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

• 13 new quinazoline nitrogen mustard derivatives were designed and synthesized.
• Their cytotoxicity in vitro was tested.
• Compound 22b could induce cell cycle delay at S and G2/M phase and cell apoptosis.
• Compound 22b could lead to obvious cancer growth regression in vivo.

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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