西柏三烯-4,6-二醇衍生物的合成及抗肿瘤活性

CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE(2020)

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Abstract
以烟草中含量丰富的大环二萜类化合物2,7,11-西柏三烯-4,6-二醇(CBT)为母体,其C6位羟基经酯化/醚化,合成了28个西柏三烯-4-醇-6-羧酸酯及西柏三烯-4-醇-6-烷氧类化合物.采用核磁共振波谱(NMR)和高分辨质谱(HRMS)对目标化合物进行了结构表征,并初步评价了其生物活性.细胞毒活性测试结果表明,部分化合物对肿瘤细胞的抑制作用与阳性对照顺铂相当,其中α-2,7,11-西柏三烯-4-醇-6-O-苯乙酸酯(1i)对乳腺癌细胞株MCF-7的IC50值为15.45μmol/L,α-2,7,11-西柏三烯-4-醇-6-O-(2-氟)苯乙酸酯(1t)对肺癌细胞株SMMC-7721的IC50值为11.44μmol/L.
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Key words
Cembratriene derivative,Antitumor,Tobacco
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