National Biopesticide Engineering Technology Research Center, Hubei Biopesticide Engineering Research Center, Hubei Academy of Agricultural Sciences, Wuhan 430064, People's Republic of China.
Sci Rep. 2017 Mar 14;7:44439. doi: 10.1038/srep44439.
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 IC 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.
设计并制备了一系列源于脱氢表雄酮的甾体[17,16-d]嘧啶类化合物，通过方便的杂环化反应。对这些获得的化合物进行了体外抗癌活性评价，针对人癌细胞系（HepG2、Huh-7 和 SGC-7901），结果表明，与 5-氟尿嘧啶（5-FU）相比，其中一些杂环嘧啶衍生物对所有测试的细胞系均表现出显著良好的细胞毒性活性，特别是化合物 3b 对所有测试的细胞系均表现出高潜在的生长抑制活性，IC 值分别为 5.41 ± 1.34、5.65 ± 1.02 和 10.64 ± 1.49 μM，可能作为发现新型抗癌剂的有前途的先导骨架。
