d-secoestrone-triazole

d-secoestrone-triazole is a semisynthetic small molecule derivative of estrone, modified to open the D-ring and introduce a triazole moiety. It exhibits potent antiproliferative activity, particularly against certain cervical cancer cell lines (notably HPV 18-positive HeLa and HPV-negative C-33A), with limited effects on HPV 16-positive SiHa cells or normal fibroblasts. Mechanistically, it induces apoptosis and causes cell cycle arrest at the G2/M phase by stabilizing microtubules through direct action on tubulin polymerization—distinctly enhancing microtubule formation rather than destabilizing it. This action is consistent with microtubule-stabilizing antitumor agents, though d-secoestrone-triazole does not bind to nuclear estrogen receptors and is not significantly estrogenic. Besides inhibiting proliferation, it also inhibits cell migration and invasion in cancer models. It is considered a promising lead for novel anticancer agents targeting the cytoskeleton in tumor cells.[1][2][3]

Other names

D-SET