Journal
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
Volume 50, Issue 4, Pages 1127-1132Publisher
ELSEVIER
DOI: 10.1016/j.ijbiomac.2012.02.006
Keywords
Steroidal pyrazolines; Aromatase inhibitor; Quinone reductase-2 inhibitor
Funding
- King Saud University [RGP-VPP-099]
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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 (R)). The aromatase inhibitory activities of these compounds were much more potent than the lead compound resveratrol, which has an IC50 of 80 mu M. 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. Crown Copyright (C) 2012 Published by Elsevier B.V. All rights reserved.
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