Incorporation of carbobenzoxy-glycylprolyl (Z-GP) to either α or β position of the hydrazine moiety in procarbazine (Pcb) has been carried on in 5-steps process. The overall yield was 32.7%. The new entity Z-GP-Pcb was confirmed targeting to fibroblast activation protein-α (FAPα). Z-GP-Pcb may be hydrolyzed by either isolated rhFAPα or tumor homogenate. It was shown far less cytotoxicity against NCI-H460 cell line than Pcb. Z-GP-Pcb was displayed the potency to reduce spermatoxcity in H22-bearing mice. The mechanism may be ascribed to the blockade of dehydrogenation by α-glycerolphosphate dehydrogenase. This candidate was further proved equal antitumor activity to Pcb. However, the introduction of Z-GP scaffold decreased myelosuppression. All the evidences support that Z-GP-Pcb is a better antitumor agent than Pcb.

将碳苯甲酰-甘氨酰脯氨酰（Z-GP）掺入到丙咔嗪（Pcb）中肼部分的α或β位置已经进行了5步。总产率为32.7％。证实了新实体Z-GP-Pcb靶向成纤维细胞活化蛋白-α（FAPα）。Z-GP-Pcb可以被分离的rhFAPα或肿瘤匀浆水解。已显示出对NCI-H460细胞系的细胞毒性远小于Pcb。Z-GP-Pcb在具有H22的小鼠中显示出降低精子能力的能力。该机制可以归因于α-甘油磷酸脱氢酶对脱氢的阻断。进一步证明了该候选物与Pcb具有相同的抗肿瘤活性。然而，Z-GP支架的引入降低了骨髓抑制。所有证据支持Z-GP-Pcb是比Pcb更好的抗肿瘤药。