title: Steroidal pyrazolines evaluated as aromatase and quinone reductase-2 inhibitors for chemoprevention of cancer.
abstract: 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 IC(50) of 80 μM. 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 LD(50). The aromatase and quinone reductase-2 inhibitors resulting from this study have potential value in the treatment and prevention of cancer.
authors.affiliation: Research Unit, Saco Pharm. Co., 6th October City 11632, Egypt.
authors.forename: Mohamed M
authors.initials: MM
authors.lastname: Abdalla
authors.forename: Mohamed A
authors.initials: MA
authors.lastname: Al-Omar
authors.forename: Mashooq A
authors.initials: MA
authors.lastname: Bhat
authors.forename: Abdel-Galil E
authors.initials: AG
authors.lastname: Amr
authors.forename: Abdullah M
authors.initials: AM
authors.lastname: Al-Mohizea
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001141:Aromatase / Q000378:metabolism*; D047072:Aromatase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D018890:Chemoprevention; D004353:Drug Evaluation, Preclinical; D006801:Humans; D020128:Inhibitory Concentration 50; D016660:NAD(P)H Dehydrogenase (Quinone) / Q000037:antagonists & inhibitors*; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013256:Steroids / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D047072:Aromatase Inhibitors; D011720:Pyrazoles; D013256:Steroids; D001141:Aromatase; D016660:NAD(P)H Dehydrogenase (Quinone)