Wensheng Zou, Liwen Jiang, Shuang Jia
Feb 1, 2018
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Abstract
(E) -3(dimethylamino) -1(1H-indol-3-yl) prop-2-en-1-one (4) is an important intermediate in many biologically active compounds such as osimertinib. In this work, compound (4) was synthesized through three steps, using 1H-indole as starting material. The synthetic method of 4 was optimized and can be used to synthesize the derivatives of (E) -3(dimethylamino) -1(1H-indol-3-yl) prop-2-en-1-one. And the structure of (E)-3(dimethylamino) -1-(1H-indol-3-yl) prop-2-en-1-one is confirmed by MS and 1 HNMR spectrum. Introduction Cancer is disease caused by the loss of normal regulation and over proliferation of cells in the bod[1]. Over-proliferation of cells called cancer cells, cancer cells can often encroach on the surrounding tissue, and even the body's circulatory system and / or lymphatic system can be transferred to other parts of the body [2]. Although there are many drugs currently used for the treatment of cancer through taking and surgery, the problem of poor drug treatment and recurrence of cancer remains to be solved urgently [3-4].To address the clinical challenge of drug resistance, the third generation of the EGFR TKI, which has been developed as a parent, can selectively act on EGFR T790M and the third generation EGFR TKI and cysteine 797 form at the ATP binding site Covalent bond. Early clinical trials have demonstrated the efficacy of the third generation of EGFR TKIs in patients with dual-mutant tumors (EGFR L858R / T790M and ex19del / T790M) and first-generation EGFR-TKI acquired resistance. Hydrophobic interaction between a large number of methionine residues in EGFR T790M and pyrimidine ring-based drugs may result in the specificity of such drugs to EGFR T790M. In recent years, many small-molecule anti-cancer drugs have been reported. Among them, (E) -3(dimethylamino) -1(1H-indol-3-yl) prop-2-en-1-one is an important intermediate for the synthesis of various active compounds. Therefore, a (E) -3(two methyl amino) -1(1H-indole -3base) propyl -2-ene -1ketone has been designed and synthesized in the study of anticancer drugs. Many (E)-3-(dimethylamino)-1-(1H-indol-3-yl)prop-2-en-1-one derivatives which exhibited potential biological activities[5]. Such as N-(2-((2-(dimethylamino) ethyl)(methyl)amino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amin o)phenyl)acrylamide(1),N-(3-((2-((4-(4-acetylpiperazin-1-yl)-2-methoxyphenyl)amin o)-5-(trifluoromethyl)pyrimidin-4-yl)oxy)phenyl)acrylamide(2)[6-7],N-(3-((5-chloro2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)oxy)phenyl)a crylamide(3)[8-9].These three drugs are the third generation of EGFR-TKI , have a good therapeutic effect on cancer. The treatment of T790M and L858R mutations is 251 Copyright © 2018, the Authors. Published by Atlantis Press. This is an open access article under the CC BY-NC license (http://creativecommons.org/licenses/by-nc/4.0/). Advances in Biological Sciences Research (ABSR), volume 6 2017 2nd International Conference on Biological Sciences and Technology (BST 2017)