El-Harairy Ahmed, Shaheen Mennatallah, Li Jun, Wu Yuzhou, Li Minghao, Gu Yanlong
Environmental, Energy and Green Chemistry Laboratory, Faculty of Agriculture, Damietta University 34511 Damietta Egypt
School of Chemistry and Chemical Engineering, Huazhong University of Science and Technology 430074 Wuhan China.
RSC Adv. 2020 Apr 2;10(23):13507-13516. doi: 10.1039/d0ra00990c. eCollection 2020 Apr 1.
In this study, new α-indolylacrylate derivatives were synthesized by the reaction of 2-substituted indoles with various pyruvates using a Brønsted acid ionic liquid catalyst in butyl acetate solvent. This is the first report on the application of pyruvate compounds for the synthesis of indolylacrylates. The acrylate derivatives could be obtained in good to excellent yields. A preliminary biological evaluation revealed their promising anticancer activity (IC = 9.73 μM for the compound 4l) and indicated that both the indole core and the acrylate moieties are promising for the development of novel anticancer drugs. The Lipinski's rule and Veber's parameters were assessed for the newly synthesized derivatives.
在本研究中，以布伦斯特酸离子液体为催化剂，2-取代吲哚与各种丙酮酸在乙酸丁酯溶剂中反应，合成了新型α-吲哚基丙烯酸酯衍生物。这是关于丙酮酸化合物用于合成吲哚基丙烯酸酯的首次报道。丙烯酸酯衍生物的产率良好至优异。初步生物学评价显示它们具有良好的抗癌活性（化合物4l的IC = 9.73 μM），表明吲哚核心和丙烯酸酯部分对于开发新型抗癌药物都很有前景。对新合成的衍生物评估了Lipinski规则和Veber参数。
