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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.
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Rationally modified SNX-class Hsp90 inhibitors disrupt extracellular fibronectin assembly without intracellular Hsp90 activity

RSC Med. Chem., 2024, 15,3609-3615
DOI: 10.1039/D4MD00501E, Research Article
Open Access
Gciniwe S. Mathenjwa, Abir Chakraborty, Abantika Chakraborty, Ronel Muller, Mathew P. Akerman, Moira L. Bode, Adrienne L. Edkins, Clinton G. L. Veale
Rationally modified Hsp90 inhibitors which retained of on-target activity but showed no engagement of intracellular Hsp90, or stimulation of the heat shock response, were found to significantly alter the extracellular fibronectin network.
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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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Exploring 7β-amino-6-nitrocholestens as COVID-19 antivirals: in silico, synthesis, evaluation, and integration of artificial intelligence (AI) in drug design: assessing the cytotoxicity and antioxidant activity of 3β-acetoxynitrocholestane

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00257A, Research Article
Shahabuddin, Uzma, Mohammad Azam, Mehtab Parveen, Nurul Huda Abd Kadir, Kim Min, Mahboob Alam
In light of the ongoing pandemic caused by SARS-CoV-2, effective and clinically translatable treatments are desperately needed for COVID-19 and its emerging variants.
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A novel, glutathione-activated prodrug of pimasertib loaded in liposomes for targeted cancer therapy

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00517A, Research Article
Open Access
Arianna Amenta, Susanna Comi, Marcelo Kravicz, Silvia Sesana, Antonia Antoniou, Daniele Passarella, Pierfausto Seneci, Sara Pellegrino, Francesca Re
A novel, glutathione-activated prodrug of pimasertib (PROPIMA) has been developed. PROPIMA showed ability to inhibit tumour cell migration and proliferation controlled over time, while also achieving a high incorporation rate into liposomes.
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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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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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Synthesis and biological evaluation of novel D-ring fused steroidal N(2)-substituted-1,2,3-triazoles

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00297K, Research Article
Branislava Tenjović, Sofija Bekić, Andjelka Ćelić, Edward Petri, Julia Scholda, Florian Kopp, Marija Sakač, Andrea Nikolić
In this study, a series of 13 new D-ring fused steroidal N(2)-substituted-1,2,3-triazoles were synthesized, characterized and evaluated for their biological activities.
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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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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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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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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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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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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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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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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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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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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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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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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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Duo arrested for possession of banned tobacco products worth ₹3 lakh in Tiruchi




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Pumping stations to be set up in eight low-lying areas in Tiruchi to prevent inundation




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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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Bids invited for setting up International Dugong Conservation Centre at Manora

The proposed centre, to be set up at an estimate of ₹41 crore, is being established to conserve endangered Dugong species and its habitat in the Palk Bay




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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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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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Small-scale handloom park to come up at Sengunthapuram

Ministers R. Gandhi and S.S. Sivashankar inspect the 13,205 sq. ft. site belonging to the Tamil Nadu Cotton Corporation at Sengunthapuram




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




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Tiruchi Corporation office expansion plan witnesses more delay




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Nagapattinam MP presses for new express trains, railway line extensions




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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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545: Arc Browser with Nate Parrott

Nate Parrott from The Browser Company of New York stops by to talk about Arc - including the history of Arc, how boosts work, building out dev features, how they deciding on what features to build, and feedback from Dave and Chris on Arc.




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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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575: CSS Errors, Proxy and Reverse Proxy, and What’s The Edge?

Bluesky adds first class support for urls as a username, text-wrap pretty update, sqwunching text update, should CSS spit out errors, anchor functionality, what does the edge mean, eSports and bowling, how to test websites on slower CPUs, and what does proxy or reverse proxy mean?




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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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587: Why Ethan Marcotte Thinks Tech Workers Deserve a Union

Ethan Marcotte is here to talk about his new book, You Deserve a Tech Union, and discusses topics such as why we need unions in tech, who gets to be in the union, how unions can help deal with the AI question, union busting, and some arguments against unions.




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592: Web Component Therapy, SEO Therapy, and Learning Something New like Swift

Talking web components, progressive enhancement, style-able components, having to pay before you get to see a demo, being annoyed at the business of SEO, and subscriptions vs ads.