| abstract |
The invention provides a series of aryl and heterocycle substituted imidazole, oxazole and thiazole derivatives, particularly stilbene tumor targeted medicine Combretastatin A4 analogs. The natural product Combretastatin A4 is used as a lead compound, and imidazole, oxazole and thiazole quinary heterocycles are substituted for vinyl chains in the structure to obtain a series of imidazole, oxazole and thiazole Combretastatin A4 analogs. The invention overcomes the defect that the vinyl group in the Combretastatin A4 structure can be easily isomerized. The stilbene tumor targeted medicine Combretastatin A4 analogs are a type of compounds in a brand new structure. The initial pharmacological activity screening test indicates that most compounds have a function on inhibiting proliferation of tumor cells in vitro, part of compounds have an obvious function on inhibiting proliferation, and IC50 is equivalent to CA4, reaching Grade nM. The aryl and heterocycle substituted imidazole, oxazole and thiazole Combretastatin A4 analogs and salts thereof are applicable to preparation of antineoplastic drugs. |