




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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.




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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?




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571: Searching vs AI, Getting Designers to Play Nice, and Web Components

Do you listen at 2x? Do Chris and Dave sound weird at normal speed IRL? How searching compares to using AI, chatbots kind of suck at context, getting a designer to work with developers at an agency, what happened to content visibility, and how to best build a design system using web components.




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573: Google Reader, Sticky and Overflow, and Figma Thoughts

Chris breaks out his banjo, some thoughts on making music vs recording music, what happened to Google Reader and social reading, what black box properties can't Dave or Chris remember, follow up for dev teams communicating with designers, and what's Adobe going to do about Figma?




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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.




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579: One Day Builds, Spicy Slugs, and What Next for CSS?

Have you ever been an auctioneer? Sometimes when God closes a shed, he opens a sauna. Dave's working on the one day build theory, how to market with fake data, an update on the Discord, marketing with a spicy slug, what we want to see next in CSS, and thoughts on component libraries.




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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.




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582: Lifetime Plan, Pricing #HotDrama, and CSS Resets

Getting tripped up on audio at conferences, announcing the ShopTalk Show Lifetime Plan, some Once pricing #hotdrama, remembering Molly Holzschlag, web components, Luro launch day thoughts, and a question about using a normalize or sanitize in 2023 prompts a run through of Andy Bell's Modern CSS Reset.




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586: Micro.blogging with Manton Reece

Manton Reece, creator of Micro.blog, stops by to talk about the history of Micro.blog, what it's written in, how it handles feeds coming in and going out, cross-posting, authentication, and the somewhat hidden features of Micro.blog: bookmarking, bookshelves, and even podcasting.




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594: Wiping Your Laptop, UX of Password Codes, and :Has Tips and Tricks

In this episode we're discussing making tech videos, website tinkering, :has tricks, SVG path commands, and the complexities of CSS & JavaScript logic.




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604: VS Code Plugins, Git as a Radical Statement, Tailwind & Arc Drama

A follow up on jQuery conversation, Microsoft owning all the things, what VS Code plugins are your ride or die, the ability to Git from wherever you want, Tailwind drama, global design system follow up, Arc Search gets roasted, and Frontend Design Conference is back!




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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 […]




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611: React! TypeScript! Jobification! Drupal!

Dave & Chris and thoughts on career advice that worked 3 years ago but isn't as helpful now, marking tests with ChatGPT, is taking a Drupal job in 2024 a good idea, Chris got #gear sniped, P3 color follow up, the confusing File System APIs, and where did all the lightboxes go?




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613: Recording Live Music, WebC, Open Source, & WordPress Studio

Chris bought recording gear off an Instagram ad, our thoughts on WebC, CodePen upgrades Yarn, thoughts on the commercial value of open source, Automattic releases an app to install WordPress locally, IBM buys Hashicorp, income tax software, and a hack for getting Safari to respect background colors used in a pseudo selector.




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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.




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623: Assigning Weight Dynamically, CoPilot vs Other AI, and Monorepos

We're talking about assigning a weight to items in a layout, differentiating between banger posts and regular blog posts, using social engineering to get PR's accepted, monorepo thoughts, using CoPilot vs other AI programming support bots, has TypeScript benefited from AI, and what happens if you turn off CoPilot?