Drug intelligence / Profile preview

MOD_67

Development stage
Preclinical
Lead developer
University of Magna Graecia
Modality
Small Molecules
Administration
Oral
01

Overview

MOD_67 is a multi-target small molecule designed as a dual modulator of human carbonic anhydrases (hCA) and estrogen receptors (ER). Developed through a structure-based repurposing strategy, MOD_67 is a hexahydrocyclopenta[c]quinoline derivative that incorporates a sulfonamide group for zinc-binding hCA inhibition and a phenolic hydroxyl group for ER modulation. It demonstrates nanomolar inhibitory potency against the tumor-associated isoforms hCA IX and XII and micromolar antagonistic activity against ER⍺ and ERβ. MOD_67 is being investigated for the treatment of breast and prostate cancers, particularly those where these targets are co-expressed, such as triple-negative breast cancer. By simultaneously targeting pH regulation and estrogen-mediated signaling, MOD_67 aims to disrupt the tumor microenvironment and inhibit cancer cell proliferation.

Other names
Compound 11Compound11Compound-114-(8-hydroxy-2,3,3a,4,5,9b-hexahydro-1H-cyclopenta[c]quinolin-4-yl)benzenesulfonamide
02

Targets

ESR2 (ERβ)CA9 (Carbonic anhydrase IX)CA12 (Carbonic anhydrase XII)ESR1 (ERα)

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