METHOD FOR PREPARING CYCLODEXTRIN-LOADED INDOLE SPIRO PYRROLE DERIVATIVE AND APPLICATION THEREOF AS ANTI-TUMOR DRUG

• Main Authors: YAO, Hong, WEI, Mengxue, ZHU, Songlei, GAO, Xiaoge, LIU, Hongzhi
• Format: Patent
• Language: Chinese; English; French
• Published: 25.10.2018
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

A method for preparing a cyclodextrin-loaded indole spiro pyrrole derivative and an application thereof as an anti-tumor drug is provided. By modulating a pH value, an indole spiro pyrrole derivative which is not readily soluble in water is loaded onto cyclodextrin to effectively solve the problem of poor drug solubility; more importantly, on a mouse tumor model, a cyclodextrin-loaded indole spiro pyrrole derivative having hexahydrospiro [indoline-3,3'-pyrrolizine]-2-one as a nucleus exhibits a definite anti-tumor effect and has almost no toxicity. Compared with the prior art, the prepared cyclodextrin-loaded indole spiro pyrrole derivative has good solubility, significant inhibition of tumor cell proliferation, low toxic side effects, etc. The types of tumors treated include but are not limited to: liver cancer, renal cancer, skin cancer, nasopharynx cancer, gastrointestinal cancer, etc. L'invention concerne un procédé de préparation d'un dérivé d'indole spiro-pyrrole chargé de cyclodextrine et une applicati