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

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

23 Citations (Scopus)

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.

Original language	English
Pages (from-to)	6751-6761
Number of pages	11
Journal	Journal of Medicinal Chemistry
Volume	55
Issue number	15
DOIs	https://doi.org/10.1021/jm3001218
Publication status	Published - Aug 9 2012
Externally published	Yes

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

UN SDGs

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

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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, vol. 55, no. 15, pp. 6751-6761. https://doi.org/10.1021/jm3001218

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

Abstract

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