1-Piperazinylphthalazines as potential VEGFR-2 inhibitors and anticancer agents: Synthesis and in vitro biological evaluation
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- 作者：Sahar M. Abou-Seria ; Wagdy M. Eldehnab ; wagdy2000@gmail.com" class="auth_mail" title="E-mail the corresponding author ; Mamdouh M. Alic ; Dalal A. Abou El Ellad ; dalal@pharma.asu.edu.eg" class="auth_mail" title="E-mail the corresponding author
- 关键词：Synthesis ; 1-Piperazinylphthalazines ; VEGFR-2 inhibitors ; Anticancer activity
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：1 January 2016
- 年：2016
- 卷：107
- 期：Complete
- 页码：165-179
- 全文大小：2110 K
文摘
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Three series of 1-piperazinyl-4-phenylphthalazines 16a-k, 18a-e & 21a-g were synthesized.
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The prepared phthalazines were evaluated for their inhibitory activity against VEGFR-2.
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16k and 21d inhibited VEGFR-2 with IC50 = 0.35 ± 0.03 and 0.40 ± 0.04 μM, respectively.
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Anticancer activity of seventeen selected compounds was screened by the NCI USA.
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Compound 16k exhibited potent broad spectrum anti-proliferative activity in NCI assay.