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Discovery of MDV6058 (PF-06952229), a selective and potent TGFßR1 inhibitor: Design, synthesis and optimization.
Pujala, Brahmam; Ramachandran, Sreekanth A; Sonawane, Mukesh; Kamble, Maruti M; Panpatil, Dayanand; Adhikari, Swati; Soni, Sanjeev; Subbareddy, Venkata; Shinde, Bharat U; Nayak, Anjan K; Bansal, Chandni; Gupta, Ashu; Mukherjee, Kakoli; Agarwal, Anil K; Guerrero, Javier; Herrera, Francisco J; Bernales, Sebastian; Guha, Mausumee; Chakravarty, Sarvajit; Pham, Son M; Rai, Roopa.
Bioorg Med Chem Lett ; 75: 128979, 2022 11 01.
Article in English | MEDLINE | ID: mdl-36089110

ABSTRACT

Compound 1 is a potent TGF-ß receptor type-1 (TGFßR1 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.


Subject(s)
Receptors, Transforming Growth Factor beta , Animals , Mice , Solvents
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