Increasing the binding affinity of VEGFR-2 inhibitors by extending their hydrophobic interaction with the active site: Design, synthesis and biological evaluation of 1-substituted-4-(4-methoxybenzyl)phthalazine derivatives
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- 作者：Wagdy M. Eldehnaa ; wagdy2000@gmail.com" class="auth_mail" title="E-mail the corresponding author ; Sahar M. Abou-Serib ; c ; saharshaarawy_69@yahoo.com" class="auth_mail" title="E-mail the corresponding author ; Ahmed M. El Kerdawyb ; c ; Rezk R. Ayyadd ; e ; Abdallah M. Hamdyf ; Hazem A. Ghabbourg ; Mamdouh M. Alih ; Dalal A. Abou El Ellai
- 关键词：Phthalazine ; VEGFR-2 ; Hydrophobic interaction
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：4 May 2016
- 年：2016
- 卷：113
- 期：Complete
- 页码：50-62
- 全文大小：2189 K
文摘
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Two series of 4-(4-methoxybenzyl)phthalazines 4a-j & 7a-i were synthesized.
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The prepared phthalazines were evaluated for their inhibitory activity against VEGFR-2.
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Molecular docking was used to improve the binding affinity for 4a–j towards VEGFR-2.
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7g–i inhibited VEGFR-2 with IC50 = 0.086, 0.083 and 0.086 μM, respectively.
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Anticancer activity of the synthesized compounds was screened by the (NCI), USA.