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Design and synthesis of novel quinazoline nitrogen mustard derivatives as potential therapeutic agents for cancer. 2013
Shilei Li, and
Xiao Wang, and
Yong He, and
Mingxia Zhao, and
Yurong Chen, and
Jingli Xu, and
Man Feng, and
Jin Chang, and
Hongyu Ning, and
Chuanmin Qi
Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
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.
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