Design and synthesis of novel quinazoline nitrogen mustard derivatives as potential therapeutic agents for cancer

被引：31

作者：

Li, Shilei ^{[1
]}

Wang, Xiao ^{[1
]}

He, Yong ^{[1
,2
]}

Zhao, Mingxia ^{[1
]}

Chen, Yurong ^{[1
]}

Xu, Jingli ^{[1
]}

Feng, Man ^{[1
]}

Chang, Jin ^{[1
]}

Ning, Hongyu ^{[1
]}

Qi, Chuanmin ^{[1
]}

机构：

[1] Beijing Normal Univ, Coll Chem, Key Lab Radiopharmaceut, Minist Educ, Beijing 100875, Peoples R China

[2] Beijing Normal Univ, Expt Chem Ctr, Beijing 100875, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 67卷

基金：

中国国家自然科学基金;

关键词：

Quinazoline; Nitrogen mustard; Anticancer; Cell cycle; Apoptosis; Xenograft model; CHRONIC LYMPHOCYTIC-LEUKEMIA; D-GLUCOSYLISOPHOSPHORAMIDE MUSTARD; ALKYLATING-AGENTS; MULTIPLE-MYELOMA; SOLID TUMORS; MELPHALAN; CELLS; TRIAL; PHARMACOKINETICS; CYCLOPHOSPHAMIDE;

D O I：

10.1016/j.ejmech.2013.06.055

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

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 mu M), which was lower than Sorafenib. Compound 22b could inhibit cell cycle at S and G(2)/M phase and induce cell apoptosis. In the HepG2 xenograft model, 22b exhibited significant cancer growth inhibition with low host toxicity in vivo. (C) 2013 Elsevier Masson SAS. All rights reserved.

引用

页码：293 / 301

页数：9

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