ANTITUMOR AND ANTIVIRAL ANALOGUES

描述：(改编自申请人摘要)新核苷和 将制备核苷酸类似物，并研究其抗病毒和抗肿瘤作用 探员们。这些化合物将包括(1)亲脂性的磷酸盐 源自能够穿透细胞的核酸碱基的烯丙醇 膜(2)含环丙烷或环丁烷的核苷类似物 部分和(3)抗HIV试剂卡维韦的类似物。抗肿瘤 将利用小鼠白血病L1210进行体外和体内活性研究 培养物和许多其他肿瘤系统，包括实体瘤。 抗病毒作用将在人体试验中进行研究。 免疫缺陷病毒(HIV)、乙肝病毒(HBV)、人类 巨细胞病毒(HCMV)和单纯疱疹病毒1型(HSV-1)。机制： 活性类似物的作用将被研究。将对腺嘌呤进行测试 作为腺苷脱氨酶的底物。

DESCRIPTION: (adapted from Applicant's Abstract) New nucleoside and nucleotide analogs will be prepared and studies as antiviral and antitumor agents. These compounds will include (1) lipophilic phosphates of allenols derived from nucleic acid bases capable of penetrating the cell membrane (2) nucleoside analogues containing cyclopropane or cyclobutane moiety and (3) analogues of the anti-HIV agent carbovir. Antitumor activity will be studies in vitro and in vivo using murine leukemia L1210 cultures and a number of other tumor systems including solid tumors. Antiviral effects will be investigated in assays with human immunodeficiency virus (HIV), hepatitis B virus (HBV), human cytomegalovirus (HCMV), and herpes simplex 1 virus (HSV-1). Mechanisms of action will be studied with the active analogues. Adenine will be tested as substrates for adenosine deaminase.