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Synthesis and anti-cancer activity of some novel C-17 analogs of ursolic and oleanolic acids

机译:熊果酸和齐墩果酸的一些新型C-17类似物的合成和抗癌活性

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摘要

A series of seventeen novel analogs of ursolic and oleanolic acid were synthesized (60-98 %), and evaluated for their anti-cancer potential against a panel of eight human cancer cell lines. Compounds (3-10) showed comparable or better activities than their respective parent compounds against SiHa and HeLa (Cervix), A-549 (Lung), and IMR-32 (Neuroblastoma) cancer cell lines. Significantly, among the bromoalkyl esters (11-19), compound 13 showed promising anti-cancer activity against Leukemia THP-1 cell line at 10 uM concentration. In this series, it is interesting to note that the increase in chain length has an adverse effect on the activity.
机译:合成了一系列十七种新的熊果酸和齐墩果酸类似物(60-98%),并评估了它们对八种人类癌细胞系的抗癌潜力。化合物(3-10)对SiHa和HeLa(宫颈),A-549(肺)和IMR-32(神经母细胞瘤)癌细胞系显示出比其相应母体化合物相近或更好的活性。值得注意的是,在溴代烷基酯(11-19)中,化合物13在10 uM浓度下显示出对白血病THP-1细胞系的有希望的抗癌活性。在这个系列中,有趣的是,链长的增加对活性有不利影响。

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