Synthesis and anti-tumor evaluation of B-ring substituted steroidal pyrazoline derivatives

被引：34

作者：

Shamsuzzaman ^{[1
]}

Khanam, Hena ^{[1
]}

Mashrai, Ashraf ^{[1
]}

Sherwani, Asif ^{[2
]}

Owais, Mohammad ^{[2
]}

Siddiqui, Nazish ^{[3
]}

机构：

[1] Aligarh Muslim Univ, Dept Chem, Aligarh 202002, Uttar Pradesh, India

[2] Aligarh Muslim Univ, Interdisciplinary Biotechnol Unit, Aligarh 202002, Uttar Pradesh, India

[3] Aligarh Muslim Univ, Dept Illmul Advia Ajmal Khan Tibbiya Coll, Aligarh 202002, Uttar Pradesh, India

来源：

STEROIDS | 2013年 / 78卷 / 12-13期

关键词：

Cholest-5-en-7-one; Pyrazolines; Anticancer; MTT; SEM; PROLIFERATION; CHOLESTEROL;

D O I：

10.1016/j.steroids.2013.09.006

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 synthesis and anti-tumor activity screening of new steroidal derivatives (4-18) containing pharmacologically attractive pyrazoline moieties are performed. During in vitro anticancer evaluation, the newly synthesized compounds displayed moderate to good cytotoxicity on cervical and leukemia cancer cell lines. In addition these compounds were found to be nontoxic to normal cell (PBMCs) (IC50 > 50 mu M). The structure-activity relationship is also discussed. The most effective anticancer compound 9 was found to be active with IC50 value of 10.6 mu M. It demonstrated significant antiproliferative influence on Jurkat cell lines. The morphological changes and growth characteristics of HeLa cells treated with compound 4 were analyzed by means of SEM. (C) 2013 Elsevier Inc. All rights reserved.

引用

页码：1263 / 1272

页数：10

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