Design and Synthesis of Mono-, Di-, Tri- and Tetraindoles Derivatives as Novel Histone Deacetylase Inhibitors

Please use this identifier to cite or link to this item: http://ir.lib.ncu.edu.tw/handle/987654321/83227

Title:	Design and Synthesis of Mono-, Di-, Tri- and Tetraindoles Derivatives as Novel Histone Deacetylase Inhibitors
Authors:	吳佳欣;Wu, Chia-Hsin
Contributors:	化學學系
Keywords:	組織蛋白去乙醯酶抑制劑;四吲哚衍生物;抗三陰性乳癌藥物;Histone deacetylase inhibitor;Tetraindole derivatives;TNBC anticancer agent
Date:	2020-07-28
Issue Date:	2020-09-02 15:11:20 (UTC+8)
Publisher:	國立中央大學
Abstract:	在這次的研究中，我們設計合成了一系列的單，雙，三，和四吲哚的衍生物(CHW01-03, CHW05, CHW04 and AMB09-10)，它們具有類似Vorinostat （suberanilohydroxamic acid）的側鏈，為FDA批准的HDAC抑制劑。在本篇論文中，我們設計和合成了一系列化合物，以測試其對組蛋白脫乙酰基酶（HDAC）的抑制和對TNBC癌細胞系MDA-MB-231的抑制生長的功能。在此系列化合物中，CHW03對MDA-MB-231細胞株具有最佳的抗增值能力，IC50值為1.4 µM。另外，關於組蛋白脫乙酰基酶抑制的進一步研究也正在研究中。;In this investigation, we discovered a series of mono-, di-, tri-, and tetraindoles derivatives (CHW01-03, CHW05, CHW04 and AMB09-10), possessing different number of indole rings and similar side chain like Vorinostat (SAHA), a HDAC inhibitor approved by FDA. Their inhibition of histone deacetylase (HDAC) and the inhibitory growth against TNBC cancer cell line MDA-MB-231 was evaluated. Among this series of compounds, CHW03 has the best antiproliferative activity against MDA-MB-231 cell line with an IC50 value of 1.4 µM. Further study in histone deacetylase inhibition is in progress.
Appears in Collections:	[Graduate Institute of Chemistry] Electronic Thesis & Dissertation

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