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OALib Journal期刊
ISSN: 2333-9721
费用：99美元
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18β-甘草次酸类衍生物的设计、合成及抑制肿瘤细胞增殖活性
, PP. 1263-1271
Keywords: 18β-甘草次酸,天然产物改造,肿瘤治疗,生长抑制
Abstract:
以18β-甘草次酸为先导化合物,考察18β-甘草次酸中c环双键位置对抗肿瘤活性的影响,设计一系列含9(11)-烯结构的衍生物,以期提高该类化合物的抗肿瘤作用。合成了23个未见文献报道的化合物,结构均经ir、lc-ms和1hnmr确证。以18β-甘草次酸为阳性对照,采用mtt法考察了24个目标化合物对人前列腺癌细胞pc-3的生长抑制活性,并采用细胞计数法测定了12个化合物对人急性早幼粒白细胞hl-60的生长抑制作用。活性结果表明,部分目标化合物的生长抑制活性优于母体,尤以化合物14的活性最强,对pc-3细胞及hl-60细胞的gi50分别为4.48μmol·l-1和1.2μmol·l-1,值得深入研究。
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