Evaluation of New Indole and Bromoindole Derivatives as pp60(c-Src) Tyrosine Kinase Inhibitors

Kilic Z., Isgor Y. G., Olgen S.

CHEMICAL BIOLOGY & DRUG DESIGN, vol.74, no.4, pp.397-404, 2009 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 74 Issue: 4
  • Publication Date: 2009
  • Doi Number: 10.1111/j.1747-0285.2009.00876.x
  • Journal Name: CHEMICAL BIOLOGY & DRUG DESIGN
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Index Chemicus (IC)
  • Page Numbers: pp.397-404
  • Keywords: indole and bromoindole derivatives, inhibition of pp60(c-Src), schiff bases, synthesis, tyrosine kinase, SRC FAMILY KINASES, DESIGN, RECEPTOR, CANCER, AMINE, DRUGS
  • Ankara University Affiliated: Yes

Abstract

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 NaBH4 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.