Mikolajczak K L, Smith C R, weisleder D
J Med Chem. 1977 Mar;20(3):328-32. doi: 10.1021/jm00213a002.
Twenty-two new esters of natural (-)-cephalotaxine with synthetic acids possessing widely divergent structural features have been synthesized. Murinichloroethyl carbonate (27) esters of cephalotaxine are the most active of this group; this activity is less than that of harringtonine and other naturally occurring cephalotaxine esters. Other synthetic esters exhibiting activity are methyl cephalotaxylfumarate (4) and the trichloroethyl carbonate of cephalotaxyl-L-mandelate (21). The specificity of this experimental tumor system apparently requires esters of (-)-cephalotaxine for tumor inhibition because methyl cephalotaxylitaconate (7b) prepared from the synthetic (+) enantiomer of cephalotaxine is inactive.
已经合成了二十二种天然（-）-三尖杉碱与具有广泛不同结构特征的合成酸的新酯。三尖杉碱的鼠氯乙基碳酸酯（27）酯是该组中活性最高的；该活性低于高三尖杉酯碱和其他天然存在的三尖杉碱酯。其他表现出活性的合成酯是三尖杉酯富马酸甲酯（4）和三尖杉酯-L-扁桃酸的三氯乙基碳酸酯（21）。该实验肿瘤系统的特异性显然需要（-）-三尖杉碱的酯来抑制肿瘤，因为由三尖杉碱的合成（+）对映体制备的三尖杉酯衣康酸甲酯（7b）没有活性。
