ANTITUMOR ACTIVITY OF DL-1-β-CHLOROETHYL-2-CHLOROMETHYLPIPERIDINE HYDROBROMIDE (CAP-1) ON SOME RODENT TUMORS^∗

Abstract

The antitumor activity of some 1, 2-bis(chloroalkyl)piperidine derivatives on Ehrlich ascites carcinoma cells was examined employing the in vitro-in vivo test method. The same compounds which have chloromethyl group in 2-position of the piperidine nucleus showed positive results. Among them, DL-1-β-chloroethyl-2chloromethylpiperidine hydrobromide (CAP-1) was found to be most effective in inhibiting the growth of tumor cells. Thus, CAP-1 was further investigated for the in vivo antitumor effect against certain rodent tumors. CAP-1 showed a remarkable prolongation of the survival time of mice bearing Ehrlich ascites carcinoma or sarcoma 180 when administrated i.p. a dose of 2-1 mg/kg/day for 7 consecutive days. This compound was also effective in inhibiting the growth of solid type of Ehrlich carcinoma. It has been observed that the average survival time of mice bearing mouse leukemia L1210 increased with i.p. administration of CAP-1 in doses ranging from 0.5 to 2 mg/kg/day for 7 days. CAP-1 was effective in prolonging the life-span of rats bearing Yoshida sarcoma or ascites hepatoma AH13 when given i.p. at a dose of 0.5-0.0625 mg/kg/day for 7 days.