Novel Hybrid Molecules of Isoxazole Chalcone Derivatives: Synthesis and Study of in vitro Cytotoxic Activities

Author(s): Arunkumar Thiriveedhi*, Ratnakaram Venkata Nadh, Navuluri Srinivasu, Kishore Kaushal

Journal Name: Letters in Drug Design & Discovery

Volume 15 , Issue 6 , 2018

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Graphical 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.

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Article Details

Year: 2018
Page: [576 - 582]
Pages: 7
DOI: 10.2174/1570180814666170914121740
Price: $65

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