药物作用机理的生物活化概念,正引起人们的重视,其重要意义在于它有助于人们判断药物分子中起活性作用的主要结构特征,从而指导合成具有生物活性的化合物。在生物活化领域中,生物还原烷化剂特别引人注目,这类化合物在体内可还原成强烷化剂,其中有些化合物具有显著的抗肿瘤活性。本文扼要综述了生物还原烷化剂,指 The concept of biological activation of the mechanism of action of drugs is attracting people’s attention. The significance of this concept is that it helps people to judge the main structural features that play an active role in the drug molecule, and thus guide the synthesis of bioactive compounds. Bioreductive alkylating agents are particularly attractive in the field of bioactivation, and these compounds can be reduced in vivo to their strong alkylating agents, some of which have significant antitumor activity. This article briefly reviewed biologically reduced alkylating agents, referring to