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, cilt.74, sa.4, ss.397-404, 2009 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 74 Sayı: 4
  • Basım Tarihi: 2009
  • Doi Numarası: 10.1111/j.1747-0285.2009.00876.x
  • Dergi Adı: CHEMICAL BIOLOGY & DRUG DESIGN
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Index Chemicus (IC)
  • Sayfa Sayıları: ss.397-404
  • Anahtar Kelimeler: indole and bromoindole derivatives, inhibition of pp60(c-Src), schiff bases, synthesis, tyrosine kinase, SRC FAMILY KINASES, DESIGN, RECEPTOR, CANCER, AMINE, DRUGS
  • Ankara Üniversitesi Adresli: Evet

Özet

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.