va

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.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




va

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.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




va

Design, synthesis, and structure–activity relationship studies of 6H-benzo[b]indeno[1,2-d]thiophen-6-one derivatives as DYRK1A/CLK1/CLK4/haspin inhibitors

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00537F, Research Article
Open Access
Abdelfattah Faouzi, Alexandre Arnaud, François Hallé, Jean Roussel, Mandy Aymard, Vincent Denavit, Cong Viet Do, Angélique Mularoni, Mohamed Salah, Ahmed ElHady, Thanh-Nhat Pham, Alexandre Bancet, Marc Le Borgne, Raphaël Terreux, Roland Barret, Matthias Engel, Thierry Lomberget
A series of sulfur-containing tetracycles was designed and evaluated for their ability to inhibit protein kinase DYRK1A, a target known to have several potential therapeutic applications including cancers, Down syndrome or Alzheimer's disease.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




va

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.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




va

Therapeutic upregulation of DNA repair pathways: strategies and small molecule activators

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00673A, Review Article
Juhyung Song, Cheoljun Park, Francis E. B. Cabanting, Yong Woong Jun
Potential therapeutic target proteins for upregulating DNA repair system are reviewed, along with reported small-molecule activators.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




va

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.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




va

Synthesis and evaluation of tetrahydropyrrolo[1,2-a]quinolin-1(2H)-ones as new tubulin polymerization inhibitors

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00541D, Research Article
Mikhail N. Anisimov, Maksim A. Boichenko, Vitaly V. Shorokhov, Julia N. Borzunova, Marina Janibekova, Vadim V. Mustyatsa, Ilya A. Lifshits, Andrey Yu. Plodukhin, Ivan A. Andreev, Nina K. Ratmanova, Sergey S. Zhokhov, Elena A. Tarasenko, Daria A. Ipatova, Alexander R. Pisarev, Ivan A. Vorobjev, Igor V. Trushkov, Olga A. Ivanova, Nikita B. Gudimchuk
New 1,5-disubstituted pyrrolidin-2-ones 1, 2 and 5-aryl-3,3a,4,5-tetrahydropyrrolo[1,2-a]quinoline-1(2H)-ones 3 were explored as inhibitors of tubulin polymerization.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




va

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.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




va

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.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




va

Recent advances from computer-aided drug design to artificial intelligence drug design

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00522H, Review Article
Keran Wang, Yanwen Huang, Yan Wang, Qidong You, Lei Wang
CADD and AIDD contribute to the drug discovery.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




va

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




va

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.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




va

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.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




va

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.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




va

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




va

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




va

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.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




va

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.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




va

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.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




va

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

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.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




va

Adjuvant strategies to tackle mcr-mediated polymyxin resistance

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00654B, Review Article
Madison R. Nuske, Junlang Zhong, Renjie Huang, Vijayalekshmi Sarojini, Jack L. Y. Chen, Christopher J. Squire, Mark A. T. Blaskovich, Ivanhoe K. H. Leung
The emergence of the mobile colistin resistance (mcr) gene is a significant threat contributing to the worldwide antibiotic resistance crisis. This review discusses adjuvant strategies to restore polymyxin sensitivity in these resistant bacteria.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry




va

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




va

Ensure time-bound implementation of development schemes, says Thirumavalavan




va

Ernakulam Express to stop at Muthupettai during Kandhoori festival




va

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




va

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




va

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




va

Advanced baggage handling system introduced in Tiruchi airport




va

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

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.




va

550: Sanity with Simen Svale Skogsrud and Espen Hovlandsdal

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.




va

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??"




va

564: Render ATL, New Colors Available, Gradients, HDR, and More

Chris previews a bit of his Render ATL 2023 talk, and then we mouth blog some color ideas, thoughts, and shame you for your non-HD websites.




va

593: Beep & Texts, Tumblr, JavaScript & Web Components, & Cool Blog Post Ideas

Thoughts on smashing all communication messaging apps together, what's happened to Tumblr under Automattic, what the situation is with native web components and JavaScript, and looking at a list of types of blog posts.




va

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?




va

Perez vs Lawson: A new F1 rivalry

RB driver Liam Lawson apologised to Sergio Perez after the pair clashed at the Mexican Grand Prix but the New Zealand rookie said he would not change his aggressive approach to Formula One racing.




va

CVC has sought report from CPWD over CM House renovation: Delhi LoP




va

Delhi to host 12th edition of North East Festival

More than 200 communities from the eight north-eastern States are expected to showcase their cultural traits on a single platform




va

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




va

Amateur Radio Activated for Late Season Hurricane

A rare November hurricane made landfall in western Cuba as a Category 3 storm Wednesday and continued to move slowly toward the northwest Thursday morning. Volunteer ham radio operators were there to provide surface reports to the National Hurricane Center in Miami.

Hurricane Rafael left Cuba’s 10 million residents without power and on Thursday afternoon was a Category 2 storm moving away from C...




va

Rare California Island to be Activated for Armed Forces Day, First Time in 53 Years

On Armed Forces Day, May 1971, 53 years ago, two amateur operators working as WZ6SNI, activated San Nicolas Island, IOTA NA-066. At 61 miles, San Nicolas is the most remote of the Channel Islands off the coast of Southern California and is owned by the US Navy.

Now, weather permitting, Will Costello, WC6DX, has been authorized to be active from San Nicolas Island November 8 - 12, 2024. He is tak...




va

Values that make a business tick

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




va

Unravelling nuggets of innovation

The journey of Tanishq’s mass market brand GoldPlus




va

Triumphs and travails of a consultant

The book is a detailed job description for anybody wanting to make consulting their career




va

Paddy varieties with protein, zinc content get thumbs up in Odisha’s tribal pocket

Paddy varieties have high protein (10.1%) and moderately high level of zinc (20 ppm) content




va

IISR-Kozhikode develops new high-yielding pepper variety

The variety named ‘IISR Chandra’ is expected to be a game changer in the black pepper industry




va

West Bengal farmers organise indigenous seed festival

Hundreds of farmers from different districts brought native varieties of paddy, pulses and vegetables and exchanged traditional knowledge




va

‘Very sweet’ variety gives fresh hope to Pineapple farmers in Kerala

Possibility for mechanised processing for value addition and export being studied




va

Innovations in traditional methods revolutionising farming in Rajasthan’s parched Shekhawati

The decline in the groundwater level is a major issue for agriculturists in all four districts of Shekhawati — Sikar, Jhunjhunu, Churu, and Neem Ka Thana




va

Space data fuels India's farming innovation drive

Satellite data has gives an Indian farmer optimal sowing times, weather warnings, and better use of irrigation and pesticides




va

 Kuruvai coverage rose by 40% above normal in last five years

The normal coverage is about 3.24 lakh acres for the delta. However, going by the average for the last five years, the figure comes to 4.57 lakh acres — a nearly 40% rise.