Evaluation of New Indole and Bromoindole Derivatives as pp60c‐Src Tyrosine Kinase Inhibitors |
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Authors: | Zühal Kılıç Yasemin G. İşgör Süreyya Ölgen |
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Affiliation: | 1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Ankara, 06100, Tando?an‐Ankara, Turkey;2. Nanomedicine Research Center, Gazi University, G?lba??, Ankara 06830, Turkey |
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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 pp60c‐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. |
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Keywords: | indole and bromoindole derivatives inhibition of pp60c‐Src schiff bases synthesis tyrosine kinase |
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