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




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




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




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




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




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Nagapattinam MP presses for new express trains, railway line extensions




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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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576: Blocks, Components, Linting Images, Engines, and “Web Integrity”

We're talking how we stay online - or not - on vacation, is create-guten-block the future for us WP developers? Can we get a state of the web component address from the President of web components? Have we seen the last new browser engine? And deciding whether to add features or remove them from your app.




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589: CSS Functions, Read It Later, Making Money in Business, and More

A quick bit of union news follow up, CSS function round up, Read It Later inside Feedbin, fun uses for a Stream Deck+, how to turn up the money dial in your own business, and having the audacity to call yourself a publisher.




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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.




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616: Strum Machine with Luke Abbott

Luke Abbott is the creator of Strum Machine, an app that simulates backing tracks by stitching together individual notes, chords, and strums recorded on guitar, standup bass, and mandolin. We talk about what Strum Machine does, why he decided to build it, how bringing on a professional designer helped, pricing thoughts, and the "fun" of building a version on iOS.




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628: Tending to RSS Feeds, Code Hike’s Fine Markdown, and Cloudflare R2

Doc told me to travel but there's COVID on the planes, Dave's got a 2x life update, how often do you manage or prune your RSS feed subscriptions, checking in on Code Hike and their fine grained Markdown approach, JavaScript decorators use case, and using Cloudflare R2 for image storage.




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633: Thomas Steiner on AI in Chrome and the Web

Thomas Steiner from Project Fugu talks with us about AI in Chrome, the small large language model in use, how features like this are rolled out, the ethics and concerns around sending and sharing data, on device vs web APIs, and ideas for use cases and ways to explore AI on the web.




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636: W Hot Drama Week (WordPress, WP Engine, and Web Components – Oh My!)

We're getting some feelings out about WordPress and Matt Mullenweg vs WP Engine drama, as well as the Web Components conversation that happened this past week.




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Sunshine cities

Kochi and Thiruvananthapuram are among the 60 cities that have received in principle approval from the Union Ministry of New and Renewable Energy to be developed as Solar Cities, 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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Why we need lane discipline

Stick to the left lane when making a turn, even in smaller lanes




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A premium for cleanliness

If you’re looking at buying a home, take a pick from one of India’s cleanest cities.




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Ferrari's Leclerc fined for swearing

Stewards at the Brazilian race summoned Leclerc on Friday, acting on a report from the governing FIA's media delegate and after reviewing a written transcript.




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The last thing business founders need is a wasteful public spat

As entrepreneurship explodes in India, we need more iconic founders who not only build sustainable firms but also retain their humility




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Flat organisation believers: Can you imagine a world without managers?

What does a manager do that we keep hiring new ones or keep promoting more of them? Which managerial layer is the most important?




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Cargo companies upsize for new business

Booming demand for ecommerce delivery spurs freight handlers to open more centres, digitise for efficiency




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Senior feline resident: Defib stays at his ambulance station 

Online petition halts re-homing of 16-year-old cat in London




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Making medicines at the point of patient care

UK readies law allowing preparation of medicines near hospital setting to reach patients safely, quickly




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Planned meals, personal trainer, and a tea for every reason

Personal fitness diary




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Delhi election: AAP to hold nine-day convention for party workers




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Delhi cop Nidhin Valsan’s inspiring journey from arresting cancer to Ironman finish line

Diagnosed with stage 4 non-Hodgkin’s lymphoma in 2021, IPS officer Nidhin Valsan resurrected himself by competing the Ironman triathlon and writing his memoir because he hopes to be a good influence on other cancer patients




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Delhi HC imposes ₹10,000 fine on advocate for casting aspersions on judge




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Delhi Cabinet passes proposal for reinstatement of bus marshals




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ARRL Members Raise $47,000 for STEM Education in Online Auction

ARRL® The National Association for Amateur Radio® is pleased to announce that the 19th annual ARRL Online Auction, sponsored by RT Systems Inc, raised $47,000 for amateur radio STEM education. 

The event was held from October 18- 24, 2024. In addition to hundreds of views, the auction saw 329 individual bidders vying for equipment, vintage books, “mystery junk boxes” from the ARRL Lab, and more....




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Amazon is designed to spin like a flywheel: Brian Dumaine

In Bezonomics, the Fortune jounralist explains how Jeff Bezos has shrewdly changed the way business is done in today’s world




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Can India arrest income inequality?

Thomas Piketty’s prescriptions are too radical. Dattopant Thengadi’s vision is more useful for us




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Values that make a business tick

The authors use their experience to show that business should be about ethics, dharma and more




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Cashing out of a business, smartly

The book draws upon diverse experiences of entrepreneurs to highlight the need for an exit strategy




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The inevitability of uncertainty

The book tells us quite convincingly that the future is unknown. But it does not offer an alternative




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International conference to recommend policies to address gender inequality at farms

“The conference aims to promote the sharing of cutting-edge knowledge on gender and inclusion in agri-food systems.”