Synthesis and biological evaluation of 1-benzyl-5-(3-biphenyl-2-yl-propyl)-1H-imidazole as novel farnesyltransferase inhibitor.
Farnesyltransferase inhibitors (FTIs) have emerged as a novel class of anti-cancer agents. Analogs of the potent FTI, 1-benzyl-5-(3-biphenyl-2-yl-propyl)-1H-imidazole, were synthesized and tested in vitro for their inhibitory activities. The most promising compound identified from this series is analog 29 that possesses potent enzymatic and cellular activities.
Lin
Nan-Horng
NH
Cancer Research, R-47B, Global Pharmaceutical Products Division, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-3500, USA. nanhorng.lin@abbott.com
Wang
Le
L
Wang
Xilu
X
Wang
Gary T
GT
Cohen
Jerry
J
Gu
Wen-Zhen
WZ
Zhang
Haiying
H
Rosenberg
Saul H
SH
Sham
Hing L
HL
D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors*; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D001682:Biological Availability; D001713:Biphenyl Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D051231:Farnesyltranstransferase; D007093:Imidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D066298:In Vitro Techniques; D051381:Rats; D013329:Structure-Activity Relationship
C498369:1-benzyl-5-(3-biphenyl-2-ylpropyl)-1H-imidazole; D000970:Antineoplastic Agents; D001713:Biphenyl Compounds; D007093:Imidazoles; D019883:Alkyl and Aryl Transferases; C083291:geranylgeranyltransferase type-I; D051231:Farnesyltranstransferase