Miura S, Yoshimura Y, Endo M, Machida H, Matsuda A, Tanaka M, Sasaki T
Biochemicals Division, Yamasa Corporation, Chiba, Japan.
Cancer Lett. 1998 Jul 3;129(1):103-10. doi: 10.1016/s0304-3835(98)00089-5.
The antitumor activity of a novel 4'-thionucleoside, 1-(2-deoxy-2-fluoro-4-thio-beta-D-arabinofuranosyl)cytosine (4'-thio-FAC), was evaluated. 4'-Thio-FAC inhibited the in vitro growth of various human cancer cell lines, particularly the growth of cell lines established from gastric and colorectal carcinomas, while its oxy-type congener 1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)cytosine (FAC) showed little or no activity against such solid cancer cell lines. 4'-Thio-FAC showed a remarkable antitumor effect against human tumors subcutaneously implanted into nude mice and was highly effective even by oral administration. 4'-Thio-FAC was less susceptible to deamination by cytidine deaminase than FAC and 2'-deoxy-2',2'-difluorocytidine (gemcitabine) and therefore is a promising drug candidate for cancer chemotherapy.
评估了一种新型4'-硫代核苷1-(2-脱氧-2-氟-4-硫代-β-D-阿拉伯呋喃糖基)胞嘧啶（4'-硫代-FAC）的抗肿瘤活性。4'-硫代-FAC抑制了多种人类癌细胞系的体外生长，尤其是源自胃癌和结直肠癌的细胞系的生长，而其氧型类似物1-(2-脱氧-2-氟-β-D-阿拉伯呋喃糖基)胞嘧啶（FAC）对这类实体癌细胞系几乎没有活性。4'-硫代-FAC对皮下植入裸鼠的人类肿瘤显示出显著的抗肿瘤作用，甚至口服给药也非常有效。4'-硫代-FAC比FAC和2'-脱氧-2',2'-二氟胞嘧啶（吉西他滨）更不易被胞苷脱氨酶脱氨，因此是一种有前景的癌症化疗候选药物。
