B 环取代甾体吡唑啉衍生物的合成及抗肿瘤活性评价。
Synthesis and anti-tumor evaluation of B-ring substituted steroidal pyrazoline derivatives.
机构信息
Department of Chemistry, Aligarh Muslim University, Aligarh 202 002, India.
出版信息
Steroids. 2013 Dec 11;78(12-13):1263-72. doi: 10.1016/j.steroids.2013.09.006. Epub 2013 Sep 21.
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 μM). The structure-activity relationship is also discussed. The most effective anticancer compound 9 was found to be active with IC50 value of 10.6 μM. 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.
进行了含有药理学上有吸引力的吡唑啉部分的新甾体衍生物（4-18）的合成和抗肿瘤活性筛选。在体外抗癌评估中，新合成的化合物对宫颈和白血病癌细胞系显示出中等至良好的细胞毒性。此外，这些化合物被发现对正常细胞（PBMCs）无毒性（IC50>50 μM）。还讨论了结构-活性关系。最有效的抗癌化合物 9 的活性 IC50 值为 10.6 μM。它对 Jurkat 细胞系显示出显著的抗增殖影响。通过 SEM 分析了用化合物 4 处理的 HeLa 细胞的形态变化和生长特征。
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