Synthesis and therapeutic evaluation of pyridyl based novel mTOR inhibitors
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- 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
- 关键词：Cyanopyridyl ; mTOR inhibitor ; Inflammation ; Ulcerative colitis ; Colon cancer
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2009
- 出版时间：1 June 2009
- 年：2009
- 卷：19
- 期：11
- 页码：2949-2952
- 全文大小：974 K
文摘
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.