设计和合成新型喹唑啉氮芥衍生物作为癌症潜在的治疗药物。
Design and synthesis of novel quinazoline nitrogen mustard derivatives as potential therapeutic agents for cancer.
机构信息
Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
出版信息
Eur J Med Chem. 2013 Sep;67:293-301. doi: 10.1016/j.ejmech.2013.06.055. Epub 2013 Jul 4.
Thirteen novel quinazoline nitrogen mustard derivatives were designed, synthesized and evaluated for their anticancer activities in vitro and in vivo. Cytotoxicity assays were carried out in five cancer cell lines (HepG2, SH-SY5Y, DU145, MCF-7 and A549) and one normal human cell line (GES-1), in which compound 22b showed very low IC50 to HepG2 (the IC50 value is 3.06 μM), which was lower than Sorafenib. Compound 22b could inhibit cell cycle at S and G2/M phase and induce cell apoptosis. In the HepG2 xenograft model, 22b exhibited significant cancer growth inhibition with low host toxicity in vivo.
设计、合成并评价了 13 种新型喹唑啉氮芥衍生物的体外和体内抗癌活性。在五种癌细胞系（HepG2、SH-SY5Y、DU145、MCF-7 和 A549）和一种正常人类细胞系（GES-1）中进行了细胞毒性测定，其中化合物 22b 对 HepG2 的 IC50 值非常低（IC50 值为 3.06 μM），低于索拉非尼。化合物 22b 可抑制 S 和 G2/M 期细胞周期，并诱导细胞凋亡。在 HepG2 异种移植模型中，22b 在体内表现出显著的肿瘤生长抑制作用，同时宿主毒性低。
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