New benzothieno[2,3-<i>c</i>]pyridines as non-steroidal CYP17 inhibitors: design, synthesis, anticancer screening, apoptosis induction, and <i>in silico</i> ADME profile studies
نویسندگان
چکیده
A series of [1]benzothieno[2,3-c]pyridines was synthesised. Most compounds were chosen by NCI-USA to evaluate their anticancer activity. Compounds 5a–c showed prominent growth inhibition against most cell lines. 5c selected at five dose concentration levels. It exhibited potent broad-spectrum activity with a GI50 4 nM–37 µM. Cytotoxicity further evaluated prostate, renal, and breast cancer double quadruple the staurosporine abiraterone, respectively, PC-3 line IC50 2.08 The possible mechanism anti-prostate explored via measuring CYP17 enzyme in mice prostate models compared abiraterone. results revealed that suppressed 15.80 nM. Moreover, it found be equipotent abiraterone testosterone production. Cell cycle analysis apoptosis performed. Additionally, ADME profile compound demonstrated both good oral bioavailability metabolic stability.
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ژورنال
عنوان ژورنال: Journal of Enzyme Inhibition and Medicinal Chemistry
سال: 2021
ISSN: ['1475-6374', '1475-6366']
DOI: https://doi.org/10.1080/14756366.2021.1958212