Premium
Evaluation of New Indole and Bromoindole Derivatives as pp60 c‐Src Tyrosine Kinase Inhibitors
Author(s) -
Kılıç Zühal,
İşgör Yasemin G.,
Ölgen Süreyya
Publication year - 2009
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2009.00876.x
Subject(s) - chemistry , amine gas treating , imine , indole test , tyrosine , biological activity , stereochemistry , tyrosine kinase , combinatorial chemistry , medicinal chemistry , organic chemistry , biochemistry , in vitro , catalysis , receptor
A series of N ‐benzyl‐indole‐3‐imine‐, amine derivatives and their 5‐bromo congeners were synthesized and their biological activity were evaluated against the pp60 c‐Src tyrosine kinase target. To afford the imine derivatives, aldehydes were reacted with substituted benzylamines and the corresponding amine derivatives were obtained by NaBH 4 reduction of these imines. Except insoluble N ‐benzyl‐indole‐3‐imine derivatives, all the derivatives showed some activity against the kinase target. Screening of these compounds for their biological activity revealed that among N ‐benzyl‐indole derivatives, those bearing 5‐bromo substitution have the enhanced potency, where the amine derivatives were more active than imines.