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

[ Vol. 15 , Issue. 6 ]

Author(s):

Arunkumar Thiriveedhi*, Ratnakaram Venkata Nadh, Navuluri Srinivasu and Kishore Kaushal   Pages 576 - 582 ( 7 )

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.

Affiliation:

Division of Chemistry, Department of Science and Humanities, Vignan's Foundation for Science Technology and Research University, Guntur-522213, GITAM University, Bengaluru Campus, Karnataka-561203, Division of Chemistry, Department of Science and Humanities, Vignan's Foundation for Science Technology and Research University, Guntur-522213, API Process Research & Development, Dr. Reddys Laboratories Ltd., Hyderabad

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