Drug intelligence / Profile preview

2-(2-chlorophenylamino)-5-(3-fluorophenyl)-1,3,4-thiadiazole

Development stage
Preclinical
Modality
Small Molecules
01

Overview

2-(2-chlorophenylamino)-5-(3-fluorophenyl)-1,3,4-thiadiazole is a synthetic small molecule and nonsteroidal aromatase inhibitor under investigation for the treatment of hormone-dependent breast cancer. It belongs to a series of halogen-substituted 1,3,4-thiadiazole derivatives designed to selectively target estrogen biosynthesis. The compound demonstrates significant cytotoxic activity against estrogen-dependent MCF-7 breast cancer cells while showing minimal effect on estrogen-independent cell lines, suggesting high selectivity. In silico studies, including molecular docking and dynamics, indicate that it binds within the active site of the aromatase enzyme (CYP19A1), forming stable interactions similar to those of established clinical inhibitors. By inhibiting aromatase, the compound prevents the conversion of androgens into estrogens, thereby depriving hormone-sensitive tumors of necessary growth signals.

02

Targets

CYP19A1 (Aromatase)

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