化学
药代动力学
药理学
铅化合物
微粒体
受体
化学合成
结构-活动关系
转化生长因子
代谢稳定性
立体化学
生物化学
体外
细胞生物学
医学
生物
作者
Brahmam Pujala,Sreekanth A. Ramachandran,Mukesh Digambar 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
标识
DOI：10.1016/j.bmcl.2022.128979
摘要
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.
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