ENZYME INHIBITORS AS PROTENTIAL ANTICANCER AND ANTIVIRAL DRUGS

该项目的范围是设计和综合基于机构的 对生长至关重要的酶反应的抑制剂 肿瘤细胞或病毒复制。由此产生的化合物是 拟用作治疗剂和研究探针。这个 当前感兴趣的主题如下：1)NAD的二核苷酸类似物 作为IMP脱氢酶的抑制剂，2)胞苷的酸稳定抑制剂 口服型脱氨酶，3)二氮杂环酮核苷的合成 脱氨酶抑制剂，4)磷酸酯类似物的合成 2‘，5’-寡腺苷三聚体作为干扰素产生的稳定诱导剂，5) 嘌呤核苷抑制剂嘌呤膦酸类化合物的合成 磷酸酶(PNP)，6)潜在的碳环核苷的合成 抗病毒药物。

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.