Novel 2H-chromen derivatives: design, synthesis and anticancer activity
Novel 2H-chromen derivatives: design, synthesis and anticancer activity
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新型2H-苯并吡喃衍生物：设计、合成和抗癌活性
DOI：
10.1039/c3ra47252c
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发表时间：
2014-01-01
期刊：
影响因子：
3.9
通讯作者：
Liu, Xin Hua
中科院分区：
文献类型：
--
作者：
Qiang, Dong Zhi;Shi, Jing Bo;Liu, Xin Hua
设计并合成了一系列与2H-色胺相连的新型二氢吡唑类化合物。所有化合物都在体外对MGC-803、BCap-37、SGC-7901和HepG(2)细胞株具有抗增殖活性。结果表明，化合物4a和10a对HepG(2)细胞有较强的抑制活性，对GES-1和L-02细胞株无明显毒性。化合物10a对端粒酶的抑制活性最强，其IC50值为0.98+/-0.11µM，与TERT的活性部位相吻合。进一步探讨了化合物10a抑制细胞增殖的分子机制，提示化合物10a可抑制hTERT的表达和抑制Wnt/β-catenin信号转导。
A series of novel dihydropyrazole derivatives linked with 2H-chromen were designed and synthesized. All of the compounds have been screened for their antiproliferative activity against MGC-803, Bcap-37, SGC-7901 and HepG(2) cell lines in vitro. The results revealed that compounds 4a and 10a exhibited strong inhibitory activity against HepG(2) cell and manifested obvious un-toxic effect on GES-1 and L-02 cell lines. Some title compounds were tested against telomerase, compound 10a showed the most potent inhibitory activity with IC50 value at 0.98 +/- 0.11 mu M, it could fit well into the active site of TERT. The further molecular mechanism of antiproliferation was explored, the data suggested that compound 10a could inhibit hTERT expression and Wnt/beta-catenin signaling.