Development of LM98, a Small‐Molecule TEAD Inhibitor Derived from Flufenamic Acid-Reference-Cited by-同舟云学术

Development of LM98, a Small‐Molecule TEAD Inhibitor Derived from Flufenamic Acid

Published:2021-07-28 Issue:19 Volume:16 Page:2982-3002
ISSN:1860-7179
Container-title:ChemMedChem
language:en
Short-container-title:ChemMedChem

Author:

Mélin Léa¹,Abdullayev Shuay¹,Fnaiche Ahmed¹,Vu Victoria²,González Suárez Narjara¹,Zeng Hong²,Szewczyk Magdalena M.²,Li Fengling²,Senisterra Guillermo²,Allali‐Hassani Abdellah²,Chau Irene²,Dong Aiping²,Woo Simon³,Annabi Borhane¹,Halabelian Levon²,LaPlante Steven R.³,Vedadi Masoud²⁴,Barsyte‐Lovejoy Dalia²⁴,Santhakumar Vijayaratnam²,Gagnon Alexandre¹^ORCID

Affiliation:

1. Département de chimie Université du Québec à Montréal C.P. 8888, Succ. Centre-Ville Montréal QC H3C 3P8 Canada

2. Structural Genomics Consortium University of Toronto 101 College St. MaRS South Tower Toronto ON M5G 1 L7 Canada

3. INRS-Centre Armand Frappier Santé Biotechnologie Université du Québec 531 Boulevard des Prairies Laval QC H7V 1B7 Canada

4. Department of Pharmacology and Toxicology University of Toronto Toronto ON M5S 1 A8 Canada

Funder

Shenzhen Gas Corporation

Publisher

Wiley

Subject

Organic Chemistry,General Pharmacology, Toxicology and Pharmaceutics,Molecular Medicine,Drug Discovery,Biochemistry,Pharmacology

Link

https://onlinelibrary.wiley.com/doi/pdf/10.1002/cmdc.202100432

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1. Development of HC-258, a Covalent Acrylamide TEAD Inhibitor That Reduces Gene Expression and Cell Migration;ACS Medicinal Chemistry Letters;2023-11-30

2. Development of LM-41 and AF-2112, two flufenamic acid-derived TEAD inhibitors obtained through the replacement of the trifluoromethyl group by aryl rings;Bioorganic & Medicinal Chemistry Letters;2023-10

3. Leveraging Advanced In Silico Techniques in Early Drug Discovery: A Study of Potent Small-Molecule YAP-TEAD PPI Disruptors;Journal of Chemical Information and Modeling;2023-04-03

4. Chloroacetamide fragment library screening identifies new scaffolds for covalent inhibition of the TEAD·YAP1 interaction;RSC Medicinal Chemistry;2023

5. Small-Molecule Cyanamide Pan-TEAD·YAP1 Covalent Antagonists;Journal of Medicinal Chemistry;2022-12-23