期刊
NEW JOURNAL OF CHEMISTRY
卷 45, 期 13, 页码 6001-6017出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/d1nj00380a
关键词
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资金
- NIGMS NIH HHS [P20 GM103429] Funding Source: Medline
A library of bioactive molecules was synthesized efficiently using environmentally friendly solvent acetic acid, resulting in the creation of novel fused-thiazole derivatives. Experimental results showed that some of these compounds exhibited potent growth inhibition against cancer cell lines.
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.
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