Mathew A E, Zee-Cheng R K, Cheng C C
J Med Chem. 1986 Sep;29(9):1792-5. doi: 10.1021/jm00159a041.
Based on the observation of outstanding antineoplastic activity of a number of amino-substituted anthraquinones, thioxanthones, and N-(aminoethyl)-substituted naphthalimides, four types of amino-substituted p-benzoquinones were designed, synthesized, and their biological activity evaluated. Although none of these compounds exhibited inhibitory activity against P388 leukemia, 2,5-bis[[4-[(dimethylamino)methyl]phenyl]amino]-3,6-dibromo-1,4- benzoquinone and the corresponding dichloro compound demonstrated good inhibitory activity against the proliferating human colon adenocarcinoma in vitro. The dichloro compound was also found to be active against the leukemia L1210 screening in vitro. 2,5-Bis[[2-(dimethylamino)ethyl]amino]-1,4-benzoquinone possessed inhibitory activity against Neisseria catarrhali.
基于对多种氨基取代蒽醌、噻吨酮和N-（氨基乙基）取代萘二甲酰亚胺显著抗肿瘤活性的观察，设计、合成了四种氨基取代对苯醌，并对其生物活性进行了评估。尽管这些化合物均未表现出对P388白血病的抑制活性，但2,5-双[[4-[(二甲氨基)甲基]苯基]氨基]-3,6-二溴-1,4-苯醌及相应的二氯化合物在体外对人结肠腺癌增殖显示出良好的抑制活性。还发现该二氯化合物在体外对白血病L1210筛选有活性。2,5-双[[2-(二甲氨基)乙基]氨基]-1,4-苯醌对卡他莫拉菌具有抑制活性。
