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Antitumor Agents 295. E-ring Hydroxylated Antofine And Cryptopleurine Analogues As Antiproliferative Agents: Design, Synthesis, And Mechanistic Studies.
X. Yang, Q. Shi, Chin-Yu Lai, C. Chen, E. Ohkoshi, S. Yang, Chih-Ya Wang, K. Bastow, Tian-Shung Wu, Shiow-Lin Pan, Che-Ming Teng, P. Yang, K. Lee
Published 2012 · Chemistry, Medicine
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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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