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

By pubs.rsc.org
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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Discovery of N-substituted-2-oxoindolin benzoylhydrazines as c-MET/SMO modulators in EGFRi-resistant non-small cell lung cancer

By pubs.rsc.org
Published On ::

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.
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Technical, preclinical, and clinical developments of Fc-glycan-specific antibody–drug conjugates

By pubs.rsc.org
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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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Property-based optimisation of PROTACs

By pubs.rsc.org
Published On ::

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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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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A practical guide for the assay-dependent characterisation of irreversible inhibitors

By pubs.rsc.org
Published On ::

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00707G, Review Article
Lavleen K. Mader, Jessica E. Borean, Jeffrey W. Keillor
Kinetic evaluations for assay dependent characterization of irreversible inhibitors.
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SIGMAP: an explainable artificial intelligence tool for SIGMA-1 receptor affinity Prediction

By pubs.rsc.org
Published On ::

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

By pubs.rsc.org
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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Adjuvant strategies to tackle mcr-mediated polymyxin resistance

By pubs.rsc.org
Published On ::

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.
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U.S. Presidential polls: Thulasendrapuram residents pray for Kamala Harris ‘victory

By www.thehindu.com
Published On :: Tue, 05 Nov 2024 12:48:36 +0530


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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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Changes in train services notified due to demolition of old bridge near Tiruchi junction

By www.thehindu.com
Published On :: Tue, 05 Nov 2024 17:30:53 +0530


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Will decide on sharing stage with actor Vijay in consultation with VCK leaders: Thirumavalavan

By www.thehindu.com
Published On :: Tue, 05 Nov 2024 17:44:09 +0530

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


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Frequent traffic snarls pose hardship to motorists in Tiruchi

By www.thehindu.com
Published On :: Tue, 05 Nov 2024 17:45:36 +0530

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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Doctor assaulted inside Tiruchi ESI Hospital

By www.thehindu.com
Published On :: Tue, 05 Nov 2024 18:29:04 +0530


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

By www.thehindu.com
Published On :: Tue, 05 Nov 2024 19:37:18 +0530


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Data crucial for building climate resilience, says ISRO scientist

By www.thehindu.com
Published On :: Tue, 05 Nov 2024 19:40:51 +0530


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Heavy weed growth at Kasi Viswanathar Temple tank prevents replenishing of underground water table, say Tiruchi residents

By www.thehindu.com
Published On :: Tue, 05 Nov 2024 21:04:51 +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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Tiruchi Today (November 7, 2024)

By www.thehindu.com
Published On :: Wed, 06 Nov 2024 18:16:44 +0530


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Duo arrested for possession of banned tobacco products worth ₹3 lakh in Tiruchi

By www.thehindu.com
Published On :: Wed, 06 Nov 2024 18:23:30 +0530


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Ensure time-bound implementation of development schemes, says Thirumavalavan

By www.thehindu.com
Published On :: Wed, 06 Nov 2024 18:29:00 +0530


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Agro-tourism push needs industry-specific policies, say farmers

By www.thehindu.com
Published On :: Wed, 06 Nov 2024 18:37:41 +0530


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Paddy crop loss compensation pegged at ₹36,500

By www.thehindu.com
Published On :: Wed, 06 Nov 2024 18:53:01 +0530


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TNSTC Kumbakonam Division mops up ₹17.13 crore in four days

By www.thehindu.com
Published On :: Wed, 06 Nov 2024 18:59:26 +0530


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Three arrested for assaulting doctor in ESI hospital

By www.thehindu.com
Published On :: Wed, 06 Nov 2024 19:23:47 +0530


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

By www.thehindu.com
Published On :: Wed, 06 Nov 2024 19:30:58 +0530


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Plea to include ‘panneer karumbu’ in Pongal gift hamper

By www.thehindu.com
Published On :: Wed, 06 Nov 2024 19:41:17 +0530


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Case filed against actor Kasthuri over remarks on Telugu community

By www.thehindu.com
Published On :: Wed, 06 Nov 2024 19:46:03 +0530


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Urban Primary Health Centre stuck in cramped, temporary facility

By www.thehindu.com
Published On :: Wed, 06 Nov 2024 20:31:50 +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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Property owners block the entrance to Balasubramanya temple in Karur

By www.thehindu.com
Published On :: Thu, 07 Nov 2024 17:35:45 +0530


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

By www.thehindu.com
Published On :: Thu, 07 Nov 2024 17:45:02 +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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Udhayanidhi lays foundation stone for infrastructure development projects in Thanjavur district

By www.thehindu.com
Published On :: Thu, 07 Nov 2024 18:48:04 +0530

Buildings at the Government Arts and Science College, Thirukkattupalli, construction of compound wall and an indoor stadium at the Government Rajah Serfoji College, Thanjavur, are among the projects


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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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Bids invited for setting up International Dugong Conservation Centre at Manora

By www.thehindu.com
Published On :: Thu, 07 Nov 2024 19:03:19 +0530

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

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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HR&CE plans to bring properties around the Vennaimalai Temple under tenants list

By www.thehindu.com
Published On :: Thu, 07 Nov 2024 19:36:32 +0530

The HR&CE department has cleared 34 properties around the Balasubramanyaswamy Temple at Vennaimalai in Karur district as per the High Court orders


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Railways using treated water from its STP for maintaining green spaces

By www.thehindu.com
Published On :: Thu, 07 Nov 2024 20:46:00 +0530

The treated water is stored in an overhead tank and used in gardens at the two railway rest houses meant for officers at Kallukuzhi near Tiruchi Railway Junction


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Tiruchi district SHGs compete to prepare healthy millet-based recipes at food festival

By www.thehindu.com
Published On :: Fri, 08 Nov 2024 07:51:25 +0530

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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Power shutdown in parts of Tiruchi on November 9

By www.thehindu.com
Published On :: Fri, 08 Nov 2024 17:45:18 +0530


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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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Peravurani farmers’ market starts functioning

By www.thehindu.com
Published On :: Fri, 08 Nov 2024 18:46:38 +0530


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High-level committee formed to facilitate clearances for companies that signed MoU, says Minister

By www.thehindu.com
Published On :: Fri, 08 Nov 2024 18:56:40 +0530

Constant monitoring was being done now from the time of signing of MoUs to providing employment in new industrial units, says Industries Minister T.R.B. Rajaa


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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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NTK chief Seeman booked for alleged ‘derogatory remarks’ against Karunanidhi

By www.thehindu.com
Published On :: Fri, 08 Nov 2024 19:03:53 +0530


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