Antitumor and Antiviral Nucleoside Analogues

抗肿瘤和抗病毒核苷类似物

• 批准号: 7005639
• 负责人: JIRI ZEMLICKA
• 金额: $ 20.39万
• 依托单位: WAYNE STATE UNIVERSITY
• 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 2009-04-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7005639
• 关键词: aminopurine; antineoplastics; antiviral agents; cell line; chemical structure function; cyclopropanes; cytomegalovirus; drug design /synthesis /production; enzyme linked immunosorbent assay; hepatitis B virus group; herpes simplex virus 1; herpes simplex virus 2; high performance liquid chromatography; human herpesvirus 6; human herpesvirus 8; human immunodeficiency virus; neoplasm /cancer; nucleic acid hybridization; nucleoside analog; nucleotide analog; phosphonate; prodrugs; stereoisomer; thiophosphate

DESCRIPTION (provided by applicant): New nucleoside and nucleotide analogues will be prepared and studied as antiviral and antitumor agents. These compounds will include (i) enantiomeric triphosphates and non-hydrolyzable triphosphates of methylenecyclopropanes, (ii) ethynyl methylenecyclopropanes, (iii) fluorinated analogues of gem-bis (hydroxymethyl)methylenecyclopropanes, (iv) tris-(hydroxymethy)methylenecyclopropanes and (v) cyclopropavir phosphonates, acyclic and cyclic. Antiviral activity will be investigated in the following viral assays: Human immunodeficiency virus (HIV), human and murine cytomegalovirus (HCMV and MCMV), herpes simplex virus type 1 and 2 (HSV-1 and HSV-2), human herpes virus 6 and 8 (HHV-6 and HHV-8) and hepatitis B virus (HBV). In vivo activity and mechanism of action of active analogues will also be studied. Selected compounds will also be tested for antitumor activity

描述（由申请人提供）：将准备新的核苷和核苷酸类似物作为抗病毒和抗肿瘤剂。这些化合物将包括（i）甲基苯甲酰丙烷的对映体三磷酸和非氢化三磷酸，（ii）乙基甲基甲基烯基环丙烷，（iii）荧光类似物（羟基甲基甲基）甲基果皮丙烷，（IV）的荧光类似物Tris-（羟甲）甲基苯丙烷丙烷和（V）环丙别普瓦尔磷酸盐，无环和环状。抗病毒活性将在以下病毒测定中进行研究：人类免疫缺陷病毒（HIV），人和鼠巨细胞病毒（HCMV和MCMV），单纯疱疹病毒1型和2型（HSV-1和HSV-2）（HSV-1和HSV-2），HUM HERPES病毒6和8（HHV-6和8（HHV-6和HHV-8）以及HHV-8）以及Hepatiation（HHV-6和HHV-8）和Hepatiation。还将研究活性类似物的体内活性和作用机理。选定的化合物还将测试抗肿瘤活性