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Novel benzenesulfonamides containing a dual triazole moiety with selective carbonic anhydrase inhibition and anticancer activity

By pubs.rsc.org
Published On ::

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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Medicinal chemistry-based perspective on thiophene and its derivatives: Exploring the structural insights to discover plausible druggable leads

By pubs.rsc.org
Published On ::

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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Ligand-centred phenotype-driven development of potent kinase inhibitors against oesophageal cancer

By pubs.rsc.org
Published On ::

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

By pubs.rsc.org
Published On ::

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

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Published On ::

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

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Published On ::

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

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Published On ::

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

By pubs.rsc.org
Published On ::

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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Synthesis of cationic N-acylated thiazolidine for selective activity against Gram-positive bacteria and evaluation of N-acylation's role in membrane-disrupting activity

By pubs.rsc.org
Published On ::

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

By pubs.rsc.org
Published On ::

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

By pubs.rsc.org
Published On ::

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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Generation and capture of naphthoquinonynes: a new frontier in the development of trypanocidal quinones via aryne chemistry

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Published On ::

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00558A, Research Article
Laura P. R. Figueroa, Renato L. de Carvalho, Renata G. Almeida, Esther R. S. Paz, Emilay B. T. Diogo, Maria H. Araujo, Warley S. Borges, Victor F. S. Ramos, Rubem F. S. Menna-Barreto, James M. Wood, John F. Bower, Eufrânio N. da Silva Júnior
This article presents A-ring functionalized quinones via a modern and efficient new strategy involving the generation and capture of benzyne quinones and their evaluation against Trypanosoma cruzi.
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Technical, preclinical, and clinical developments of Fc-glycan-specific antibody–drug conjugates

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Published On ::

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

By pubs.rsc.org
Published On ::

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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3-Thio-3,4,5-Trisubstituted-1,2,4-Triazoles: High Affinity Somatostatin Receptor-4 Agonist Synthesis and Structure-Activity Relationships

By pubs.rsc.org
Published On ::

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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Synthesis and antifungal evaluation of new azole derivatives containing 1,2,3-triazole

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Published On ::

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00724G, Research Article
Zhengxiao Huang, Hongjie Chen, Xiao Zhang, Ruirui Wang, Chunyan Hu, Zewei Mao
A series of novel azole derivatives containing 1,2,3-triazole have been synthesized with good antifungal effects on sensitive and drug-resistant C. albicans.
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Four schools and a college in Tiruchi receive hoax bomb threats

By www.thehindu.com
Published On :: Tue, 05 Nov 2024 14:34:30 +0530

Three schools declared a holiday on Tuesday as a precautionary measure


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Water level in Mettur Dam stands at 107.04 feet

By www.thehindu.com
Published On :: Tue, 05 Nov 2024 16:35:38 +0530


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Water level in Mettur dam stands at 106.89 feet

By www.thehindu.com
Published On :: Wed, 06 Nov 2024 18:06:24 +0530


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HC directs authorities to maintain park and ensure no encroachment

By www.thehindu.com
Published On :: Wed, 06 Nov 2024 21:09:52 +0530


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Deputy CM releases commemorative flag of Bharat Scouts and Guides

By www.thehindu.com
Published On :: Thu, 07 Nov 2024 17:48:40 +0530


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Farmers demand withdrawal of Tamil Nadu Land Consolidation Act

By www.thehindu.com
Published On :: Thu, 07 Nov 2024 17:59:18 +0530

The Coordination Committee of All Farmers’ Associations of Tamil Nadu says the State government has created a situation where industries can acquire fertile lands


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Ernakulam Express to stop at Muthupettai during Kandhoori festival

By www.thehindu.com
Published On :: Thu, 07 Nov 2024 18:51:18 +0530


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

By www.thehindu.com
Published On :: Thu, 07 Nov 2024 19:10:58 +0530

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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Consultant to be appointed soon to design Kalaignar grand library in Tiruchi

By www.thehindu.com
Published On :: Fri, 08 Nov 2024 18:41:18 +0530

The centre will offer translation, services for persons with disabilities and children, training and mentorship programmes, besides hosting monthly literary events


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Fishermen seek healthcare and cold storage facilities

By www.thehindu.com
Published On :: Fri, 08 Nov 2024 19:03:17 +0530


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Small-scale handloom park to come up at Sengunthapuram

By www.thehindu.com
Published On :: Fri, 08 Nov 2024 19:09:38 +0530

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

By www.thehindu.com
Published On :: Fri, 08 Nov 2024 19:20:03 +0530

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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Advanced baggage handling system introduced in Tiruchi airport

By www.thehindu.com
Published On :: Sat, 09 Nov 2024 18:01:36 +0530


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Man attempts to end life, kills his wife and daughter

By www.thehindu.com
Published On :: Sat, 09 Nov 2024 18:03:18 +0530


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

By www.thehindu.com
Published On :: Sat, 09 Nov 2024 18:07:57 +0530


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Water level in Mettur Dam stands at 106.58 feet

By www.thehindu.com
Published On :: Sat, 09 Nov 2024 18:10:37 +0530


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Site identified for small-scale handloom park in Karur

By www.thehindu.com
Published On :: Sat, 09 Nov 2024 19:30:54 +0530


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

By www.thehindu.com
Published On :: Sat, 09 Nov 2024 20:32:48 +0530


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AIADMK ready to join hands with like-minded parties to defeat DMK: Palaniswami

By www.thehindu.com
Published On :: Mon, 11 Nov 2024 00:39:42 +0530


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

By www.thehindu.com
Published On :: Mon, 11 Nov 2024 17:08:51 +0530

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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542: Breaking Up with CSS-in-JS, Mastodon, and Stories on the Web

By shoptalkshow.com
Published On :: Mon, 21 Nov 2022 08:00:51 +0000

We're talking CSS-in-JS, Token CSS, Matuzo being suspended from Twitter, trying out Mastodon, testing out stable diffusion, stories on the web, and Jake Albaugh's new social network.


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543: Zach Leatherman on Eleventy, Mastodon, Twitter, and is-land

By shoptalkshow.com
Published On :: Tue, 29 Nov 2022 16:30:32 +0000

Zach Leatherman talks with us about what's new with Eleventy, setting up on Mastodon, what's happened with Twitter, and is-land.


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

By shoptalkshow.com
Published On :: Mon, 05 Dec 2022 08:15:42 +0000

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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546: Ryan Dahl and Deno

By shoptalkshow.com
Published On :: Mon, 19 Dec 2022 09:11:01 +0000

Ryan Dahl stops by to talk about Node, Deno, JavaScript, testing, V8, and thoughts around getting started with Deno.


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547: WordPress and GraphQL with Jason Bahl

By shoptalkshow.com
Published On :: Mon, 09 Jan 2023 09:31:13 +0000

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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548: Infinite Canvas, Luro + Figma, and Scraping or Crawling

By shoptalkshow.com
Published On :: Mon, 16 Jan 2023 10:41:42 +0000

What's going to happen to homework with AI? Thoughts on infinite canvas which leads into Luro and Sigma integration, and Chris gets nerdsniped and tries to scrap (or should he crawl?) websites for data.


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550: Sanity with Simen Svale Skogsrud and Espen Hovlandsdal

By shoptalkshow.com
Published On :: Mon, 30 Jan 2023 10:11:40 +0000

Simen and Espen from Sanity stop by to talk about the origins of Sanity, how Sanity Studio works, good use cases for Sanity, how Sanity does real time updates, what Groq is, and where to start with Sanity.


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551: PlanetScale with Iheanyi Ekechukwu and Mike Coutermarsh

By shoptalkshow.com
Published On :: Mon, 06 Feb 2023 19:44:27 +0000

Iheanyi Ekechukwu and Mike Coutermarsh talk about PlanetScale, what Vitess is, if PlanetScale is for both side and big projects, what read only regions are, what schema changes are, and how PlanetScale compares to other projects.


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553: TypeScript, DX, GripeScript, and Astro v2 with Fred Schott

By shoptalkshow.com
Published On :: Mon, 20 Feb 2023 10:37:22 +0000

Fred Schott stops by to talk about TypeScript, what DX means in 2023, a bit of GripeScript, and being transparent about what Astro is good at, and what it's not.


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

By shoptalkshow.com
Published On :: Mon, 06 Mar 2023 09:39:37 +0000

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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556: Andrey Sitnik and Using OKLCH for Color

By shoptalkshow.com
Published On :: Mon, 13 Mar 2023 16:38:12 +0000

Andrey Sitnik from Evil Martians talks with us about why OKCLH is the best way forward for color on the web, how to incorporate it into design systems, getting your designers to use OKCLH, and what kind of fallback support is needed.


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557: ChatGPT, Conferences, Fidgets on the Web, and Modern CSS in Real Life

By shoptalkshow.com
Published On :: Mon, 20 Mar 2023 07:01:51 +0000

When will AI be able to tell you the risk / reward of cleaning up trees? Are conferences back? Bringing fidgets to the web, internet as an anxiety machine, and Chris is working on talk on modern CSS in real life.


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560: Oh Biscuits! Cascade Layers, Block Links, Emoji Lists, and more CSS!

By shoptalkshow.com
Published On :: Mon, 10 Apr 2023 08:53:57 +0000

After a brief visit from Hip Hop Dad Dave, we're talking cascade layers updates, block link practices, search element getting dropped, how to use cite, emoji list accessibility, scrollbar state, and trigonometric functions in CSS.


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561: Web Perf News, Web Sommelier, Data Analytics, and Passkeys

By shoptalkshow.com
Published On :: Mon, 17 Apr 2023 08:00:36 +0000

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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