Search

Your search keyword '"Chandni Bansal"' showing total 1 results
Start Over Author "Chandni Bansal" Journal bioorganicmedicinal chemistry letters
1 results on '"Chandni Bansal"'

1. Discovery of MDV6058 (PF-06952229), a selective and potent TGFβR1 inhibitor: Design, synthesis and optimization

Author

Brahmam Pujala, Sreekanth A. Ramachandran, Mukesh Sonawane, Maruti M. Kamble, Dayanand Panpatil, Swati Adhikari, Sanjeev Soni, Venkata Subbareddy, Bharat U. Shinde, Anjan K. Nayak, Chandni Bansal, Ashu Gupta, Kakoli Mukherjee, Anil K. Agarwal, Javier Guerrero, Francisco J. Herrera, Sebastian Bernales, Mausumee Guha, Sarvajit Chakravarty, Son M. Pham, and Roopa Rai

Subjects
Mice, Organic Chemistry, Clinical Biochemistry, Drug Discovery, Solvents, Pharmaceutical Science, Molecular Medicine, Animals, Molecular Biology, Biochemistry, Receptors, Transforming Growth Factor beta
Abstract

Compound 1 is a potent TGF-β receptor type-1 (TGFβR1 or ALK5) inhibitor but is metabolically unstable. A solvent-exposed part of this molecule was used to analogue and modulate cell activity, liver microsome stability and mouse pharmacokinetics. The evolution of SAR that led to the selection of 2 (MDV6058 / PF-06952229) as a preclinical lead compound is described.

Published
2022

Catalog

Books, media, physical & digital resources
See catalog results