The project has designed a novel drug formulation that inhibits breast cancer causing agent using carbonitrile group.

Inhibition of aromatase, a cytochrome P-450 enzyme responsible for biosynthesis of estrogens, is an effective approach for the prevention and treatment of estrogen-dependent breast cancer. Carbonitrile containing compound shows enhancement in aromatase inhibiting activity. The present work aims to introduce carbinitrile group in ring-D and to observe its impact on the aromatase inhibiting activity of the molecule. A novel A- and D-ring substituted steroid 16β-cyano-17β-hydroxy-4-phenylthia-4-androsten-3-one (7) has been synthesized and evaluated for its potential as aromatase inhibitor using human placental microsomal preparation as the enzyme source  and [1β-3H]androstenedione as substrate.

Dr. Prafulla M. Sabale
Parul Institute of Pharmacy, Vadodara