Novel Tumor-selective Anticancer Agents

新型肿瘤选择性抗癌药物

• 批准号: 6739779
• 负责人: YUQIANG WANG
• 金额: $ 14.6万
• 依托单位: PANORAMA RESEARCH, INC.
• 依托单位国家: 美国
• 财政年份: 2004
• 资助国家: 美国
• 起止时间: 2004-03-01 至 2005-02-28
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6739779
• 关键词: adenocarcinoma; antineoplastics; camptothecin; cell line; chemical conjugate; chemical synthesis; colon neoplasms; cytotoxicity; drug design /synthesis /production; laboratory mouse; leukemia; lung neoplasms; neoplasm /cancer pharmacology; omega 3 fatty acid; pharmacokinetics

DESCRIPTION (provided by applicant): Recently, tumor cells have been found to selectively accumulate certain n-3 fatty acids such as cis-4,7,10,13,16,19-docosahexenoic acid (DHA). DHA-paclitaxel, a conjugate of DHA and paclitaxel, has a greatly increased therapeutic efficacy and reduced side effects in both experimental animals and patients compared to free paclitaxel. We have synthesized a proprietary DHA-camptothecin conjugate that showed remarkable antitumor activity in experimental animals. We have filed a provisional patent application covering this invention (US 60/401,195). The objectives of this proposal are to synthesize novel DHA camptothecin conjugates, evaluate their antitumor activity in vitro and in experimental animals. It is expected that the novel DHA conjugates will have increased antitumor efficacies and reduced toxic side effects.

描述（由申请人提供）：最近，发现肿瘤细胞有选择地积累了某些N-3脂肪酸，例如CIS-4,7,10,13,16,16,16-多核酸（DHA）。 DHA-PACLITAXEL是DHA和紫杉醇的结合物，与游离紫杉醇相比，实验动物和患者的治疗功效大大提高，并且副作用降低。我们已经合成了专有的DHA-羊皮蛋白结合物，该结合物在实验动物中表现出显着的抗肿瘤活性。我们已经提出了涵盖本发明的临时专利申请（美国60/401,195）。该提案的目标是合成新型的DHA Camptothecin结合物，在体外和实验动物中评估其抗肿瘤活性。可以预期，新型的DHA结合物将具有抗肿瘤功效和毒性副作用降低。