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Privileged fragment-based design, synthesis and in vitro antitumor activity of imatinib analogues
2023
Journal:  
Turkish Journal of Chemistry
Author:  
DOI:  
10.55730/1300-0527.3549
Abstract:

Based on the privileged fragment-based drug design strategy, a series of imatinib analogues bearing the moiety of 3-(2-amino- 2-oxoacetyl)-1H-indole were designed and synthesized, and the in vitro antitumor activity of these compounds was detected by MTT method using K562 (human myeloid leukemia) and K562R (imatinib-resistant chronic myeloid leukemia) cell lines. Molecular docking was used to preliminarily explain the possible binding modes. The most potent compound I2 exhibited better antitumor activity than those of imatinib against K562 and K562R cancer cells with IC50 values of 0.8 ?M and 0.7 ?M.

Keywords:

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Turkish Journal of Chemistry

Field :   Fen Bilimleri ve Matematik

Journal Type :   Uluslararası

Metrics
Article : 2.410
Cite : 1.692
2023 Impact : 0.068
Details
Turkish Journal of Chemistry