abstract |
The invention discloses a class of naphthyl urea compounds with anti-cancer effect, a preparation method and application thereof. The biologically active naphthyl urea core group contained in it is further chemically modified to produce many compound groups with higher biological activity, which expands the The wide application of these compounds in biomedicine and the development prospect of pharmaceutical preparations. These compounds can significantly inhibit the activation of JAK2/STAT3 signals at low doses (sub-micromolar), and the results of MTT, molecular docking and western blotting experiments show that the compounds can specifically inhibit the activation of JAK2 signals and downstream STAT3, CyclinD1, CyclinB1 and The expression of target genes such as MMP9 induces cell cycle arrest and apoptosis, and significantly inhibits the proliferation of various tumor cell lines such as breast cancer, liver cancer, lung cancer, drug-resistant lung cancer, colon cancer and leukemia. Prospects of JAKs/STAT3-targeted anticancer drugs. |