2-取代亚胺基-3-[N-(2-氯乙基)]氨甲酰四氢噻唑的合成及其抗肿瘤活性研究

SYNTHESIS AND ANTITUMOR ACTIVITY OF 2-SUBSTITUTEDIMNO-3-[N-(2-CHLOROETHYL)]CARBAMOYLTHIAZOLINES

本文通过2-氯乙基异氰酸酯与各种N-取代-2-氨基-2-噻唑啉反应合成了十三个未见文献报道的2-取代亚胺基-3-[N-(2-氯乙基)]氨甲酰四氢噻唑化合物,其结构均经~1HNMR,IR、MS等得到证实。初步药效表明:2-苄基亚胺基-3-(N-(2-氯乙基)]氨甲酰四氢噻唑(2)对小白鼠爱氏腹水癌(EAC)有较高的抑制率(60.5％)。

Thirteen 2-substitutedimno-3-[N-(2-chloroethyl)]carbamoylthiazolines were synthesized by the reaction of N-substituted-2-amino-2-thiazoline with 2-chloroethylisocyanate in dioxane at ambient tempreture(20℃).All the unknown compounds synthesized were confirmed through IR, ~1H-NMR and MS.These compounds(1～2)were synthesized in another way, although the reaction steps were more,the yield was higher. Preliminary screening revealed that 2-benylimno-3-[N-(2-chloroethyl)] carbamoylthiazoline exhibited marked inhibitory activity against Ehrlich Ascites Carcinoma(EAC)in mice,the inhibition ratio is 60.5% at the dosage of 0.35mg/kg.