PYRIMIDINE NUCLEOSIDE PHOSPHORYLASES/CANCER CHEMOTHERAPY

这项赠款建议的目标是： 1. BAU类似物和衍生物的化学合成 （5-苄氧基苄酰基尿苷）和BBAU（5-苄氧基苄酰基尿苷），强效 尿苷磷酸化酶抑制剂和抗肿瘤增效剂 FUdR的作用，旨在改善临床使用设施，以产生 新的抗肿瘤药物和前体药物，并进一步探索其生物活性， 特性. 2.这些新药物作为尿苷抑制剂的生物学试验 磷酸化酶和胸苷磷酸化酶（如有说明）作为转运蛋白 体外和体内的抑制剂、抗肿瘤剂和增效剂， 并作为获得与核酸相关的新的生物化学知识的工具， 酸代谢 这些研究将与以下机构的同事合作进行： 罗杰威廉姆斯癌症中心。

The objectives of this grant proposal are: 1. Chemical synthesis of analogs and derivatives of BAU (5-benzylacyclouridine) and BBAU (5-benzyloxybenzylacyclouridine), potent inhibitors of uridine phosphorylase and potentiators of the anti-tumor action of FUdR, designed to improve facility of clinical use, to produce new anti-tumor drugs and pro-drugs, and to explore further their biological properties. 2. Biological testing of these new agents as inhibitors of uridine phosphorylase and, where indicated, thymidine phosphorylase, as transport inhibitors, anti-tumor agents and potentiators both in vitro and in vivo, and as tools for obtaining new biochemical knowledge related to nucleic acid metabolism. These studies will be performed in collaboration with colleagues in the Roger Williams Cancer Center.