MOD_66

MOD_66 is a first-in-class small molecule dual modulator designed to target both human carbonic anhydrases (hCA) and estrogen receptors (ER). Specifically, it acts as a potent inhibitor of the cancer-related hCA isoforms IX and XII and as a modulator of estrogen receptor subtypes ERα and ERβ. Developed using a multi-target repurposing strategy based on a hexahydrocyclopenta[c]quinoline scaffold, MOD_66 incorporates a sulfonamide zinc-binding group for hCA inhibition and a phenolic hydroxyl group for ER modulation. In preclinical studies, the compound demonstrated nanomolar inhibitory potency against hCA IX and XII and micromolar potency in reducing estrogen-driven ER activity. It has shown anti-proliferative effects in breast and prostate cancer cell lines, making it a potential candidate for treating cancers where these targets are co-expressed, including triple-negative breast cancer.

Other names

(±)-3b MOD_66