Thiazole- and Coumarin-Conjugated (β-Lactam Scaffold) Azetidinones Synthesis and Their Substitution Effect in In Silico, and In Vitro Cell Viability Studies

噻唑 活力测定 化学 香豆素 连接器 组合化学 立体化学 生物化学 体外 有机化学 操作系统 计算机科学
作者
Afreen,Shireesha Manturthi,Amar nath Velidandi
出处
期刊:Russian Journal of Bioorganic Chemistry [Pleiades Publishing]
卷期号:48 (6): 1273-1281 被引量:5
标识
DOI:10.1134/s1068162022060036
摘要

In present pandemic situations, we need more and more care on the medication, to treat the ill cells or to control the growth of the cells we need better transfection with active pharmaceutical ingredients. In chemotherapy many drugs are working on the target as well as on adjacent organs, to avoid such conditions, we required active compounds, coumarin, and thiazole-based compounds can function in this way. This research work illustrated better transfection and percentage of cell viability of azetidinones by the insertion of thiazole and (or) coumarin groups. Synthesized the tilted compounds from Thiazole (or) Coumarin-based Schiff base, and chloroacetyl chloride with good yields. Herein, the β-lactam group acts as a linker, to this linker one side heterocyclic ring acts as the anchoring group, and the other side of the aromatic ring acts as the hydrophobic group; in silico studies of this series, results have shown that many compounds are having anti-cancer activity along with other biological activities. The in vitro cell viability studies IC50 values of Azetidinone (III): 1.5608, (IV): 1.5694, (V): 1.5489, and (VI): 1.7452 are better than the reference Lipofectamine 2000 (L2K): 2.0280 against oral cancer cell line (CAL-27), this result supported by the cellular uptake against HEK-293, DNA binding, and β-galactose activity.
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