2-Amino-3,4,5-Trimethoxybenzophenones as Potent Tubulin Polymerization Inhibitors

Hsun-Yueh Chuang, Jang-Yang Chang, Mei-Jung Lai, Ching-Chuan Kuo, Hsueh Yun Lee, Hsing-Pang Hsieh, Ying-Jen Chen, Li-Tzong Chen, Wen-Yu Pan, Jing Ping Liou

研究成果: 雜誌貢獻文章

12 引文 (Scopus)

摘要

A series of novel 2-amino-3,4,5-trimethoxybenzophenone analogues exhibited excellent activity as tubulin polymerization inhibitors by targeting the colchicine binding site of microtubules. The lead compound 17 exhibited an IC50 value of 1.6μM, similar to that of combretastatin A-4 (IC50=1.9μM). It also displayed remarkable anti-proliferative activity, with IC50 values ranging from 7-16nM against a variety of human cancer cell lines and one MDR(+) cancer cell line. SAR information indicated that the introduction of an amino group at the C2 position of benzophenone ringA and the C3' position of benzophenone ringB play important roles in maximizing activity.

原文英語
頁(從 - 到)450-456
頁數7
期刊ChemMedChem
6
發行號3
DOIs
出版狀態已發佈 - 三月 7 2011

指紋

Tubulin Modulators
Inhibitory Concentration 50
Cells
Lead compounds
Colchicine
Cell Line
Binding Sites
Microtubules
Neoplasms
benzophenone

ASJC Scopus subject areas

  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Organic Chemistry
  • Molecular Medicine

引用此文

2-Amino-3,4,5-Trimethoxybenzophenones as Potent Tubulin Polymerization Inhibitors. / Chuang, Hsun-Yueh; Chang, Jang-Yang; Lai, Mei-Jung; Kuo, Ching-Chuan; Lee, Hsueh Yun; Hsieh, Hsing-Pang; Chen, Ying-Jen; Chen, Li-Tzong; Pan, Wen-Yu; Liou, Jing Ping.

於: ChemMedChem, 卷 6, 編號 3, 07.03.2011, p. 450-456.

研究成果: 雜誌貢獻文章

Chuang, H-Y, Chang, J-Y, Lai, M-J, Kuo, C-C, Lee, HY, Hsieh, H-P, Chen, Y-J, Chen, L-T, Pan, W-Y & Liou, JP 2011, '2-Amino-3,4,5-Trimethoxybenzophenones as Potent Tubulin Polymerization Inhibitors', ChemMedChem, 卷 6, 編號 3, 頁 450-456. https://doi.org/10.1002/cmdc.201000479
Chuang, Hsun-Yueh ; Chang, Jang-Yang ; Lai, Mei-Jung ; Kuo, Ching-Chuan ; Lee, Hsueh Yun ; Hsieh, Hsing-Pang ; Chen, Ying-Jen ; Chen, Li-Tzong ; Pan, Wen-Yu ; Liou, Jing Ping. / 2-Amino-3,4,5-Trimethoxybenzophenones as Potent Tubulin Polymerization Inhibitors. 於: ChemMedChem. 2011 ; 卷 6, 編號 3. 頁 450-456.
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abstract = "A series of novel 2-amino-3,4,5-trimethoxybenzophenone analogues exhibited excellent activity as tubulin polymerization inhibitors by targeting the colchicine binding site of microtubules. The lead compound 17 exhibited an IC50 value of 1.6μM, similar to that of combretastatin A-4 (IC50=1.9μM). It also displayed remarkable anti-proliferative activity, with IC50 values ranging from 7-16nM against a variety of human cancer cell lines and one MDR(+) cancer cell line. SAR information indicated that the introduction of an amino group at the C2 position of benzophenone ringA and the C3' position of benzophenone ringB play important roles in maximizing activity.",
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AU - Chang, Jang-Yang

AU - Lai, Mei-Jung

AU - Kuo, Ching-Chuan

AU - Lee, Hsueh Yun

AU - Hsieh, Hsing-Pang

AU - Chen, Ying-Jen

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AU - Pan, Wen-Yu

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