1-O-Acetyl-2-deoxy-3,5-di-O-toluoyl-4-thio-D-erythro-pentofuranose and 2-deoxy-1,3,5-tri-O-acetyl-4-thio-L-threo-pentofuranose were coupled with 5-azacytosine to obtain alpha and beta anomers of nucleosides. All four nucleosides were reduced to the corresponding dihydro derivatives and deblocked to give target compounds. All eight target compounds were evaluated in a series of human cancer cell lines
1-O-乙酰基-2-脱氧-3,5-二-O-
甲苯基-4-
硫代-D-赤型戊
呋喃糖和2-脱氧-1,3,5-三-O-乙酰基-4-
硫代-将L-苏-戊
呋喃糖与5-氮杂
胞嘧啶偶联以获得核苷的α和β异构体。将所有四个核苷还原为相应的二氢衍
生物,并解封以得到目标化合物。在培养的一系列人类癌
细胞系中评估了所有八个目标化合物。发现仅2'-脱氧-4'-
硫代-
5-氮杂胞苷(3beta)在所有
细胞系中均具有细胞毒性,并在体内进行了进一步评估。报告了合成和
生物活性的细节。