x

Lead optimisation of OXS007417: in vivo PK profile and hERG liability modulation to optimise a small molecule differentiation agent for the potential treatment of acute myeloid leukaemia

RSC Med. Chem., 2024, 15,3495-3506
DOI: 10.1039/D4MD00275J, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Thomas J. Cogswell, Laia Josa-Culleré, David Zimmer, Sébastien R. G. Galan, Morgan Jay-Smith, Kate S. Harris, Carole J. R. Bataille, Thomas R. Jackson, Douzi Zhang, Stephen G. Davies, Paresh Vyas, Thomas A. Milne, Graham M. Wynne, Angela J. Russell
The optimisation of a class of AML differentiation agents is described to show improved potency, solubility and stability, reduced off target toxicity, and tumour regression in a murine model in vivo.
The content of this RSS Feed (c) The Royal Society of Chemistry




x

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




x

Synthesis and cytotoxic activity of madecassic acid–silybin conjugate compounds in liver cancer cells

RSC Med. Chem., 2024, 15,3418-3432
DOI: 10.1039/D4MD00170B, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Chien Van Tran, Thao Thi Phuong Tran, Anh The Nguyen, Loc Van Tran, Ninh Thi Pham, Luu Thi Nguyen, Dung Thi Nguyen, Michelle D. Garrett, Nga Thi Nguyen, Thao Thi Do, Christopher J. Serpell, Sung Van Tran
Madecassic acid and silybin have been conjoined to produce hybrid compounds with improved and different activity against liver cancer cells.
The content of this RSS Feed (c) The Royal Society of Chemistry




x

A comprehensive apoptotic assessment of niloticin in cervical cancer cells: a tirucallane-type triterpenoid from Aphanamixis polystachya (Wall.) Parker

RSC Med. Chem., 2024, 15,3444-3459
DOI: 10.1039/D4MD00318G, Research Article
Anuja Gracy Joseph, Mohanan Biji, Vishnu Priya Murali, Daisy R. Sherin, Alisha Valsan, Vimalkumar P. Sukumaran, Kokkuvayil Vasu Radhakrishnan, Kaustabh Kumar Maiti
Niloticin, a triterpenoid from Aphanamixis polystachya, induces apoptosis in HeLa cells which is primarily validated through in silico analysis and subsequently in vitro apoptotic evaluation by modulating the apoptotic proteins.
The content of this RSS Feed (c) The Royal Society of Chemistry




x

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




x

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




x

Exploring apoptotic induction of malabaricone A in triple-negative breast cancer cells: an acylphenol phyto-entity isolated from the fruit rind of Myristica malabarica Lam.

RSC Med. Chem., 2024, 15,3558-3575
DOI: 10.1039/D4MD00391H, Research Article
Pothiyil S. Vimalkumar, Neethu Sivadas, Vishnu Priya Murali, Daisy R. Sherin, Madhukrishnan Murali, Anuja Gracy Joseph, Kokkuvayil Vasu Radhakrishnan, Kaustabh Kumar Maiti
Malabaricone A isolated from Myristica malabarica induces apoptosis in triple-negative breast cancer cells through intrinsic and extrinsic pathways, which is validated through in vitro and in silico studies and resembles a potent phyto-entity.
The content of this RSS Feed (c) The Royal Society of Chemistry




x

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




x

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




x

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.
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




x

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.
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




x

Correction: Anti-schistosomal activity and ADMET properties of 1,2,5-oxadiazinane-containing compound synthesized by visible-light photoredox catalysis

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD90044H, Correction
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Kennosuke Itoh, Hiroki Nakahara, Atsushi Takashino, Aya Hara, Akiho Katsuno, Yuriko Abe, Takaaki Mizuguchi, Fumika Karaki, Shigeto Hirayama, Kenichiro Nagai, Reiko Seki, Noriko Sato, Kazuki Okuyama, Masashi Hashimoto, Ken Tokunaga, Hitoshi Ishida, Fusako Mikami, Kofi Dadzie Kwofie, Hayato Kawada, Bangzhong Lin, Kazuto Nunomura, Toshio Kanai, Takeshi Hatta, Naotoshi Tsuji, Junichi Haruta, Hideaki Fujii
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




x

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




x

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




x

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




x

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




x

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.
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




x

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.
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




x

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




x

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




x

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.
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




x

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.
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




x

SIGMAP: an explainable artificial intelligence tool for SIGMA-1 receptor affinity Prediction

RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00722K, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Maria Cristina Lomuscio, Nicola Corriero, Vittoria Nanna, Antonio Piccinno, Michele Saviano, Rosa Lanzilotti, Carmen Abate, Domenico Alberga, Giuseppe Felice Mangiatordi
Developing sigma-1 receptor (S1R) modulators is considered a valuable therapeutic strategy to counteract neurodegeneration, cancer progression, and viral infections, including COVID-19. In this context, in-silico tools capable of accurately predicting...
The content of this RSS Feed (c) The Royal Society of Chemistry




x

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




x

Four schools and a college in Tiruchi receive hoax bomb threats

Three schools declared a holiday on Tuesday as a precautionary measure




x

Govt. urged to extend last date to pay crop insurance premium by farmers




x

Ernakulam Express to stop at Muthupettai during Kandhoori festival




x

Tiruchi Corporation office expansion plan witnesses more delay




x

Nagapattinam MP presses for new express trains, railway line extensions




x

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

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.




x

572: Text Sqwunch Property, Figma Developer Mode, Stripe Elements

Show DescriptionDave reports back from the Figma Conference, how to build a better developer to designer bridge, do clients really want to update their website, using Stripe in 2023, permissions and sharing, and are you feeling overwhelmed by CSS in 2023? Listen on Website →Links Config 2023 | Figma’s Annual Conference Figma Visual Studio Code […]




x

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?




x

579: One Day Builds, Spicy Slugs, and What Next for CSS?

Have you ever been an auctioneer? Sometimes when God closes a shed, he opens a sauna. Dave's working on the one day build theory, how to market with fake data, an update on the Discord, marketing with a spicy slug, what we want to see next in CSS, and thoughts on component libraries.




x

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.




x

594: Wiping Your Laptop, UX of Password Codes, and :Has Tips and Tricks

In this episode we're discussing making tech videos, website tinkering, :has tricks, SVG path commands, and the complexities of CSS & JavaScript logic.




x

608: Can WordPress Kill Your Resume, Fav Parts of Web Dev, Exploring HTMX, and more!

We're opening up the ShopTalk mailbag and answering your questions, including does WordPress on your resume kill your job chances, what are our fav and least fav parts of web dev, our thoughts on HTMX, and what is it like to use pnpm instead of npm.




x

635: Jeff Robbins and Visibox as an Instrument for Video

Jeff Robbins stops by to talk about his software, Visibox, that was used at Frostapalooza for presenting video at the concert, what it's like building an app with Electron, how it's distributed, how files are used and managed, and how he supports hardware devices inside Electron.




x

639: DX, JSON, XML, HTML, and Databases! Oh My!

How important is the DX of software vs how important is the person showing off the software, Douglas Crockford and JSON, remembering XML, trying to write better HTML for email, new TC39 proposal, workshopping t-shirts, and what do you do if you want a little bit of database on your website?




x

Saving six rivers

Unless an institution is created and armed with powers to manage the Nandi Hills range we will see the gradual demise of a culture centered around water and the death of six rivers.




x

Beware of excess cement

Cement deteriorates with age, and has an inherent weakness of cracking.




x

Could Maini be India's next F1 driver?

India could finally have a driver on the F1 grid after 13 long years.




x

Startups join the party with craft mixers

How non-alcoholic mixers, handcrafted by small players, are edging out sugary soft drinks, sodas in cocktail glasses




x

Flexing it

The Tata Nexon has a wide array of engine and gearbox choices, and the inclusion of a CNG-powered version allows Tata to flaunt its advantage over each of its rivals




x

Brand expertise and heritage bubbling in a moka pot

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




x

To the eMAX 7

The new BYD eMAX 7 aims to reduce pollution and keep fuel bills in check without compromising on space and practicality




x

Toxic air chokes urban India 

Residents grapple with respiratory, cardiac, and other ailments as the air thickens




x

GalaxEye: A multi-sensor peek at earth from outer space

Startup sets out to fill a crucial gap in satellite imagery for real-world applications




x

Several Delhi govt. schemes to tackle toxic air yet to take off

AAP govt. yet to implement at least 5 programmes it announced over the past two years to curb air pollution; these include using drones to map bad air sources and making PUC mandatory to buy fuel; our plans have been stopped by Centre: AAP




x

Delhi enveloped in toxic haze, AQI in severe zone in some areas

Data from the CPCB's Sameer app, which provides hourly AQI updates, showed that out of the 38 monitoring stations, 13 were in the severe category with readings above 400




x

Chhath Puja: Devotees take dip in Yamuna even as toxic foam floats over river