European Journal of Medicinal Chemistry p. 249 - 261 (2016)
Update date:2022-08-05
Topics:
Chen, Wei
Zhang, Guoxian
Guo, Liang
Fan, Wenxi
Ma, Qin
Zhang, Xiaodong
Du, Runlei
Cao, Rihui
We have synthesized and evaluated a series of novel alkyl diamine linked bivalent β-carbolines as potent angiogenesis inhibitors. The results demonstrated that most bivalent β-carbolines exhibited significant antiproliferative effects against human umbilical vein cell lines EA.HY926. Compound 4m was found to be the most potent antiproliferative agent with IC50value of 2.16?μM against EA.HY926?cell lines. Mechanism investigations revealed that compound 4m could significantly inhibit EA.HY926?cells migration and tube formation in a dose-dependent manner. Moreover, compound 4m also showed obvious angiogenesis inhibitory effects in CAM assay, and the antiangiogenetic potency was more potent than the reference drug Endostar. The bivalent β-carbolines might be served as candidates for the development of vascular targeting antitumor drugs.
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