Steroidal[17,16-d]pyrimidines derived from dehydroepiandrosterone: A convenient synthesis, antiproliferation activity, structure-activity relationships, and role of heterocyclic moiety.
Steroidal[17,16-d]pyrimidines derived from dehydroepiandrosterone: A convenient synthesis, antiproliferation activity, structure-activity relationships, and role of heterocyclic moiety.
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脱氢表雄酮衍生的甾体[17,16-d]嘧啶：便捷的合成、抗增殖活性、结构-活性关系和杂环部分的作用
DOI：
10.1038/srep44439
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发表时间：
2017-03-14
影响因子：
4.6
通讯作者：
Yang Z
中科院分区：
文献类型：
--
作者：
Ke S;Shi L;Zhang Z;Yang Z
以脱氢表雄酮为原料，设计并合成了一系列甾体[17，16-d]嘧啶类化合物。这些化合物的体外抗癌活性对人癌细胞系进行了评价（HepG 2、Huh-7和SGC-7901），其证明与5-氟尿嘧啶（5-FU）相比，这些杂环嘧啶衍生物中的一些对所有测试的细胞系表现出显著良好的细胞毒活性，尤其是，化合物3b对所有测试的细胞系均表现出高的潜在生长抑制活性，IC 50值分别为5.41 ± 1.34、5.65 ± 1.02和10.64 ± 1.49 μM，有望成为发现新型抗癌药物的先导支架。
A series of steroidal[17,16-d]pyrimidines derived from dehydroepiandrosterone were designed and prepared by a convenient heterocyclization reaction. The in vitro anticancer activities for these obtained compounds were evaluated against human cancer cell lines (HepG2, Huh-7, and SGC-7901), which demonstrated that some of these heterocyclic pyrimidine derivatives exhibited significantly good cytotoxic activities against all tested cell lines compared with 5-fluorouracil (5-FU), especially, compound 3b exhibited high potential growth inhibitory activities against all tested cell lines with the IC50 values of 5.41 ± 1.34, 5.65 ± 1.02 and 10.64 ± 1.49 μM, respectively, which might be used as promising lead scaffold for discovery of novel anticancer agents.