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Synthesis and therapeutic evaluation of pyridyl based novel mTOR inhibitors

  作者 Deore, V; Yewalkar, N; Bhatia, D; Desai, N; Gupte, RD; Dadarkar, SS; Jadhav, MG; Tannu, AA; Bhatt, P; Nemmani, KVS; Vishwakarma, RA; Sharma, S; Roychowdhury, A; Dagia, NM; Bhonde, MR; Kumar, S  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2009年19-11;  页码  2949-2952  
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[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.

 
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