Rapid microwave assisted synthesis and antiproliferative evaluation of novel steroidal thiazole derivatives

Abstract

Three series of novel steroidal thiazole derivatives were synthesized by microwave assisted one-pot reaction from pregnenolone, testosterone and estrone, respectively. Their structures were characterized by IR, NMR and HRMS, and the antiproliferative activities of all the synthesized compounds against human cervical carcinoma (HeLa), human liver carcinoma(HepG2), human lung carcinoma(A549), nasopharyngeal carcinoma(CNE2) and normal kidney epithelial cells(HEK293T) were screened. Among the compounds, 1-estron-17′-ylidene-2-[4′-(p-bromophenyl)-2′-thiazol] hydrazone(12) displayed distinct antiproliferative activity against all the tested cancer cell lines and was almost inactive to normal kidney epithelial cells.

Keywords

Microwave assisted synthesis / Pregnenolone / Testosterone / Estrone / Steroidal thiazole derivative

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