Evaluation of new indole and bromoindole derivatives as pp60(c-Src) tyrosine kinase inhibitors.
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.
Kiliç
Zühal
Z
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Ankara, 06100, Tandoğan-Ankara, Turkey.
Işgör
Yasemin G
YG
Olgen
Süreyya
S
D007097:Imines / Q000737:chemistry; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D016392:Proto-Oncogene Proteins pp60(c-src) / Q000037:antagonists & inhibitors* / Q000378:metabolism; D012545:Schiff Bases / Q000737:chemistry
D007097:Imines; D007211:Indoles; D047428:Protein Kinase Inhibitors; D012545:Schiff Bases; D016392:Proto-Oncogene Proteins pp60(c-src)