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Synthesis of α-indolylacrylates as potential anticancer agents using a Brønsted acid ionic liquid catalyst and the butyl acetate solvent
RSC Advances ( IF 3.9 ) Pub Date : 2020-4-2 , DOI: 10.1039/d0ra00990c Ahmed El-Harairy 1, 2 , Mennatallah Shaheen 3 , Jun Li 2 , Yuzhou Wu 2 , Minghao Li 2 , Yanlong Gu 2, 4
RSC Advances ( IF 3.9 ) Pub Date : 2020-4-2 , DOI: 10.1039/d0ra00990c Ahmed El-Harairy 1, 2 , Mennatallah Shaheen 3 , Jun Li 2 , Yuzhou Wu 2 , Minghao Li 2 , Yanlong Gu 2, 4
Affiliation
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 (IC50 = 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.
中文翻译:
使用布朗斯台德酸离子液体催化剂和乙酸丁酯溶剂合成 α-吲哚丙烯酸酯作为潜在的抗癌剂
在这项研究中,使用布朗斯台德酸离子液体催化剂在乙酸丁酯溶剂中,2-取代的吲哚与各种丙酮酸盐反应合成了新的 α-吲哚丙烯酸酯衍生物。这是关于丙酮酸化合物在合成丙烯酸吲哚酯中的应用的第一篇报道。可以以良好至极好的产率获得丙烯酸酯衍生物。初步生物学评估揭示了它们有希望的抗癌活性(化合物4l的 IC 50 = 9.73 μM ),并表明吲哚核心和丙烯酸酯部分都有望用于开发新型抗癌药物。对新合成的衍生物评估了 Lipinski 规则和 Veber 参数。
更新日期:2020-04-02
中文翻译:
使用布朗斯台德酸离子液体催化剂和乙酸丁酯溶剂合成 α-吲哚丙烯酸酯作为潜在的抗癌剂
在这项研究中,使用布朗斯台德酸离子液体催化剂在乙酸丁酯溶剂中,2-取代的吲哚与各种丙酮酸盐反应合成了新的 α-吲哚丙烯酸酯衍生物。这是关于丙酮酸化合物在合成丙烯酸吲哚酯中的应用的第一篇报道。可以以良好至极好的产率获得丙烯酸酯衍生物。初步生物学评估揭示了它们有希望的抗癌活性(化合物4l的 IC 50 = 9.73 μM ),并表明吲哚核心和丙烯酸酯部分都有望用于开发新型抗癌药物。对新合成的衍生物评估了 Lipinski 规则和 Veber 参数。