7-ethyl-10-hydroxycamptothecin derivatives, and preparation and application thereof

• Main Authors: MA JUANJUAN, GAO BAOAN, YAO JIANZHONG, YU NONG, CHEN JIANMING, ZHANG YUANSHENG, LIU WENLI, WU CHAN, DENG LI, CHEN LINA
• Format: Patent
• Language: Chinese; English
• Published: 20.07.2016
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The invention relates to the technical field of medicine. According to the invention, omega-3 unsaturated fatty acid is used for modifying the 10-site hydroxyl group of 7-ethyl-10-hydroxycamptothecin (SN-38), such that a type of novel 7-ethyl-10-hydroxycamptothecin derivatives are formed. The invention further provides a preparation method of the type of compounds, and an application thereof in preparing anti-tumor drugs. The compound provided by the invention has relatively high lipid solubility, such that medicine preparation is facilitated. The type of compounds have a targeting effect upon tumor tissues, and have good anti-tumor effects and low toxic and side effects. 本发明涉及医药技术领域。本发明通过ω-3不饱和脂肪酸对7-乙基-10-羟基喜树碱(SN-38)的10位羟基进行修饰，形成类新的7-乙基-10-羟基喜树碱的衍生物，本发明进步提供了该类化合物的制备方法以及在制备抗肿瘤药物中的应用。本发明的化合物的脂溶性较高，有利成药，该类化合物对肿瘤组织有靶向作用，抗肿瘤效果好，毒副作用低。