engleski

Antitumor activity of novel N-sulfonylpyrimidine derivatives on the growth of anaplastic mammary carcinoma in vivo

The aim of the present study was to investigate in vivo antitumor activity of newly synthesized N-sulfonylpyrimidine derivatives. Antitumor activity was examined for 1-(p-toluenesulfonyl)cytosine (4H), 1-(p-toluenesulfonyl)cytosine hydrochloride (4HxHCl), and zinc(II) complex of 1-(p-toluenesulfonyl)cytosine (4K). The model for investigation of antitumor activity was a mouse anaplastic mammary carcinoma transplanted into the thigh of the right hind leg of CBA mice. Antitumor effect of these compounds depends on drug doses, time interval between tumor transplantation and drug application. Further on the efficacy of these compounds depends on number of drug injection, i. e. if drug was given in single or in multiple doses. Multiple dose of 400 mg/kg of 1-(p-toluenesulfonyl)cytosine showed good antitumor effect when applied on day 1, 3, 5, 7 and 9 after tumor transplantation. Still good but little less antitumor effect was also achieved when that compound was given in single dose (1200 mg/kg) on day one after tumor transplantation. The longest period of tumor growth time was obtained after application of 1-(p-toluenesulfonyl)cytosine hydrochloride given as a single dose (300 mg/kg) on day one or on day six after tumor implantation. But anitumor effect of zinc(II) complex of 1-(p-toluenesulfonyl)cytosine was very strong when 300 mg/kg was given on day 1 or day 6 and this effect was little less when drug (200 mg/kg/inj) was given on day 1, 3, 5, 7 and 9 or on day 6, 8, 10, 12 and 14.

N-1-sulfonylcytosine derivatives; mice; anaplastic mammary carcinoma; antitumor activity

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