Synthesis and structure-activity relationships of 2-amino-1- aroylnaphthalene and 2-hydroxy-1-aroylnaphthalenes as potent antitubulin agents

Gadarla Randheer Reddy; Ching Chuan Kuo; Uan Kang Tan; Mohane Selvaraj Coumar; Chi Yen Chang; Yi Kun Chiang; Mei Jung Lai; Jiann Yih Yeh; Su Ying Wu; Jang Yang Chang; Jing Ping Liou; Hsing Pang Hsieh

doi:10.1021/jm8008635

Synthesis and structure-activity relationships of 2-amino-1- aroylnaphthalene and 2-hydroxy-1-aroylnaphthalenes as potent antitubulin agents

Gadarla Randheer Reddy, Ching Chuan Kuo, Uan Kang Tan, Mohane Selvaraj Coumar, Chi Yen Chang, Yi Kun Chiang, Mei Jung Lai, Jiann Yih Yeh, Su Ying Wu, Jang Yang Chang, Jing Ping Liou, Hsing Pang Hsieh

Research output: Contribution to journal › Article › peer-review

26 Citations (Scopus)

Abstract

A series of aroylnaphthalene derivatives were prepared as bioisosteres of combrestatin A-4 and evaluated for anticancer activity. 2-Amino-1- aroylnaphthalene and 2-hydroxy-1-aroylnaphthalene, 9 and 8, respectively, showed strong antiproliferative activity with IC₅₀ values of 2.1-26.3 nM against a panel of human cancer cell lines including multiple-drug resistant cell line. Compound 9 demonstrated better antiproliferative activity and has a comparable tubulin binding efficacy as that of colchicine.

Original language	English
Pages (from-to)	8163-8167
Number of pages	5
Journal	Journal of Medicinal Chemistry
Volume	51
Issue number	24
DOIs	https://doi.org/10.1021/jm8008635
Publication status	Published - 2008 Dec 25

All Science Journal Classification (ASJC) codes

Molecular Medicine
Drug Discovery

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Reddy, G. R., Kuo, C. C., Tan, U. K., Coumar, M. S., Chang, C. Y., Chiang, Y. K., Lai, M. J., Yeh, J. Y., Wu, S. Y., Chang, J. Y., Liou, J. P., & Hsieh, H. P. (2008). Synthesis and structure-activity relationships of 2-amino-1- aroylnaphthalene and 2-hydroxy-1-aroylnaphthalenes as potent antitubulin agents. Journal of Medicinal Chemistry, 51(24), 8163-8167. https://doi.org/10.1021/jm8008635

Reddy, Gadarla Randheer ; Kuo, Ching Chuan ; Tan, Uan Kang ; Coumar, Mohane Selvaraj ; Chang, Chi Yen ; Chiang, Yi Kun ; Lai, Mei Jung ; Yeh, Jiann Yih ; Wu, Su Ying ; Chang, Jang Yang ; Liou, Jing Ping ; Hsieh, Hsing Pang. / Synthesis and structure-activity relationships of 2-amino-1- aroylnaphthalene and 2-hydroxy-1-aroylnaphthalenes as potent antitubulin agents. In: Journal of Medicinal Chemistry. 2008 ; Vol. 51, No. 24. pp. 8163-8167.

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abstract = "A series of aroylnaphthalene derivatives were prepared as bioisosteres of combrestatin A-4 and evaluated for anticancer activity. 2-Amino-1- aroylnaphthalene and 2-hydroxy-1-aroylnaphthalene, 9 and 8, respectively, showed strong antiproliferative activity with IC50 values of 2.1-26.3 nM against a panel of human cancer cell lines including multiple-drug resistant cell line. Compound 9 demonstrated better antiproliferative activity and has a comparable tubulin binding efficacy as that of colchicine.",

author = "Reddy, {Gadarla Randheer} and Kuo, {Ching Chuan} and Tan, {Uan Kang} and Coumar, {Mohane Selvaraj} and Chang, {Chi Yen} and Chiang, {Yi Kun} and Lai, {Mei Jung} and Yeh, {Jiann Yih} and Wu, {Su Ying} and Chang, {Jang Yang} and Liou, {Jing Ping} and Hsieh, {Hsing Pang}",

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Synthesis and structure-activity relationships of 2-amino-1- aroylnaphthalene and 2-hydroxy-1-aroylnaphthalenes as potent antitubulin agents. / Reddy, Gadarla Randheer; Kuo, Ching Chuan; Tan, Uan Kang; Coumar, Mohane Selvaraj; Chang, Chi Yen; Chiang, Yi Kun; Lai, Mei Jung; Yeh, Jiann Yih; Wu, Su Ying; Chang, Jang Yang; Liou, Jing Ping; Hsieh, Hsing Pang.

In: Journal of Medicinal Chemistry, Vol. 51, No. 24, 25.12.2008, p. 8163-8167.

Research output: Contribution to journal › Article › peer-review

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