Introduction of a cyano group at the 2-position of an (R,S)-3-hydroxy-2-(phosphonomethoxy)propyl (HPMP) derivative of thymine elicits selective anti-HBV activity

JOURNAL ARTICLE published 2021 in RSC Medicinal Chemistry

Research funded by China Scholarship Council (201606220077)

Authors: Shuai Tan | Elisabetta Groaz | Mark N. Prichard | Raj Kalkeri | Roger Ptak | Piet Herdewijn

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JOURNAL ARTICLE published 2022 in RSC Medicinal Chemistry

Structure–activity relationship study of PROTACs against hematopoietic prostaglandin D₂ synthase

JOURNAL ARTICLE published 2022 in RSC Medicinal Chemistry

Research funded by Japan Society for the Promotion of Science (21K05320,JP18H05502,JP21K06075) | Japan Agency for Medical Research and Development (22fk0210110j0401,22fk0310506j0701,22mk0101197j0002)

Authors: Yuki Murakami | Hinata Osawa | Takashi Kurohara | Yuta Yanase | Takahito Ito | Hidetomo Yokoo | Norihito Shibata | Mikihiko Naito | Kosuke Aritake | Yosuke Demizu

Design and synthesis of atorvastatin derivatives with enhanced water solubility, hepatoselectivity and stability

JOURNAL ARTICLE published 2023 in RSC Medicinal Chemistry

Research funded by Russian Science Foundation (20-63-46029,20-73-00219)

Authors: Svetlana Yu. Maklakova | Anton V. Lopukhov | Alexandr D. Khudyakov | Sergey V. Kovalev | Maria P. Mazhuga | Olga E. Chepikova | Andrey A. Zamyatnin | Alexander G. Majouga | Natalia L. Klyachko | Elena K. Beloglazkina

Design, synthesis and immunological evaluation of monophosphoryl lipid A derivatives as adjuvants for a RBD-hFc based SARS-CoV-2 vaccine

JOURNAL ARTICLE published 2023 in RSC Medicinal Chemistry

Research funded by Guangdong Science and Technology Department (2022B1111020005) | Department of Education of Guangdong Province (2020KQNCX016)

Authors: Shiwei Su | Liqing Chen | Menglan Yang | Dan Liang | Bixia Ke | Zhongqiu Liu | Changwen Ke | Guochao Liao | Liang Liu | Xiang Luo

Drugging the undruggable: a computational chemist's view of KRAS^G12C

JOURNAL ARTICLE published 2021 in RSC Medicinal Chemistry

Authors: Michael S. Bodnarchuk | Doyle J. Cassar | Jason G. Kettle | Graeme Robb | Richard A. Ward

Design, synthesis and anti-mycobacterial evaluation of imidazo[1,2-a]pyridine analogues

JOURNAL ARTICLE published 2022 in RSC Medicinal Chemistry

Research funded by Council of Scientific and Industrial Research, India (F.No. 02(392)/21/EMR II) | Birla Institute of Technology and Science, Pilani (201920-NFST-TEL- 01497)

Authors: Yogesh Mahadu Khetmalis | Surendar Chitti | Anjani Umarani Wunnava | Banoth Karan Kumar | Muthyala Murali Krishna Kumar | Sankaranarayanan Murugesan | Kondapalli Venkata Gowri Chandra Sekhar

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JOURNAL ARTICLE published 2022 in RSC Medicinal Chemistry

Development of 2-deoxystreptamine–nucleobase conjugates for the inhibition of oncogenic miRNA production

JOURNAL ARTICLE published 2022 in RSC Medicinal Chemistry

Research funded by Agence Nationale de la Recherche (ANR-11-JS07-011-1) | Ministry of Science and Technology (911)

Authors: Thi Phuong Anh Tran | Sylvain Poulet | Mélanie Pernak | Anita Rayar | Stéphane Azoulay | Audrey Di Giorgio | Maria Duca

4-Aminopyrazolopyrimidine scaffold and its deformation in the design of tyrosine and serine/threonine kinase inhibitors in medicinal chemistry

JOURNAL ARTICLE published 2022 in RSC Medicinal Chemistry

Authors: Xiaolu Chen | Yajiao Huang | Wanghan Xu | Yuepiao Cai | Yuanrong Yang

The right tools for the job: the central role for next generation chemical probes and chemistry-based target deconvolution methods in phenotypic drug discovery

JOURNAL ARTICLE published 2021 in RSC Medicinal Chemistry

Research funded by Research England (ref.131911)

Authors: Manuela Jörg | Katrina S. Madden

Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype

JOURNAL ARTICLE published 2021 in RSC Medicinal Chemistry

Research funded by Carnegie Trust for the Universities of Scotland (Ref-70260) | Biotechnology and Biological Sciences Research Council (BB/N007638/1)

Authors: Daniel P. Brooke | Leah M. C. McGee | Federica Giordani | Jasmine M. Cross | Abedawn I. Khalaf | Craig Irving | Kirsten Gillingwater | Craig D. Shaw | Katharine C. Carter | Michael P. Barrett | Colin J. Suckling | Fraser J. Scott

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JOURNAL ARTICLE published 2020 in RSC Medicinal Chemistry

Oxazolidinones as versatile scaffolds in medicinal chemistry

JOURNAL ARTICLE published 2023 in RSC Medicinal Chemistry

Research funded by H2020 Marie Skłodowska-Curie Actions (101027065)

Authors: Guilherme Felipe Santos Fernandes | Cauê Benito Scarim | Seong-Heun Kim | Jingyue Wu | Daniele Castagnolo

A new class of 7-deazaguanine agents targeting autoimmune diseases: dramatic reduction of synovial fibroblast IL-6 production from human rheumatoid arthritis patients and improved performance against murine experimental autoimmune encephalomyelitis

JOURNAL ARTICLE published 2024 in RSC Medicinal Chemistry

Research funded by Science Foundation Ireland (17/TIDA/502) | Enterprise Ireland (CF/2015//0029)

Authors: Michelle Cotter | Shauna M. Quinn | Ursula Fearon | Sharon Ansboro | Tatsiana Rakovic | John M. Southern | Vincent P. Kelly | Stephen J. Connon

De novo molecular drug design benchmarking

JOURNAL ARTICLE published 2021 in RSC Medicinal Chemistry

Research funded by Natural Sciences and Engineering Research Council of Canada (510963,RGPIN-2017-05813)

Authors: Lauren L. Grant | Clarissa S. Sit

Potential of covalently linked tamoxifen hybrids for cancer treatment: recent update

JOURNAL ARTICLE published 2024 in RSC Medicinal Chemistry

Authors: Irshad Ahmad | Donna J. Nelson | Maheen Imtiaz Hussain | Noora Ali Nasar

N-Aryl mercaptoacetamides as potential multi-target inhibitors of metallo-β-lactamases (MBLs) and the virulence factor LasB from Pseudomonas aeruginosa

JOURNAL ARTICLE published 2021 in RSC Medicinal Chemistry

Research funded by Deutsche Forschungsgemeinschaft (PR1405/7-1)

Authors: Samir Yahiaoui | Katrin Voos | Jörg Haupenthal | Thomas A. Wichelhaus | Denia Frank | Lilia Weizel | Marco Rotter | Steffen Brunst | Jan S. Kramer | Ewgenij Proschak | Christian Ducho | Anna K. H. Hirsch

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JOURNAL ARTICLE published 2023 in RSC Medicinal Chemistry

Identification and analysis of small molecule inhibitors of FosB from Staphylococcus aureus

JOURNAL ARTICLE published 2023 in RSC Medicinal Chemistry

Research funded by National Institute of General Medical Sciences (1R15GM148956,S10OD028690) | Cystic Fibrosis Foundation (THOMPS2010)

Authors: Skye Travis | Keith D. Green | Nishad Thamban Chandrika | Allan H. Pang | Patrick A. Frantom | Oleg V. Tsodikov | Sylvie Garneau-Tsodikova | Matthew K. Thompson