PYRIMIDINE NUCLEOSIDE PHOSPHORYLASES/CANCER CHEMOTHERAPY

这项赠款提案的目标是： 1.BAU类似物及其衍生物的化学合成 (5-苄基酰基)和BBAU(5-苄氧基苄基)，有效 尿苷磷酸化酶抑制剂和抗肿瘤增强剂 FUDR的作用，旨在提高临床使用的便利性，以生产 新的抗肿瘤药物和促癌药物，并进一步探讨其生物学意义 属性。 2.这些新药物作为尿苷抑制剂的生物测试 磷酸化酶和胸苷磷酸化酶(如有指示)，作为转运体 体外和体内的抑制剂、抗肿瘤药物和增效剂， 作为获得与核有关的新的生物化学知识的工具 酸代谢。 这些研究将与 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.