磺胺劑亞硝基脲衍生物之分解度研究

Abstract

比較潛能抗癌劑N-（2-氯乙基）-N-（亞硝基）?基磺胺甲噁性[1]，N-（2-氯乙基）-N-（亞硝基）?基磺胺甲氧噠[2]，N-（2氯乙基）-N-（亞硝基）?基磺胺二甲嘧啶[3]及N-（2氯乙基）-N-（亞硝基）?基磺胺異噁唑[4]等之分解速率，固態狀況時在室溫及50℃，液態狀況在pH7.4，37℃之緩衝溶液中等三種不同狀況下測定，求時間與分解度關係。發現化合物(2)在pH7.4的緩衝溶液中之半衰期為60分與現臨床上使用之涇化劑類抗癌藥BCNU相同，因此可能有抗癌作用。

This paper attempts to study decomposition of potential anticancer agents, N- (2-chloroethyl) -N-nitrosoureido-sulfamethoxazole (1), N- (2-chloroethyl) -N-nitrosoureido-sulfamethoxypyridazine (2), N-(2-chloroethyl) -N-nitrosoureido-sulfamethazine (3), and N- (2-chloroethyl) -N-nitrosoureido-sulfisoxazole (4) at various conditions such as solid state at room temperature and 50 °C, or in buffer solution of pH 7.4 at 37 °C. Half life time of compound (2) in pH 7.4 buffer solution shows 60 min. and this value is equal to that of anticancer drug BCNU. So compound (2) might posses an anticancer effect.