ENZYME INHIBITORS AS PROTENTIAL ANTICANCER AND ANTIVIRAL DRUGS

本项目的范围是设计和合成基于机制的 酶促反应的抑制剂，这是关键的生长 肿瘤细胞或病毒复制。 所得化合物 预期用作治疗剂和研究探针。 的 以下是当前感兴趣的主题：1）NAD的二核苷酸类似物 作为IMP脱氢酶的抑制剂，2）胞苷的酸稳定性抑制剂 用于口服的脱氨酶，3）二氮杂卓酮核苷的合成， dCMP脱氨酶抑制剂，4）DCMP脱氨酶抑制剂的膦酸酯类似物的合成 作为干扰素产生的稳定诱导剂的2 ′，5 ′-寡腺苷酸三聚体，5） 嘌呤核苷抑制剂嘌呤膦酸酯的合成 磷酸化酶（PNP），6）作为潜在的碳环核苷的合成 抗病毒剂。

The scope of this project is to design and synthesize mechanism-based inhibitors of enzymatic reactions that are critical for the growth of neoplastic cells or viral replication. The resulting compounds are intended to be used as therapeutic agents and research probes. The following topics are of current interest: 1) Dinucleotide analogues of NAD as inhibitors of IMP dehydrogenase, 2) Acid-stable inhibitors of cytidine deaminase intended for oral use, 3) Synthesis of diazepinone nucleosides as dCMP deaminase inhibitors, 4) Synthesis of phosphonate analogues of the 2',5'-oligoadenylate trimer as stable inducers of interferon production, 5) Synthesis of purine phosphonates as inhibitors of purine nucleoside phosphorylase (PNP), 6) Synthesis of carbocyclic nucleosides as potential anti-viral agents.