作者:Vijaykumar Deore、Nilambari Yewalkar、Dimple Bhatia、Nikesh Desai、Ravindra D. Gupte、Shruta S. Dadarkar、Mahesh G. Jadhav、Aditi A. Tannu、Pooja Bhatt、Kumar V.S. Nemmani、Ram A. Vishwakarma、Somesh Sharma、Abhijit Roychowdhury、Nilesh M. Dagia、Mandar R. Bhonde、Sanjay Kumar
DOI:10.1016/j.bmcl.2009.04.055
日期:2009.6
A series of novel cyanopyridyl based molecules (1-14) were designed, synthesized and probed for inhibition of mammalian target of rapamycin (mTOR) activity. Compound 14 was found to be a potent inhibitor of mTOR activity as assessed by enzyme-linked immunoassays and Western blot analysis. Most importantly, systemic application (intraperitoneal; ip) of compound 14 significantly suppressed macroscopic and histological abnormalities associated with chemically-induced murine colitis. (C) 2009 Elsevier Ltd. All rights reserved.