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b-双(β-氯乙基)氨甲基苯丙氨酸双盐酸盐(1,AT-581,邻脂苯芥)对多种动物肿瘤及临床均有效,但毒性较大.氮芥类的毒性与氮芥基中氯原子的化学活性有一定关系.一般说来,化学活性愈高,毒性愈大.鉴于AT-581苯环的5-硝基衍生物(2,AT-1258,消瘤芥)具有更明显的抗癌作用,毒性亦较低;又鉴于苄胺氮芥的对位甲氧基衍生物(3,Pyroxylon)具有更好的抗癌作用,作者将AT-1258苯环上的吸电性硝基用推电性的甲氧基取代,合成了化合物4,以研究此类化合物的化学结构与抗癌活性和毒性间的关系.同时,亦合成了化合物3的甲基衍生物5.
b-bis (β-chloroethyl) aminomethylphenylalanine dihydrochloride (1, AT-581, olanipine) is effective on a variety of animal tumors and clinically but is more toxic Cytotoxicity is related to the chemical activity of chlorine atom in nitrogen mustard.In general, the higher the chemical activity, the greater the toxicity.Taking into account the 5-nitro derivatives of AT-581 benzene ring (AT-1258, The tumor suppressor mustard) has a more obvious anti-cancer effect, and the toxicity is also lower. In addition, due to the better anticancer effect of the para-methoxy derivative (3, Pyroxylon) of benzylamine and nitrogen mustard, The electronegative nitro group on the ring was replaced by a potent methoxyl group to synthesize the compound 4 to study the relationship between the chemical structure of the compound and its anticancer activity and toxicity.At the same time, Derivatives 5.