This invention discloses 2'-hydroxy-4,4',6'-trimethoxychalcone and 5,7,4'-trimethoxyflavanone sulfonamide derivatives, their
synthesis methods and applications, belonging to the field of
pharmaceutical technology, and involving two series of compounds: 3-sulfonamido-2'-hydroxy-4,4',6'-trimethoxychalcone and 8,3'-disulfonamido-5,7,4'-trimethoxyflavanone, and their preparation methods. Starting with 2-hydroxy-4,6-dimethoxyacetophenone and p-anisaldehyde or 4-methoxy-3-nitrobenzaldehyde, 2'-hydroxy-4,4',6'-trimethoxychalcone or 3-amino-2'-hydroxy-4,4',6'-trimethoxychalcone intermediates were synthesized via the Claisen-Schmidt reaction. Then, through sulfonation and intramolecular Michael addition reactions, 2'-hydroxy-4,4',6'-trimethoxychalcone and 5,7,4'-trimethoxyflavanone sulfonamide derivatives were synthesized. The preparation method is simple, mild, and yields high results.
In vitro and
in vivo activity tests show that the derivatives disclosed in this invention have significant
in vitro inhibitory activity against gastric
cancer,
esophageal cancer,
colorectal cancer, and
lung cancer cell lines, acting as inhibitors of the
protein YBX1 / RPN1. Clinically, they can be applied to
targeted therapy for cancers such as gastric
cancer,
esophageal cancer,
colorectal cancer, and
lung cancer.