Design, Synthesis and Cytotoxic Evaluation of Novel Imatinib Amide Derivatives that Target Abl Kinase

ISSN: 1875-628X (Online)
ISSN: 1570-1808 (Print)


Volume 14, 12 Issues, 2017


Download PDF Flyer




Letters in Drug Design & Discovery

This journal supports open access

Aims & ScopeAbstracted/Indexed in


Submit Abstracts Online Submit Manuscripts Online

Editor-in-Chief:
G. Perry
University of Texas
San Antonio, TX
USA


View Full Editorial Board

Subscribe Purchase Articles Order Reprints

Current: 0.974
5 - Year: 2.25

Design, Synthesis and Cytotoxic Evaluation of Novel Imatinib Amide Derivatives that Target Abl Kinase



Letters in Drug Design & Discovery, 12(1): 20-28.

Author(s): Ri-Sheng Yao, Qiu-Xiang Guan, Xiao-Qin Lu and Ban-Feng Ruan.

Affiliation: School of Medical Engineering, Hefei University of Technology, Hefei, 230009, PR China.

Abstract

Novel imatinib amide derivatives (a1-28, b1-9) were synthesized and evaluated for their biological activities. All compounds were characterized by 1H NMR, MS and elemental analysis. Among all the derivatives, compounds a4, a10, a21, b1 and b2 displayed the most significant ability of inhibiting K562 cell proliferation with the IC50 values of 0.67, 0.66, 0.65, 0.59 and 0.62 µM, respectively, indicating that these compounds were potent inhibitors of Bcr-Abl in leukemic K562 cells, comparable to the reference compound imatinib. Molecular docking study was performed to position compounds a21 and b1 into the active site of Abl to determine the probable binding modes.




Keywords:

Amide derivatives, Bcr-Abl inhibitors, chronic myeloid leukemia, imatinib, inhibiting activity, molecular docking, SAR.



Download Free Order Reprints Order Eprints Rights and Permissions




Article Details

Volume: 12
Issue Number: 1
First Page: 20
Last Page: 28
Page Count: 9
DOI: 10.2174/1570180811666140812231519
Advertisement
Global Biotechnology Congress 2017Drug Discovery and Therapy World Congress 2017

Related Journals




Related eBooks



Webmaster Contact: urooj@benthamscience.org Copyright © 2017 Bentham Science