https://scholars.lib.ntu.edu.tw/handle/123456789/626959
標題: | Antitumor agents 295. E-ring hydroxylated antofine and cryptopleurine analogues as antiproliferative agents: design, synthesis, and mechanistic studies | 作者: | Yang, Xiaoming Shi, Qian Lai, Chin-Yu Chen, Chi-Yuan Ohkoshi, Emika Yang, Shuenn-Chen Wang, Chih-Ya Bastow, Kenneth F Wu, Tian-Shung Pan, Shiow-Lin CHE-MING TENG PAN-CHYR YANG Lee, Kuo-Hsiung |
關鍵字: | PHENANTHROINDOLIZIDINE ALKALOIDS PERGULARININE; PHENANTHROQUINOLIZIDINE ALKALOIDS; THYMIDYLATE SYNTHASE; BIOLOGICAL-ACTIVITY; ANTICANCER AGENTS; CELL-GROWTH; TYLOPHORINIDINE; INHIBITION; PROTEIN; TYLOCREBRINE | 公開日期: | 9-八月-2012 | 出版社: | AMER CHEMICAL SOC | 卷: | 55 | 期: | 15 | 起(迄)頁: | 6751 | 來源出版物: | Journal of medicinal chemistry | 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. |
URI: | https://scholars.lib.ntu.edu.tw/handle/123456789/626959 | ISSN: | 0022-2623 | DOI: | 10.1021/jm3001218 |
顯示於: | 醫學系 |
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