ANTITUMOR AND ANTIVIRAL NUCLEOSIDE ANALOGUES

描述：（改编自申请人摘要）。 新型核苷 类似物将被制备和研究作为潜在的抗病毒和抗肿瘤药物 剂. i）活性抑制剂的对映体 艾滋病病毒，腺苷二烯和cytallene。 ii）丙二烯的其它类似物 包括氟衍生物和丙二醇，iii）螺环 丙二烯的类似物，iv）炔属和烯属无环核苷 类似物和它们的膦酸酯，v）2 ′-氧杂碳环类似物， 和vi）丙二烯的三磷酸衍生物 用于研究腺苷联烯和cytalene的作用机制。 抗肿瘤 活性类似物的活性和作用机制将在 体外和体内使用小鼠白血病L 1210和许多其他肿瘤 包括实体瘤在内的系统。 抗病毒作用将在 用DNA和RNA病毒进行的几种测定，特别强调HIV。 将对适当的类似物（腺嘌呤衍生物）进行检测， 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.