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

被引：44

作者：

Abdalla, Mohamed M. ^{[2
]}

Al-Omar, Mohamed A. ^{[3
]}

Bhat, Mashooq A. ^{[3
]}

Amr, Abdel-Galil E. ^{[1
,4
]}

Al-Mohizea, Abdullah M. ^{[5
]}

机构：

[1] King Saud Univ, Coll Pharm, DEDC, Riyadh 11451, Saudi Arabia

[2] Saco Pharm Co, Res Unit, Cairo 11632, Egypt

[3] King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, Riyadh 11451, Saudi Arabia

[4] Natl Res Ctr, Appl Organ Chem Dept, Cairo 12622, Egypt

[5] King Saud Univ, Coll Pharm, Dept Pharmaceut, Riyadh 11451, Saudi Arabia

来源：

INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES | 2012年 / 50卷 / 04期

关键词：

Steroidal pyrazolines; Aromatase inhibitor; Quinone reductase-2 inhibitor; RECEPTOR MODULATORS SERMS; HETEROCYCLIC-COMPOUNDS; BREAST-CANCER; POTENTIAL ANTICANCER; DERIVATIVES; MELATONIN; ANALOGS;

D O I：

10.1016/j.ijbiomac.2012.02.006

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页码：1127 / 1132

页数：6

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