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(17beta)-17-(cyanomethyl)-2-methoxyestra-1(10),2,4-trien-3-yl sulfamate

Development stage
Preclinical
Modality
Small Molecules
01

Overview

This compound is a synthetic estrane steroid derivative featuring a cyanomethyl group at the C17 position and a methoxy group at C2 with a 3-sulfamate ester moiety. It has been studied as an experimental anticancer agent due to its potent antiproliferative effects in vitro against human cancer cell lines such as MCF‑7 and MDA-MB‑231. The compound acts via multiple mechanisms including inhibition of steroid sulfatase and carbonic anhydrase II (hCAII), disruption of microtubules leading to antiangiogenic activity and cell cycle arrest in cancer cells. Preclinical studies have demonstrated promising antitumor activity in xenograft models of breast cancer[5]. It is not approved for clinical use but remains under investigation as an experimental small molecule anticancer agent[2][5][6].

Other names
(1S,10S,11S,14R,15R)-14-(cyanomethyl)-4-methoxy-15-methyltetracyclo[8.7.0.02,?.011,1?]heptadeca-2,4,6-trien-5-yl sulfamate2-methoxy-17beta-cyanomethylestra-1,3,5(10)-trien-3-O-sulfamate[(8S,9S,13R,14S,17R)-17-(cyanomethyl)-2-methoxy-13-methyl-decahydrocyclopenta[a]phenanthren]-3yl sulfamate
02

Targets

CA2 (Carbonic Anhydrase 2)STS (Steroid sulfatase)TUBB (Tubulin (alpha and beta subunits))

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