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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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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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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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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.
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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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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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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.
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Advances in antibacterial agents for Mycobacterium fortuitum

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00508B, Review Article
Carlos Roberto Tavolari Jortieke, Angélica Rocha Joaquim, Fernando Fumagalli
This review presents the recent findings on antibacterial agents against Mycobacterium fortuitum and reveals the most promising and effective chemical frameworks to inspire the development of new drugs.
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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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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...
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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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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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Property-based optimisation of PROTACs

RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00769G, Opinion
James Scott, Iacovos Michaelides, Markus Schade
PROTACs are an emerging therapeutic approach towards targeted protein degradation. This article examines the leading examples of this modality that are in clinical development through the prism of their physicochemical...
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Duo arrested for possession of banned tobacco products worth ₹3 lakh in Tiruchi




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TNSTC Kumbakonam Division mops up ₹17.13 crore in four days




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Urban Primary Health Centre stuck in cramped, temporary facility




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Property owners block the entrance to Balasubramanya temple in Karur




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Tiruchi Corporation embarks on special drive at night to capture and sterilise street dogs

About 125 stray dogs have been caught and sterilised at Tiruchi animal birth control centres in the last 10 days after the Corporation launched the special drive




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




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




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Advanced baggage handling system introduced in Tiruchi airport




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544: Feedback, RSS Talk, Arc Brower, and Product Talk

Getting feedback for what you're building or writing, RSS feed reminiscing, Arc browser thoughts, products that didn't make that should have.




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547: WordPress and GraphQL with Jason Bahl

Jason Bahl joins the show to talk about the GraphQL and WordPress connection, his work on WP GraphQL plugin, Faust and Atlas from WP Engine, Jamstack and Wordpress, and more.




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601: Brad Frost on A Global Design System + Frostapalooza

Brad Frost has got design systems on his mind—at a global scale. What is a global design system? Are two design systems ever the same? How would this slot inside atomic design? What has been the response from the web community to global design system as an idea? And what's Frostapalooza?




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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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607: Astro Launches an Integrated Database

Fred K. Schott stops by to talk about Astro announcement of Astro DB, the pluses and minuses of it, whether you have to always use the database with Astro DB, how to migrate data, seeding your database, upgrading the database, and what about Astro DB pricing?




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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.




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624: Blogging, In App Browsers are Bad, and Teaching CSS from Scratch

On this epsiode we're talking about the current state of blogging and social media, the polyfill hack, whether in app browsers should be banned, web components and the difficulty of front end web dev, and how we would go about teaching CSS from scratch in 2024.




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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.




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630: Frostapalooza Recap, Follow Up, and Messy Codebases

Chris has a birthday today 🎉, we recap our Frostapalooza experience celebrating Brad Frost's birthday, do all codebases become a mess, Mermaid, TLDraw, and Figjam thoughts, making tiny games, where's the follow up in web and world news, and what's the current state of CMS' on the web?




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639: DX, JSON, XML, HTML, and Databases! Oh My!

How important is the DX of software vs how important is the person showing off the software, Douglas Crockford and JSON, remembering XML, trying to write better HTML for email, new TC39 proposal, workshopping t-shirts, and what do you do if you want a little bit of database on your website?




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Laying a strong base

The Centre has various plans to meet the housing needs of the country, writes K.A. Martin




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Guidelines for green urbanisation

The Ministry of Urban Development has proposed environmental guidelines for construction projects in urban areas. Nidhi Adlakha reports




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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




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Balrampur Chini hopes success of polylactic acid plant will be sweet

In conversation with Avantika Saraogi, ED, and Stefan Barot, President, Chemicals Division, Balrampur Chini Mills




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How ‘priority sector’ status can rev up Jan Dhan banking

How regulation can nudge private banks to promote financial inclusion




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Urban Safari

Old or new, whichever iteration of the Tata Safari you look at, there’s a lot of charm, utility, and driving appeal, but which one gets our vote?




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The delicate balance in doctor-patient interaction

How clear communication and accountability in healthcare can significantly improve patient outcomes




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Putting cholera back in focus

Surge in cholera cases renews attention on the need to fortify public health




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Why banks are branching furiously

From financial inclusion to wooing back savings deposits, lenders have reasons to reject digital-only mode




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Galathea Bay: New major port can be game changer

Transshipment port at Galathea Bay is strategically located on the East-West international trade and shipping route




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A ‘shadow ban’ in plain sight

The confusion and stigma surrounding the ‘morning after’ pill puts women’s health at risk




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Indo National plans battery of home-care launches

The maker of Nippo batteries plans to innovate in its core business and get into LED bulbs




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Getting the gig economy to care for its backbone

Why startups in India cannot afford to take a hands-off approach towards the armies of gig workers they have created




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Bengaluru startup develops new tech for battery recycling, begins production

Li-ion battery recycler Metastable Materials launches commercial ops




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Toxic air chokes urban India 

Residents grapple with respiratory, cardiac, and other ailments as the air thickens