Antitumor and Antiviral Nucleoside Analogues

说明(申请人提供)：新的核苷和核苷酸类似物将作为抗病毒和抗肿瘤药物进行制备和研究。这些化合物将包括(I)对映体三磷酸盐和亚甲基环丙烷的非水解性三磷酸盐，(Ii)乙炔基亚甲基环丙烷，(Iii)GEM-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)环丙韦磷酸盐，无环和环状。抗病毒活性将在以下病毒检测中进行：人类免疫缺陷病毒(HIV)、人和小鼠巨细胞病毒(HCMV和MCMV)、1型和2型单纯疱疹病毒(HSV-1和HSV-2)、人类疱疹病毒6和8型(HHV-6和HHV-8)以及乙肝病毒(乙肝)。活性类似物的体内活性和作用机制也将被研究。选定的化合物也将进行抗肿瘤活性测试。

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