Anderson W K, Dewey R H
J Med Chem. 1977 Feb;20(2):306-8. doi: 10.1021/jm00212a025.
Dimethyl exo-5,6-oxido-7-oxabicyclo[2.2.1]hept-2-ene-2,3-dicarboxylate (1) and the 1-methyl homologue 2 were shown to exhibit significant cytotoxicity in the 9KB tissue culture assay. Several analogues of 1 were prepared and it was found that removal of the epoxide, or the oxygen bridge, or the 2,3 double bond from 1 resulted in loss of significant cytotoxic activity. One compound which lacked the epoxide moiety, dimethyl 1-methyl-7-oxabicyclo[2.2.1]hepta-2,5-diene-2,3-dicarboxylate (5), also exhibited marginal cytotoxic activity.
外-5,6-环氧-7-氧杂双环[2.2.1]庚-2-烯-2,3-二甲酸二甲酯（1）及其1-甲基同系物2在9KB组织培养试验中显示出显著的细胞毒性。制备了1的几种类似物，发现从1中去除环氧化物、氧桥或2,3-双键会导致显著的细胞毒性活性丧失。一种缺乏环氧化物部分的化合物，1-甲基-7-氧杂双环[2.2.1]庚-2,5-二烯-2,3-二甲酸二甲酯（5），也表现出轻微的细胞毒性活性。
