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Antitumor and Antiviral Nucleoside Analogues

Antitumor and Antiviral Nucleoside Analogues
抗肿瘤和抗病毒核苷类似物
批准号:
7069997
负责人:
JIRI ZEMLICKA
金额:
$19.91万
依托单位:
依托单位国家:
美国
项目类别:
财政年份:
1984
资助国家:
美国
项目状态:
已结题
起止时间:
1984-07-01 至 2009-04-30

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中文摘要
翻译
描述(由申请人提供):将制备和研究新的核苷和核苷酸类似物作为抗病毒和抗肿瘤药物。这些化合物将包括(i)亚甲基环丙烷的对映体三磷酸盐和不可水解的三磷酸盐,(ii)乙基亚甲基环丙烷,(iii)双(羟甲基)亚甲基环丙烷的氟化类似物,(iv)三(羟甲基)亚甲基环丙烷和(v)环丙帕韦磷酸盐,无环和环。抗病毒活性将在以下病毒检测中进行调查:人类免疫缺陷病毒(HIV)、人类和小鼠巨细胞病毒(HCMV和MCMV)、单纯疱疹病毒1型和2型(HSV-1和HSV-2)、人类疱疹病毒6和8型(HHV-6和HHV-8)和乙型肝炎病毒(HBV)。活性类似物的体内活性和作用机制也将被研究。选定的化合物还将测试其抗肿瘤活性
英文摘要
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
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METHYLENECYCLOPROPANE ANALOGS AND PRODRUGS FOR HCMV
METHYLENECYCLOPROPANE ANALOGS AND PRODRUGS FOR HCMV
METHYLENECYCLOPROPANE ANALOGS AND PRODRUGS FOR HCMV
METHYLENECYCLOPROPANE ANALOGS AND PRODRUGS FOR HCMV
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