title: Synthesis and therapeutic evaluation of pyridyl based novel mTOR inhibitors.
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 histological abnormalities associated with chemically-induced murine colitis.
authors.affiliation: Department of Medicinal Chemistry, Piramal Life Sciences, 1-Nirlon Complex, Goregaon (E), Mumbai, India.
authors.forename: Vijaykumar
authors.initials: V
authors.lastname: Deore
authors.forename: Nilambari
authors.initials: N
authors.lastname: Yewalkar
authors.forename: Dimple
authors.initials: D
authors.lastname: Bhatia
authors.forename: Nikesh
authors.initials: N
authors.lastname: Desai
authors.forename: Ravindra D
authors.initials: RD
authors.lastname: Gupte
authors.forename: Shruta S
authors.initials: SS
authors.lastname: Dadarkar
authors.forename: Mahesh G
authors.initials: MG
authors.lastname: Jadhav
authors.forename: Aditi A
authors.initials: AA
authors.lastname: Tannu
authors.forename: Pooja
authors.initials: P
authors.lastname: Bhatt
authors.forename: Kumar V S
authors.initials: KV
authors.lastname: Nemmani
authors.forename: Ram A
authors.initials: RA
authors.lastname: Vishwakarma
authors.forename: Somesh
authors.initials: S
authors.lastname: Sharma
authors.forename: Abhijit
authors.initials: A
authors.lastname: Roychowdhury
authors.forename: Nilesh M
authors.initials: NM
authors.lastname: Dagia
authors.forename: Mandar R
authors.initials: MR
authors.lastname: Bhonde
authors.forename: Sanjay
authors.initials: S
authors.lastname: Kumar
mesh_terms: D000178:Acrylamides / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000627:therapeutic use; D000818:Animals; D045744:Cell Line, Tumor; D003093:Colitis, Ulcerative / Q000139:chemically induced / Q000188:drug therapy; D004195:Disease Models, Animal; D006801:Humans; D051379:Mice; D009570:Nitriles / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000627:therapeutic use; D011494:Protein Kinases / Q000737:chemistry / Q000378:metabolism*; D011725:Pyridines / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000627:therapeutic use; D058570:TOR Serine-Threonine Kinases
chemical_list: D000178:Acrylamides; D009570:Nitriles; D047428:Protein Kinase Inhibitors; D011725:Pyridines; D011494:Protein Kinases; C546842:MTOR protein, human; C546843:mTOR protein, mouse; D058570:TOR Serine-Threonine Kinases