Antitumor Agents. 111.† New 4-Hydroxylated and 4-Halogenated Anilino Derivatives of 4'-Demethylepipodophyllotoxin as Potent Inhibitors of Human DNA Topoisomerase II

Kuo Hsiung Lee; Scott A. Beers; Masami Mori; Zhe Qing Wang; Yao Haur Kuo; Li Li; Su Ying Liu; Jang Yang Chang; Fu Sheng Han; Yung Chi Cheng

doi:10.1021/jm00167a013

Antitumor Agents. 111.† New 4-Hydroxylated and 4-Halogenated Anilino Derivatives of 4'-Demethylepipodophyllotoxin as Potent Inhibitors of Human DNA Topoisomerase II

Kuo Hsiung Lee, Scott A. Beers, Masami Mori, Zhe Qing Wang, Yao Haur Kuo, Li Li, Su Ying Liu, Jang Yang Chang, Fu Sheng Han, Yung Chi Cheng

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Abstract

A series of C-4 hydroxylated and halogenated anilino derivatives of epipodophyllotoxin or 4'-demethylepipodophyllotoxin have been synthesized and evaluated for their inhibitory activity against the human DNA topoisomerase II as well as for their activity in causing cellular protein-linked DNA breakage. Compounds 11-17 and 22 are more potent than etoposide in causing DNA breakage, while compounds 11-13, 15, 16, and 20 are as active or more active than etoposide in their inhibition of the human DNA topoisomerase II. The cytotoxicity in KB cells appears to have no direct correlation with their ability to inhibit DNA topoisomerase II and to cause protein-linked DNA breaks in cells.

Original language	English
Pages (from-to)	1364-1368
Number of pages	5
Journal	Journal of Medicinal Chemistry
Volume	33
Issue number	5
DOIs	https://doi.org/10.1021/jm00167a013
Publication status	Published - May 1990
Externally published	Yes

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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Lee, K. H., Beers, S. A., Mori, M., Wang, Z. Q., Kuo, Y. H., Li, L., Liu, S. Y., Chang, J. Y., Han, F. S., & Cheng, Y. C. (1990). Antitumor Agents. 111.† New 4-Hydroxylated and 4-Halogenated Anilino Derivatives of 4'-Demethylepipodophyllotoxin as Potent Inhibitors of Human DNA Topoisomerase II. Journal of Medicinal Chemistry, 33(5), 1364-1368. https://doi.org/10.1021/jm00167a013

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abstract = "A series of C-4 hydroxylated and halogenated anilino derivatives of epipodophyllotoxin or 4'-demethylepipodophyllotoxin have been synthesized and evaluated for their inhibitory activity against the human DNA topoisomerase II as well as for their activity in causing cellular protein-linked DNA breakage. Compounds 11-17 and 22 are more potent than etoposide in causing DNA breakage, while compounds 11-13, 15, 16, and 20 are as active or more active than etoposide in their inhibition of the human DNA topoisomerase II. The cytotoxicity in KB cells appears to have no direct correlation with their ability to inhibit DNA topoisomerase II and to cause protein-linked DNA breaks in cells.",

author = "Lee, {Kuo Hsiung} and Beers, {Scott A.} and Masami Mori and Wang, {Zhe Qing} and Kuo, {Yao Haur} and Li Li and Liu, {Su Ying} and Chang, {Jang Yang} and Han, {Fu Sheng} and Cheng, {Yung Chi}",

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doi = "10.1021/jm00167a013",

language = "English",

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AU - Lee, Kuo Hsiung

AU - Beers, Scott A.

AU - Mori, Masami

AU - Wang, Zhe Qing

AU - Kuo, Yao Haur

AU - Li, Li

AU - Liu, Su Ying

AU - Chang, Jang Yang

AU - Han, Fu Sheng

AU - Cheng, Yung Chi

PY - 1990/5

Y1 - 1990/5

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AB - A series of C-4 hydroxylated and halogenated anilino derivatives of epipodophyllotoxin or 4'-demethylepipodophyllotoxin have been synthesized and evaluated for their inhibitory activity against the human DNA topoisomerase II as well as for their activity in causing cellular protein-linked DNA breakage. Compounds 11-17 and 22 are more potent than etoposide in causing DNA breakage, while compounds 11-13, 15, 16, and 20 are as active or more active than etoposide in their inhibition of the human DNA topoisomerase II. The cytotoxicity in KB cells appears to have no direct correlation with their ability to inhibit DNA topoisomerase II and to cause protein-linked DNA breaks in cells.

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Antitumor Agents. 111.† New 4-Hydroxylated and 4-Halogenated Anilino Derivatives of 4'-Demethylepipodophyllotoxin as Potent Inhibitors of Human DNA Topoisomerase II

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