Antitumor agents 295. E-ring hydroxylated antofine and cryptopleurine analogues as antiproliferative agents: Design, synthesis, and mechanistic studies

Xiaoming Yang; Qian Shi; Chin Yu Lai; Chi Yuan Chen; Emika Ohkoshi; Shuenn Chen Yang; Chih Ya Wang; Kenneth F. Bastow; Tian Shung Wu; Shiow Lin Pan; Che Ming Teng; Pan Chyr Yang; Kuo Hsiung Lee

doi:10.1021/jm3001218

Antitumor agents 295. E-ring hydroxylated antofine and cryptopleurine analogues as antiproliferative agents: Design, synthesis, and mechanistic studies

Xiaoming Yang, Qian Shi, Chin Yu Lai, Chi Yuan Chen, Emika Ohkoshi, Shuenn Chen Yang, Chih Ya Wang, Kenneth F. Bastow, Tian Shung Wu, Shiow Lin Pan, Che Ming Teng, Pan Chyr Yang, Kuo Hsiung Lee

研究成果: 雜誌貢獻 › 文章 › 同行評審

23 引文斯高帕斯（Scopus）

摘要

Various E-ring hydroxylated antofine and cryptopleurine analogues were designed, synthesized, and tested against five human cancer cell lines. Interesting structure-activity relationship (SAR) correlations were found among these new compounds. The most potent compound 13b was further tested against a series of nonsmall cell lung cancer (NSCLC) cell lines in which it showed impressive antiproliferative activity. Mechanistic studies revealed that 13b is able to down-regulate HSP90 and β-catenin in A549 lung adenocarcinoma cells in a dose-dependent manner, suggesting a potential use for treating hedgehog pathway-driven tumorigenesis.

原文	英語
頁（從 - 到）	6751-6761
頁數	11
期刊	Journal of Medicinal Chemistry
卷	55
發行號	15
DOIs	https://doi.org/10.1021/jm3001218
出版狀態	已發佈 - 8月 9 2012
對外發佈	是

ASJC Scopus subject areas

分子醫學
藥物發現

UN SDG

此研究成果有助於以下永續發展目標

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10.1021/jm3001218

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Yang, X., Shi, Q., Lai, C. Y., Chen, C. Y., Ohkoshi, E., Yang, S. C., Wang, C. Y., Bastow, K. F., Wu, T. S., Pan, S. L., Teng, C. M., Yang, P. C., & Lee, K. H. (2012). Antitumor agents 295. E-ring hydroxylated antofine and cryptopleurine analogues as antiproliferative agents: Design, synthesis, and mechanistic studies. Journal of Medicinal Chemistry, 55(15), 6751-6761. https://doi.org/10.1021/jm3001218

Yang, X, Shi, Q, Lai, CY, Chen, CY, Ohkoshi, E, Yang, SC, Wang, CY, Bastow, KF, Wu, TS, Pan, SL, Teng, CM, Yang, PC & Lee, KH 2012, 'Antitumor agents 295. E-ring hydroxylated antofine and cryptopleurine analogues as antiproliferative agents: Design, synthesis, and mechanistic studies', Journal of Medicinal Chemistry, 卷 55, 編號 15, 頁 6751-6761. https://doi.org/10.1021/jm3001218

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abstract = "Various E-ring hydroxylated antofine and cryptopleurine analogues were designed, synthesized, and tested against five human cancer cell lines. Interesting structure-activity relationship (SAR) correlations were found among these new compounds. The most potent compound 13b was further tested against a series of nonsmall cell lung cancer (NSCLC) cell lines in which it showed impressive antiproliferative activity. Mechanistic studies revealed that 13b is able to down-regulate HSP90 and β-catenin in A549 lung adenocarcinoma cells in a dose-dependent manner, suggesting a potential use for treating hedgehog pathway-driven tumorigenesis.",

author = "Xiaoming Yang and Qian Shi and Lai, {Chin Yu} and Chen, {Chi Yuan} and Emika Ohkoshi and Yang, {Shuenn Chen} and Wang, {Chih Ya} and Bastow, {Kenneth F.} and Wu, {Tian Shung} and Pan, {Shiow Lin} and Teng, {Che Ming} and Yang, {Pan Chyr} and Lee, {Kuo Hsiung}",

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doi = "10.1021/jm3001218",

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AU - Shi, Qian

AU - Lai, Chin Yu

AU - Chen, Chi Yuan

AU - Ohkoshi, Emika

AU - Yang, Shuenn Chen

AU - Wang, Chih Ya

AU - Bastow, Kenneth F.

AU - Wu, Tian Shung

AU - Pan, Shiow Lin

AU - Teng, Che Ming

AU - Yang, Pan Chyr

AU - Lee, Kuo Hsiung

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AB - Various E-ring hydroxylated antofine and cryptopleurine analogues were designed, synthesized, and tested against five human cancer cell lines. Interesting structure-activity relationship (SAR) correlations were found among these new compounds. The most potent compound 13b was further tested against a series of nonsmall cell lung cancer (NSCLC) cell lines in which it showed impressive antiproliferative activity. Mechanistic studies revealed that 13b is able to down-regulate HSP90 and β-catenin in A549 lung adenocarcinoma cells in a dose-dependent manner, suggesting a potential use for treating hedgehog pathway-driven tumorigenesis.

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Antitumor agents 295. E-ring hydroxylated antofine and cryptopleurine analogues as antiproliferative agents: Design, synthesis, and mechanistic studies

摘要

ASJC Scopus subject areas

UN SDG

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