Synthesis and therapeutic evaluation of pyridyl based novel mTOR inhibitors

…, RA Vishwakarma, S Sharma, A Roychowdhury…

Index: Deore, Vijaykumar; Yewalkar, Nilambari; Bhatia, Dimple; Desai, Nikesh; Gupte, Ravindra D.; Dadarkar, Shruta S.; Jadhav, Mahesh G.; Tannu, Aditi A.; Bhatt, Pooja; Nemmani, Kumar V.S.; Vishwakarma, Ram A.; Sharma, Somesh; Roychowdhury, Abhijit; Dagia, Nilesh M.; Bhonde, Mandar R.; Kumar, Sanjay Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 11 p. 2949 - 2952

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Citation Number: 10

Abstract

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 ...