Benign synthesis of fused-thiazoles with enone-based natural products and drugs for lead discovery

Rawan Alnufaie, Mohamad Akbar Ali, Ibrahim S. Alkhaibari, Subrata Roy, Victor W. Day, Mohammad A. Alam

Research output: Contribution to journalArticlepeer-review

8 Scopus citations

Abstract

In an effort to synthesize a library of bioactive molecules, we present an efficient synthesis of fused-thiazole derivatives of natural products and approved drugs by using an environmentally usable solvent, acetic acid, and without any external reagent. Cholestenone, ethisterone, progesterone, and nootkatone-derived epoxyketones have been utilized to synthesize 50 novel compounds. The plausible mechanism of the reaction has been determined by theoretical calculation using M06-2X/6-31+G(d,p). These novel molecules have been tested against cancer cell lines and pathogenic bacterial strains. Several ethisterone-based fused-thiazole compounds are found to be potent growth inhibitors of cancer cell lines at submicromolar concentrations.

Original languageBritish English
Pages (from-to)6001-6017
Number of pages17
JournalNew Journal of Chemistry
Volume45
Issue number13
DOIs
StatePublished - 7 Apr 2021

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