新型胞苷衍生物二聚体及其应用

• Format: Patent
• Language: Chinese
• Published: 01.03.2019
• Subjects: CHEMISTRY; DERIVATIVES THEREOF; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; NUCLEIC ACIDS; NUCLEOSIDES; NUCLEOTIDES; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; SUGARS

本发明公开了种新型胞苷衍生物二聚体及其应用，具有下述通式(Ⅰ)：本发明通过对胞苷化合物进行分子优化设计，制备的新型的胞苷衍生物二聚体对人结肠癌HCT-116肿瘤细胞有明显的抑制作用，同时对荷瘤裸小鼠人结肠癌HCT-116移植瘤具有强烈的生长抑制作用；本发明的新型胞苷衍生物二聚体化合物的抗肿瘤活性非常高，同时化合物的毒性很低。 The present disclosure provides cytidine derivative dimers, salts and compositions of the cytidine derivative dimers, and methods of making and using the cytidine derivative dimers that are useful for treating a neoplasm in mammalian subjects. A cytidine derivative dimer may have the following general formula (I): By molecularly designing such cytidine-based compounds, the disclosed cytidine-based derivative dimers/salts show significant inhibiting effects on HCT-116 human colon cancer cells, and exhibit strong growth inhibiting effects on HCT-116 human colon cancer xenografts grown in nude mice. The disclosed cytidine derivative dimers/salts provide high anti-tumor activity with low toxicity and are useful for treating cancers.