烯丙基酯作为潜在的抗肿瘤药物。2,3-双（羟甲基）-7-氧杂双环[2.2.1]庚-2-烯的衍生物和类似物。
Allylic esters as potential antitumor agents. Derivatives and analogues of 2,3-bis(hydroxymethyl)-7-oxabicyclo[2.2.1]hept-2-ene.
作者信息
Anderson W K, Dewey R H, Mulumba B
出版信息
J Med Chem. 1979 Oct;22(10):1270-2. doi: 10.1021/jm00196a024.
PMID:513076
Abstract
Derivatives and analogues of 2,3-bis(hydroxymethyl)-7-oxabicyclo[2.2.1]hept-2-ene were synthesized. Of the compounds prepared, dimethyl 2,3-bis(acetoxymethyl)-7-oxabicyclo[2.2.1]hepta-2,5-diene-5,6-dicarboxylate (5) was the most potent in a leukemia L1210 tissue culture assay (93% inhibition at 10(-6) M). None of the compounds showed significant reproducible in vivo antileukemic activity.
摘要
合成了2,3-双（羟甲基）-7-氧杂双环[2.2.1]庚-2-烯的衍生物及类似物。在所制备的化合物中，2,3-双（乙酰氧基甲基）-7-氧杂双环[2.2.1]庚-2,5-二烯-5,6-二甲酸二甲酯（5）在白血病L1210组织培养试验中活性最强（在10⁻⁶ M时抑制率为93%）。这些化合物均未显示出显著且可重复的体内抗白血病活性。
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