Yamato M, Hashigaki K, Sakai J, Takeuchi Y, Tsukagoshi S, Tashiro T, Tsuruo T
J Med Chem. 1987 Jul;30(7):1245-8. doi: 10.1021/jm00390a022.
As part of a study on the structure-activity relationship of antitumor-active tropolone derivatives, a series of bistropone analogues, related to potently active bistropolone 1a, were synthesized and tested for their antitumor activity in in vitro (KB cell) and in vivo (leukemia P388 in mice) systems. The methoxytropones 3 and 5, hydroxytropothione 10, and (N-methylamino)tropones 12 and 13 were inactive in both systems. Methoxytropone 6 exhibited weak activity, whose potency was equal to that of monotropolone 2a.
作为一项关于抗肿瘤活性托酚酮衍生物构效关系研究的一部分，合成了一系列与强效活性双托酚酮1a相关的双托酚酮类似物，并在体外（KB细胞）和体内（小鼠白血病P388）系统中测试了它们的抗肿瘤活性。甲氧基托酚酮3和5、羟基硫代托酚酮10以及（N-甲基氨基）托酚酮12和13在这两个系统中均无活性。甲氧基托酚酮6表现出较弱的活性，其效力与单托酚酮2a相当。
