Benign synthesis of fused-thiazoles with enone-based natural products and drugs for lead discovery. (18th March 2021)

• Record Type: Journal Article
• Authors: Alnufaie, Rawan; Ali, Mohamad Akbar; Alkhaibari, Ibrahim S.; Roy, Subrata; Day, Victor W.; Alam, Mohammad A.
• Is Part Of: New journal of chemistry. Volume 45:Number 13(2021)
• Page Start: 6001
• Page End: 6017
• Publication Date: 2021-03-18
• Subjects: Chemistry -- Periodicals; Chimie -- Périodiques; 540
• DOI: 10.1039/d1nj00380a
• Languages: English
• ISSNs: 1144-0546

Abstract

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. 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.