ANTITUMOR AND ANTIVIRAL ANALOGUES

抗肿瘤和抗病毒类似物

• 批准号: 2422377
• 负责人: JIRI ZEMLICKA
• 金额: $ 19.8万
• 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 1998-12-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/2422377
• 关键词: AIDS; adenosine deaminase; antineoplastics; antiviral agents; cytomegalovirus; drug design /synthesis /production; enzyme substrate; hepatitis B virus group; herpes simplex virus 1; human immunodeficiency virus; laboratory mouse; nucleoside analog; tissue /cell culture; AIDS; adenosine deaminase; antineoplastics; antiviral agents; cytomegalovirus; drug design /synthesis /production; enzyme substrate; hepatitis B virus group; herpes simplex virus 1; human immunodeficiency virus; laboratory mouse; nucleoside analog; tissue /cell culture

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.

描述：（改编自申请人的摘要）新的核苷和 将准备核苷酸类似物，并作为抗病毒和抗肿瘤进行研究 代理商。 这些化合物将包括（1） 源自能够穿透细胞的核酸碱的艾烯醇 膜（2）含有环丙烷或环丁烷的核苷类似物 抗HIV剂Carbovir的部分和（3）类似物。 抗肿瘤 活动将是使用鼠白血病L1210在体外和体内研究 培养物和许多其他肿瘤系统，包括实体瘤。 将在人类的测定中研究抗病毒作用 免疫缺陷病毒（HIV），丙型肝炎病毒（HBV），人 巨细胞病毒（HCMV）和单纯疱疹1病毒（HSV-1）。 机制 将使用主动类似物研究动作。 腺嘌呤将进行测试 作为腺苷脱氨酶的底物。