Journal
TETRAHEDRON LETTERS
Volume 57, Issue 26, Pages 2829-2832Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2016.04.074
Keywords
2,2-Di(1H-indol-3-yl)-N-phenylacetamide derivatives; Indole; Unsymmetrical; AlCl3; Antiproliferative activity
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Funding
- National Science Foundation of China [81573286]
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A mild and highly efficient method has been developed for the synthesis of unsymmetrical 2,2di(1H-indol-3-yl)-N-phenylacetamide derivatives by the regioselective Friedel-Crafts alkylation of 2-hydroxy-2-(1H-indol-3-yl)-N-phenylacetamide derivatives with various indoles catalyzed by AlCl3 at room temperature in a short reaction time in high yields (up to 96%). All these compounds were screened for their antiproliferative activity against human colorectal carcinoma HCT116 cell line. The preliminary biological study showed that some of them exhibited moderate to good antiproliferative activity in vitro. Especially, compound 3e exerted the most powerful antiproliferative activity even better than the positive control MDM-2/p53 antagonist Nutlin-3a. (C) 2016 Elsevier Ltd. All rights reserved.
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