目的 設(shè)計合成頭孢美法侖，并對其進行體外抗腫瘤活性研究。方法 以二苯甲酮、美法侖和7-苯乙酰胺基-3-氯甲基頭孢烷酸對甲氧基芐酯（GCLE）為原料，經(jīng)酯化、碘代、偶聯(lián)、氧化、水解等反應(yīng)得到目標(biāo)化合物頭孢美法侖，并采用MTT法對其進行體外抗腫瘤活性研究。結(jié)果 設(shè)計并合成了目標(biāo)產(chǎn)物頭孢美法侖，利用MS和¹H-NMR確證了結(jié)構(gòu)；體外活性實驗中，頭孢美法侖在體外基本無毒，酶解后IC₅₀為（101.97±1.705）μmol/L。結(jié)論 頭孢美法侖酶解后能夠充分發(fā)揮細(xì)胞毒作用，而酶解前在體外基本無毒性，為頗具前景的前藥，值得進一步研究。

Objective To design and synthesize cephalosporin melphalan, and to evaluate its antitumor activity in vitro. Methods Benzophenone, melphalan, and 7-phenylacetamide-3-chloromethyl-3-cepham-4-carboxylic acid p-methyl-oxybenzyl ester (GCLE) were used as starting materials to synthesize the target compound cephalosporin melphalan by esterification, iodine, coupling, oxidation, and hydrolysis reactions. The antitumor activity in vitro was evaluated by MTT method. Results The target compound cephalosporin melphalan was synthesized and characterized by MS and ¹H-NMR. The antitumor activity experiments showed that cephalosporin melphalan was nontoxic in vitro, while after enzymolysis, the IC₅₀ value was (101.97 ± 1.705) μmol/L. Conclusion After enzymolysis, cephalosporin melphalan has the cytotoxic effect. While before enzymolysis, cephalosporin melphalan has been found to be nontoxic in vitro, which could be a valuable candidate for further development.