Paull K D, Zee-Cheng R K, Cheng C C
J Med Chem. 1976 Feb;19(2):337-9. doi: 10.1021/jm00224a029.
Some 2,3-bis(substituted methyl)naphthazarins and related compounds were synthesized by the Diels-Alder reaction of benzoquinone and 2,3-dimethylbutadiene followed by oxidation and substitution reactions. These compounds were prepared as potential biological alkylating agents. Screening results indicated that 1,4-diacetyl-6,7-dimethyl-4a,5,8,8a-tetrahydronaphthalene and 5,8-bis(benzoyloxy)-2,3-dimethyl-1,4-naphthoquinone possessed borderline activity against leukemia P388 and that naphthazarin diacetate possessed confirmed cytotoxicity against the cell culture of human epidermoid carcinoma of the nasopharynx.
通过苯醌与2,3 - 二甲基丁二烯的狄尔斯 - 阿尔德反应，随后进行氧化和取代反应，合成了一些2,3 - 双（取代甲基）萘并azarins及其相关化合物。这些化合物被制备为潜在的生物烷基化剂。筛选结果表明，1,4 - 二乙酰基 - 6,7 - 二甲基 - 4a,5,8,8a - 四氢萘和5,8 - 双（苯甲酰氧基） - 2,3 - 二甲基 - 1,4 - 萘醌对白血病P388具有临界活性，而萘并azarin二乙酸酯对人鼻咽癌表皮样癌细胞培养物具有确定的细胞毒性。
