Diagnosis and treatment integrated antitumor drug Caba-808 and preparation method thereof

• Main Authors: HOU GUANGDONG, ZHANG GENG, WEI DI, ZHANG LEI, DUN XINLONG, MENG PING, ZHENG YU, YAN FEI, YUAN JIANLIN, JU DONG'EN, ZHENG WANXIANG, GAO MING, HE WEI, WANG FULI, LAN TING
• Format: Patent
• Language: Chinese; English
• Published: 16.04.2021
• Subjects: ADHESIVES; CHEMISTRY; DYES; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MATERIALS FOR MISCELLANEOUS APPLICATIONS, NOT PROVIDED FORELSEWHERE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; MISCELLANEOUS APPLICATIONS OF MATERIALS; MISCELLANEOUS COMPOSITIONS; NATURAL RESINS; ORGANIC CHEMISTRY; PAINTS; POLISHES; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The invention discloses a diagnosis and treatment integrated antitumor drug Caba-808 and a preparation method thereof, the structural formula of the Caba-808 is as shown in formula I as shown in the description, wherein R1 is any one of -H, -CH3 or -CH3CO, and R1 is any one of -C6H5, -NHCOC6H5 or -NHCOOC(CH3)3. The anti-tumor drug Caba-808 provided by the invention can be combined with tubulin to inhibit mitosis of cells, so that an anti-tumor effect is achieved. Meanwhile, the drug has a good fluorescence imaging effect in a near-infrared region, and can clearly display the part and size of a tumor. On the other hand, the preparation method of the novel anti-tumor medicine is simple and easy to operate, and the production cost can be effectively reduced to realize industrial production. 本发明公开了诊疗一体化抗肿瘤药物Caba-808及其制备方法，Caba-808的结构式如式Ⅰ所示：其中，R1为-H、-CH3或-CH3CO中任一个；R2为-C6H5、-NHCOC6H5或-NHCOOC(CH3)3中任一个。本发明提供的抗肿瘤药物Caba-808能与微管蛋白结合，抑制细胞有丝分裂，从而发挥抗肿瘤作用。同时，该药物在近红外区有较好的荧光成像效果，能清晰的显示出肿瘤的部位与大小。另一方面，本发明新型抗肿瘤药物的制备方法简单易操作，能够有