ON ANTITUMOR ACTIVITY OF A NOVEL COMPOUND – A PYRIDINE DERIVATIVE

Abstract

The work studied the antitumor activity of a new compound, a pyridine derivative LHT-13-19. To determine the effective inhibitory concentration, a culture of human colon cancer HCT116 was used. Incubation of tumor cells was carried out in the presence of LHT-13-19 in the concentration range from 10-9 to 10-7 M. The survival of tumor cells was determined in MTT test. In vivo experiments were performed on thirty athymic humanized 12-week-old female BALB/c nu/nu mice with xenograft colorectal adenocarcinoma. All animals were divided into 3 groups, 10 mice in each: animals of the control group were injected daily intraperitoneally with 0.5 ml of PBS, animals of the second group were treated with a cyclophosphamide at a dose of 10 mg/kg, mice of the third the groups received LHT-13-19 as experimental therapy at a daily dose of 3.7 mg/kg during 10 days. Animals’ survival and antitumor activity were assessed. Tumor-doubling time, the number of liver superficial metastases and survival time were estimated. Daily incubation of human colon tumor cells with LHT-13-19 is accompanied by the formation of the cytotoxic effect of the compound. On a xenograft model of colon adenocarcinoma in humanized BALB/c nu/nu mice, a 10-day course of 3.7 mg/kg LHT-13-19 leads to the formation of an antitumor effect due to increase in the time of tumor doubling, animal survival and a decrease in the frequency of metastasis