Abstract
Background: Now-a-days, the model of “hybrid drugs” has acquired recognition in medicine due to their significant role in the treatment of different health problems.
Methods: We have synthesized new series of isoxazole-chalcone conjugates (14a-m) by the Claisen-Schmidt condensation of suitable substituted acetophenones with isoxazole aldehydes (12a-d). In vitro cytotoxic activity of the synthesized compounds was studied against four different selected human cancer cell lines by using sulforhodamine B (SRB) method.
Results: The adopted scheme resulted in good yields of new series of isoxazole-chalcone conjugates (14a-m). Potent cytotoxic activity was observed for compounds -14a, 14b, 14e, 14i, 14j and 14k against prostate DU-145 cancer cell line.
Conclusion: The observed potent cytotoxic activities were due to the presence of 3,4,5- trimethoxyphenyl group.
Keywords: l-(3, 4, 5-trimethoxyphenyl)ethanone, isoxazole-chalcone, hybrid molecules, antiproliferative activity, claisenschmidt condensation, cytotoxic activities.
Graphical Abstract
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