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A chemodosimetric chemosensor for the ratiometric detection of nerve agent-mimic DCP in solution and vapor phases

Anal. Methods, 2024, Advance Article
DOI: 10.1039/D4AY00451E, Paper
Shilpita Banerjee, Pintu Ghosh, Anirban Karak, Dipanjan Banik, Ajit Kumar Mahapatra
The probe MNFZ undergoes a hydrolysis reaction in the presence of DCP to exhibit a naked eye color change from blue to cyan. It was successfully applied to sense DCP in the vapor phase.
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Missing the obvious




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​Weather gods: On ‘Mission Mausam’

Attempts at controlling the weather are still in the realm of uncertainty




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​Last mile woes: On inflation data and the challenges

Inflation should not be allowed to undermine the economic momentum 




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A fair share: On the concerns of high performing States

The Sixteenth Finance Commission must address the concerns of high-performing States




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Party on the move: On the Aam Aadmi Party, its leader

AAP’s Arvind Kejriwal continues to surprise, also outlining his political ambitions




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 Milestones and U-turns: On the government in its third term

The optics of the 100-day mark cannot conceal changed dynamics for the BJP




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​Kashmir conflict: On the J&K elections

The political divide between national parties and regional parties is clear 




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​Embattled CM: On Karnataka Chief Minister Siddaramaiah

Anti-graft moves should not be overshadowed by political motive




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​Delay and bail: On former Tamil Nadu Minister V. Senthilbalaji’s case

Senthilbalaji’s release on bail was overdue, but he should not be made a Minister




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​Demand flux: On growth dynamics

Growth dynamics may falter with waning urban consumption




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​Steady but slow: On the VIPER mission, lessons for India

India’s space programme needs more resources to realise its full potential




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​Changes at the top: On the Tamil Nadu cabinet reshuffle 

Ministers must infuse confidence in the people they serve 




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Caste in jail: On discrimination in prisons

Time for State governments to end systemic discrimination in prisons




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​Respect the mandate: On the 2024 Jammu and Kashmir elections

With elections done and dusted, J&K now must return to statehood




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Biology transformed: On the Nobel Prize in chemistry

Nobel for determining protein structure recognises a big advance




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Fate of nations: On the 2024 Economics Nobel

The 2024 Nobel recognises the need for ‘inclusive’ institutions




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​Governor vs Government: On the hostilities in Tamil Nadu

Mr. Ravi must be withdrawn for needlessly wading into controversies




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Growth prescription: On the latest World Economic Outlook 

The IMF’s ‘mediocre’ medium-term outlook merits policy attention




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​Building blocks: On the 16th BRICS Summit in Kazan  

The BRICS Summit showed that Russia was not without friends




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​Beautifully vague: On the Tamilaga Vettri Kazhagam’s inaugural conference  

Actor Vijay seems to be targeting both the BJP and the DMK 




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Sun signs: On extreme heat and Tamil Nadu’s policy decision

States should prepare to assist the vulnerable during extreme heat events




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The Raj & DK Line-Up You Cannot Miss

Sukanya Verma looks at their eclectic career of over two decades as their latest offering Citadel: Honey Bunny, the Indian leg of the Russo Brothers globetrotting spy universe series, drops on Amazon Prime Video on November 7.




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Why Abhishek Missed Aishwarya's Birthday

When Aishwarya celebrated her birthday in Dubai on November 1, the speculation regarding the Abhishek-Aishwarya marital rift ran even higher.




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Design, synthesis, inhibitory activity, and molecular simulations study for D-glucose-conjugated thioureas containing pyrimidine ring as multitarget inhibitors against α-amylase, α-glucosidase, DDP-4, and PTP1B in Type 2 diabetes mellitus

RSC Med. Chem., 2024, 15,3395-3417
DOI: 10.1039/D4MD00334A, Research Article
Vu Ngoc Toan, Do Son Hai, Hoang Thi Kim Van, Nguyen Minh Tri, Duong Ngoc Toan, Nguyen Thi Thanh Mai, Nguyen Dinh Thanh
D-Glucose-conjugated thioureas from 2-aminopyrimidines had inhibitory activity against α-amylase, α-glucosidase, DPP-4, PTP1B. The cytotoxicity, inhibitory kinetics, and molecular simulations of the most potent inhibitors 8k, 8j, 8f, and 8h were studied.
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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.
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Integrating amino acids into Bcr-Abl inhibitors: design, synthesis, biological evaluation, and in silico studies

RSC Med. Chem., 2024, 15,3507-3528
DOI: 10.1039/D4MD00417E, Research Article
Yuying Liu, Zeyu Yang, Jie Zhang, Na Guo, Nanxin Liu, Qingqing Zhang, Xintao Dang, Yanchen Li, Jie Zhang, Xiaoyan Pan
In continuation of our previous research, a series of novel Bcr-AblT315I inhibitors with tert-leucine or serine as a flexible linker were developed and biological evaluation was performed in vitro.
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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.
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Semisynthetic phytochemicals in cancer treatment: a medicinal chemistry perspective

RSC Med. Chem., 2024, 15,3345-3370
DOI: 10.1039/D4MD00317A, Review Article
Meghna Arora, Ankit Kumar Singh, Adarsh Kumar, Harshwardhan Singh, Prateek Pathak, Maria Grishina, Jagat Pal Yadav, Amita Verma, Pradeep Kumar
Semisynthetic phytochemicals in cancer treatment.
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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.
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Pyridazinone-based derivatives as anticancer agents endowed with anti-microbial activity: molecular design, synthesis, and biological investigation

RSC Med. Chem., 2024, 15,3529-3557
DOI: 10.1039/D4MD00481G, Research Article
Mohamed K. S. El-Nagar, Mai I. Shahin, Mohammed F. El-Behairy, Ehab S. Taher, Mohamed F. El-Badawy, Marwa Sharaky, Dalal A. Abou El Ella, Khaled A. M. Abouzid, Mai Adel
Discovery of novel pyridazinone derivatives with dual antimicrobial and anticancer activities.
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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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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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Introduction to the themed collection on ‘AI in Medicinal Chemistry’

RSC Med. Chem., 2024, 15,3284-3285
DOI: 10.1039/D4MD90035A, Editorial
Jian Zhang, Ola Engkvist, Gerhard Hessler
Jian Zhang, Ola Engkvist and Gerhard Hessler introduce the RSC Medicinal Chemistry themed collection on ‘AI in Medicinal Chemistry’.
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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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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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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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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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Continuous flow synthesis of N,N-dimethyltryptamine (DMT) analogues with therapeutic potential

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00562G, Research Article
Open Access
Andreas Simoens, Andreas Dejaegere, Marthe Vandevelde, Christian V. Stevens
Flow chemistry allows for the rapid and clean synthesis of therapeutically relevant tryptamines in good yields, including the large scale drug rizatriptan.
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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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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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Miniaturized click chemistry and direct screening facilitate the discovery of triazole piperazine SARS-CoV-2 Mpro inhibitors with improved metabolic stability

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

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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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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50 new primary health centres to be opened in State soon: Minister