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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.
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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.
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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.
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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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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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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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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...
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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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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.
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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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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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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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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,...
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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




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




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Case filed against actor Kasthuri over remarks on Telugu community




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Deputy CM releases commemorative flag of Bharat Scouts and Guides




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Fishermen seek healthcare and cold storage facilities




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NTK chief Seeman booked for alleged ‘derogatory remarks’ against Karunanidhi




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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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‘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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Nagapattinam MP presses for new express trains, railway line extensions




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




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Students cautioned against drug addiction




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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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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?




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584: Community, Partnerships, Images, and Astro with Fred K. Schott

Fred K. Schott stops by to talk about building community, open source and sponsorship, building on partnerships in the dev community, WordPress + Astro, view transitions, using Discord for support, and leaking secret Astro Studio details.




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595: MedTalk Show, Plagiarism and Code Grifting, and How We’re Testing Code

Blood pressure, stress, and COVID highlight the MedTalk Show portion of this episode, a new "Did You Know" segment about dev tools in Chrome, 4 hour video on plagiarism and code grifters, typography, breaking out of CSS Grid, the oldest things Chris and Dave worked on, and what the testing process is like at Luro or CodePen.




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641: Passkey Usage, Writing Code with a Bot, and What’s Up With Java?

We've got a few leftovers from Halloween to process, what's been happening with Passkeys in late 2024, have you tried to write HTML faster than a bot can suggest it to you, CSS anchor positioning and popover polyfills, scroll driven animation thoughts, CSS nesting, and what's the reason for Java?




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Sunny days are here again

Despite the cost, a solar energy system is a great energy saver and a boon during power cuts, says Anamika Mukherjee




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The fight against encroachment

No one has the right to use precious road space as their private storage yard.




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The management of sludge

There is a need for building bye-laws to insist on a range of on-plot sanitation as mandatory, depending on the location and the groundwater table.




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From agri waste to industrial raw material

altM is developing alternatives to mined materials and petrochemicals 




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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.




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Aggregated customer power

User-friendly financial services are a click away with account aggregators




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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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New venture Zerofifty from ad veterans wants to simplify the agency model

ZeroFifty Mediaworks, set up by three ad veterans, wants to bring in Bandra vibes into the agency model




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Brand expertise and heritage bubbling in a moka pot

Lessons from European brands that have won consumers’ mindspace for long years




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Sport against strokes

World Stroke Day — October 29




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Magnite opus

Improved features, better practicality, and a familiar design, all make the new Nissan Magnite worth a second look




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Spotlight on ways to end violence against children




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Mislabelled agri loans face culling

Why some banks are under the RBI’s lens for demanding gold surety for small-value farm credit




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IAF Mig-29 fighter crashes near Agra, pilot ejects to safety

An enquiry has been ordered by the IAF, to ascertain the cause of the accident




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Two juveniles apprehended for dragging policemen on car’s bonnet 




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Delhi riots case: HC dismisses plea by Khalid Saifi against attempt to murder charge

Mr. Saifi submitted that once the offences under the Arms Act were dropped against him and neither any weapon was recovered nor the alleged gunshot was attributed to him, the charge of attempt to murder could not be framed




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Campaign to discourage open burning from Nov 6, 588 teams to be deployed: Delhi Minister Rai

Mr. Rai said 588 teams from different civic agencies, including the Municipal Corporation of Delhi (MCD), will be deployed to report open burning incidents across the national capital