Synthesis and anticancer activity of chromone-based analogs of lavendustin A

European Journal of Medicinal Chemistry
Dong Hyuk NamYong Sup Lee

Abstract

Lavendustin A and hormothamnione were reported to exhibit cytotoxic effects on tumor cell lines. In the present studies, a series of chromone-based lavendustin analogs were synthesized as a simplified hybrid of hormothamnione and lavendustin A by the reductive-amination of formyl-chromone 5 with various amines followed by aminoalkylation. Most compounds synthesized showed significantly improved potencies compared to the standard compound 3 against most of cancer cell lines tested indicating that the removal of styryl group enhanced cancer cell growth inhibitory activities. Compound 4h and 4k showed the most potent inhibitory activities with GI(50) values in the range of 6.01-9.92 microg/ml on A-549 and HCT-15 cells.

Citations

Mar 10, 2015·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Cristovao F LimaCristina Pereira-Wilson
Apr 3, 2014·European Journal of Medicinal Chemistry·Rangappa S KeriR Geetha Balakrishna
Jul 4, 2012·International Journal of Molecular Sciences·Santosh Kumar, Joonseok Koh
Nov 22, 2014·Organic & Biomolecular Chemistry·Mykhaylo S FrasinyukVitaliy M Sviripa
Aug 25, 2020·Pharmaceutical Chemistry Journal·Noor Ul Amin MohsinUsman Saleem
Apr 28, 2021·Bioorganic & Medicinal Chemistry·Emmanuel Ramsey Buabeng, Maged Henary
Feb 22, 2014·Chemical Reviews·Alexandra GasparFernanda Borges
May 11, 2011·Bioorganic & Medicinal Chemistry·Mariya al-RashidaGhulam Abbas

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