Steroidal pyrazolines evaluated as aromatase and quinone reductase-2 inhibitors for chemoprevention of cancer

The aromatase and quinone reductase-2 inhibition of synthesized heterocyclic pyrazole derivatives fused with steroidal structure for chemoprevention of cancer is reported herein. All compounds were interestingly less toxic than the reference drug (Cyproterone®). The aromatase inhibitory activities of these compounds were much more potent than the lead compound resveratrol, which has an IC50 of 80μM. In addition, all the compounds displayed potent quinone reductase-2 inhibition. Initially the acute toxicity of the compounds was assayed via the determination of their LD50. The aromatase and quinone reductase-2 inhibitors resulting from this study have potential value in the treatment and prevention of cancer. © 2012.