Synthesis and therapeutic evaluation of pyridyl based novel mTOR inhibitors

被引：9

作者：

Deore, Vijaykumar ^{[1
]}

Yewalkar, Nilambari ^{[1
]}

Bhatia, Dimple ^{[2
]}

Desai, Nikesh ^{[2
]}

Gupte, Ravindra D. ^{[2
]}

Dadarkar, Shruta S. ^{[2
]}

Jadhav, Mahesh G. ^{[2
]}

Tannu, Aditi A. ^{[2
]}

Bhatt, Pooja ^{[2
]}

Nemmani, Kumar V. S. ^{[2
]}

Vishwakarma, Ram A. ^{[1
]}

Sharma, Somesh ^{[1
,2
]}

Roychowdhury, Abhijit ^{[1
]}

Dagia, Nilesh M. ^{[2
]}

Bhonde, Mandar R. ^{[2
]}

Kumar, Sanjay ^{[1
]}

机构：

[1] Piramal Life Sci, Dept Med Chem, Bombay 400063, Maharashtra, India

[2] Piramal Life Sci, Dept Pharmacol, Bombay 400063, Maharashtra, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 11期

关键词：

Cyanopyridyl; mTOR inhibitor; Inflammation; Ulcerative colitis; Colon cancer; COLITIS; LIPOPOLYSACCHARIDE; MACROPHAGES; RAPAMYCIN; MICE;

D O I：

10.1016/j.bmcl.2009.04.055

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

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.

引用

页码：2949 / 2952

页数：4

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