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

177 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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This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

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10.1021/jm020471r

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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 - https://www.scopus.com/pages/publications/0037464479

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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