ANTITUMOR AND ANTIVIRAL NUCLEOSIDE ANALOGUES

抗肿瘤和抗病毒核苷类似物

• 批准号: 3170632
• 负责人: JIRI ZEMLICKA
• 金额: $ 26.81万
• 依托单位: BARBARA ANN KARMANOS CANCER INSTITUTE
• 依托单位国家: 美国
• 财政年份: 1984
• 资助国家: 美国
• 起止时间: 1984-07-01 至 1995-12-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3170632
• 关键词: AIDS; adenosine deaminase; antineoplastics; antiviral agents; chemical synthesis; enzyme substrate; human immunodeficiency virus; laboratory mouse; mouse leukemia; nucleoside analog; tissue /cell culture; AIDS; adenosine deaminase; antineoplastics; antiviral agents; chemical synthesis; enzyme substrate; human immunodeficiency virus; laboratory mouse; mouse leukemia; nucleoside analog; tissue /cell culture

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.

描述：（改编自申请人的摘要）。 新的核苷 类似物将作为潜在的抗病毒和抗肿瘤进行准备并研究 代理商。 这些化合物将包括：i）活性抑制剂的对映异构体 艾滋病毒，腺苷和细胞烯。 ii）Allene的其他类似物 包括氟衍生物和艾列烯二元在内的类型，iii）螺旋细胞 Allenes，IV）乙酰基因和烯烃无环核苷的类似物 类似物及其磷酸盐，v）2'-oxaCarbocyclic类似物的类似物 核苷（“异核苷”）和vi）艾伦的三磷酸衍生物 用于研究腺苷和细胞烯的作用机理。 抗肿瘤 将研究活动类似物的活动和作用机理 使用鼠白血病L 1210和许多其他肿瘤的体外和体内 包括实体瘤在内的系统。 抗病毒作用将在 具有DNA和RNA病毒的几种测定，特别强调HIV。 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。