Synthesis of cephalotaxine esters and correlation of their structures with antitumor activity

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Abstract
Twenty-two new esters of natural (-)-cephalotaxine with synthetic acids possessing widely divergent structural features were synthesized. Murine antitumor (P388 [leukemia] system) test data reveal that the methyl itaconate and trichloroethyl carbonate 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 and the trichloroethyl carbonate of cephalotaxyl-L-mandelate. The specificity of this experimental tumor system apparently requires esters of (-)-cephalotaxine for tumor inhibition because methyl cephalotaxylitaconate prepared from the synthetic (+) enantiomer of cephalotaxine is inactive.

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