ANTITUMOR AND ANTIVIRAL NUCLEOSIDE ANALOGS

描述：(改编自申请人摘要)。新核苷 类似物将作为潜在的抗病毒和抗肿瘤药物进行制备和研究 探员们。这些化合物将包括：i)活性抑制剂的对映体 艾滋病毒，腺烯和胞烯。二)丙二烯的附加类似物 类型包括氟衍生物和烯二醇，III)螺环 烯烃的类似物，IV)乙炔和烯烃类无环核苷 类似物及其磷酸盐，v)2‘-氧碳环类似物 核苷(“异核苷”)和联烯的三磷酸衍生物 用于研究腺烯和胞烯的作用机理。抗肿瘤 活性类似物的活性和作用机理将在 用小鼠白血病L 1210等多个肿瘤进行体外和体内实验 包括实体瘤在内的系统。抗病毒效果将在#年进行研究 对DNA和RNA病毒的几种检测，特别强调艾滋病毒。 适当的类似物(腺嘌呤衍生物)将被测试为 腺苷脱氨酶的底物。

DESCRIPTION: ( Adapted from Applicant's Abstract). New nucleoside analogues will be prepared and studied as potential antiviral and antitumor agents. These compounds will include: i) Enantiomers of active inhibitors of HIV, adenallene and cytallene. ii) Additional analogues of an allene type including fluoro derivatives and allenediols, iii) spirocyclic analogues of allenes, iv) acetylenic and olefinic acyclic nucleoside analogues and their phosphonates, v) 2'-oxacarbocyclic analogues of nucleosides ("isonucleosides") and vi) triphosphate derivatives of allenes for studies of mechanisms of action of adenallene and cytallene. Antitumor activity and mechanism of action of the active analogues will be studied in vitro and in vivo using murine leukemia L 1210 and a number of other tumor systems including solid tumors. Antiviral effects will be investigated in several assays with DNA and RNA viruses with a particular emphasis on HIV. The appropriate analogues (adenine derivatives) will be tested as substrates for adenosine deaminase.