Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents

Wen Tai Li; Der Ren Hwang; Ching Ping Chen; Chien Wei Shen; Chen Long Huang; Tung Wei Chen; Chi Hung Lin; Yee Ling Chang; Ying Ying Chang; Yue Kan Lo; Huan Yi Tseng; Chu Chung Lin; Jeng Shin Song; Hua Chien Chen; Shu Jen Chen; Se Hui Wu; Chiung Tong Chen

doi:10.1021/jm020471r

Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents

Wen Tai Li, Der Ren Hwang, Ching Ping Chen, Chien Wei Shen, Chen Long Huang, Tung Wei Chen, Chi Hung Lin, Yee Ling Chang, Ying Ying Chang, Yue Kan Lo, Huan Yi Tseng, Chu Chung Lin, Jeng Shin Song, Hua Chien Chen, Shu Jen Chen, Se Hui Wu, Chiung Tong Chen^*

^*Corresponding author for this work

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

174 Scopus citations

Abstract

A series of N-heterocyclic indolyl glyoxylamides were synthesized and evaluated for in vitro and in vivo anticancer activities. They exhibited a broad spectrum of anticancer activity not only in murine leukemic cancer cells but also in human gastric, breast, and uterus cancer cells as well as their multidrug resistant sublines with a wide range of IC₅₀ values. They also induced apoptosis and caused DNA fragmentation in human gastric cancer cells. Among the compounds studied, 7 showed the most potent activity of growth inhibition (IC₅₀ 17-1711 nM) in several human cancer cells. Given orally, compounds 7 and 13 dose-dependently prolonged the survival of animals inoculated with P388 leukemic cancer cells. N-Heterocyclic indolyl glyoxylamides may be useful as orally active chemotherapeutic agents against cancer and refractory cancerous diseases of multidrug resistance phenotype.

Original language	English
Pages (from-to)	1706-1715
Number of pages	10
Journal	Journal of Medicinal Chemistry
Volume	46
Issue number	9
DOIs	https://doi.org/10.1021/jm020471r
State	Published - 24 04 2003
Externally published	Yes

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Li, W. T., Hwang, D. R., Chen, C. P., Shen, C. W., Huang, C. L., Chen, T. W., Lin, C. H., Chang, Y. L., Chang, Y. Y., Lo, Y. K., Tseng, H. Y., Lin, C. C., Song, J. S., Chen, H. C., Chen, S. J., Wu, S. H., & Chen, C. T. (2003). Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents. Journal of Medicinal Chemistry, 46(9), 1706-1715. https://doi.org/10.1021/jm020471r

@article{6419e080d9db4c79982194dd36f4a99c,

title = "Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents",

abstract = "A series of N-heterocyclic indolyl glyoxylamides were synthesized and evaluated for in vitro and in vivo anticancer activities. They exhibited a broad spectrum of anticancer activity not only in murine leukemic cancer cells but also in human gastric, breast, and uterus cancer cells as well as their multidrug resistant sublines with a wide range of IC50 values. They also induced apoptosis and caused DNA fragmentation in human gastric cancer cells. Among the compounds studied, 7 showed the most potent activity of growth inhibition (IC50 17-1711 nM) in several human cancer cells. Given orally, compounds 7 and 13 dose-dependently prolonged the survival of animals inoculated with P388 leukemic cancer cells. N-Heterocyclic indolyl glyoxylamides may be useful as orally active chemotherapeutic agents against cancer and refractory cancerous diseases of multidrug resistance phenotype.",

author = "Li, {Wen Tai} and Hwang, {Der Ren} and Chen, {Ching Ping} and Shen, {Chien Wei} and Huang, {Chen Long} and Chen, {Tung Wei} and Lin, {Chi Hung} and Chang, {Yee Ling} and Chang, {Ying Ying} and Lo, {Yue Kan} and Tseng, {Huan Yi} and Lin, {Chu Chung} and Song, {Jeng Shin} and Chen, {Hua Chien} and Chen, {Shu Jen} and Wu, {Se Hui} and Chen, {Chiung Tong}",

year = "2003",

month = apr,

day = "24",

doi = "10.1021/jm020471r",

language = "英语",

volume = "46",

pages = "1706--1715",

journal = "Journal of Medicinal Chemistry",

issn = "0022-2623",

publisher = "American Chemical Society",

number = "9",

}

Li, WT, Hwang, DR, Chen, CP, Shen, CW, Huang, CL, Chen, TW, Lin, CH, Chang, YL, Chang, YY, Lo, YK, Tseng, HY, Lin, CC, Song, JS, Chen, HC, Chen, SJ, Wu, SH & Chen, CT 2003, 'Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents', Journal of Medicinal Chemistry, vol. 46, no. 9, pp. 1706-1715. https://doi.org/10.1021/jm020471r

TY - JOUR

T1 - Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents

AU - Li, Wen Tai

AU - Hwang, Der Ren

AU - Chen, Ching Ping

AU - Shen, Chien Wei

AU - Huang, Chen Long

AU - Chen, Tung Wei

AU - Lin, Chi Hung

AU - Chang, Yee Ling

AU - Chang, Ying Ying

AU - Lo, Yue Kan

AU - Tseng, Huan Yi

AU - Lin, Chu Chung

AU - Song, Jeng Shin

AU - Chen, Hua Chien

AU - Chen, Shu Jen

AU - Wu, Se Hui

AU - Chen, Chiung Tong

PY - 2003/4/24

Y1 - 2003/4/24

N2 - A series of N-heterocyclic indolyl glyoxylamides were synthesized and evaluated for in vitro and in vivo anticancer activities. They exhibited a broad spectrum of anticancer activity not only in murine leukemic cancer cells but also in human gastric, breast, and uterus cancer cells as well as their multidrug resistant sublines with a wide range of IC50 values. They also induced apoptosis and caused DNA fragmentation in human gastric cancer cells. Among the compounds studied, 7 showed the most potent activity of growth inhibition (IC50 17-1711 nM) in several human cancer cells. Given orally, compounds 7 and 13 dose-dependently prolonged the survival of animals inoculated with P388 leukemic cancer cells. N-Heterocyclic indolyl glyoxylamides may be useful as orally active chemotherapeutic agents against cancer and refractory cancerous diseases of multidrug resistance phenotype.

AB - A series of N-heterocyclic indolyl glyoxylamides were synthesized and evaluated for in vitro and in vivo anticancer activities. They exhibited a broad spectrum of anticancer activity not only in murine leukemic cancer cells but also in human gastric, breast, and uterus cancer cells as well as their multidrug resistant sublines with a wide range of IC50 values. They also induced apoptosis and caused DNA fragmentation in human gastric cancer cells. Among the compounds studied, 7 showed the most potent activity of growth inhibition (IC50 17-1711 nM) in several human cancer cells. Given orally, compounds 7 and 13 dose-dependently prolonged the survival of animals inoculated with P388 leukemic cancer cells. N-Heterocyclic indolyl glyoxylamides may be useful as orally active chemotherapeutic agents against cancer and refractory cancerous diseases of multidrug resistance phenotype.

UR - http://www.scopus.com/inward/record.url?scp=0037464479&partnerID=8YFLogxK

U2 - 10.1021/jm020471r

DO - 10.1021/jm020471r

M3 - 文章

C2 - 12699388

AN - SCOPUS:0037464479

SN - 0022-2623

VL - 46

SP - 1706

EP - 1715

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 9

ER -

Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents

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