含1,3,4-噻二唑的5-氟尿嘧啶衍生物的合成及其抗肿瘤活性

OBJECTIVE To synthesize N1-acetylamino-(5-alkyl/aryl-1, 3, 4-thia-diazole-2-yl)-5-fluorouracil derivatives which has less toxicities and higher antitumor activities. METHODS The target compounds were sythesized from the reactions of 5-fluorouracil and chloroacetic acid in the existence of potassium hydroxide, then coupled with 2-amino-5-alkyl/aryl-1, 3, 4-thiadiazole. Their bioactivities were evaluated. RESULTS and CONCLUSION Seven novel target compounds 3 a-3 g were synthesized which had been confirmed by IR, 1HNMR and HRMS. 3 d, 3 f and 3 g could strongly inhibit the proliferation of tumor cells in vitro.