[EN] 3-DIARYLMETHYLENES AND USES THEREOF<br/>[FR] 3-DIARYLMÉTHYLÈNES ET LEURS UTILISATIONS
申请人:ATUX ISKAY LLC
公开号:WO2021188949A1
公开(公告)日:2021-09-23
3-Diarylmethylenes are disclosed. The compounds activate PP2A, suppress oncogenic kinase signaling, and negatively regulate MYC and MYCN in cancer. The compounds also induce FOXO transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a monotherapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.
3-二芳基亚甲基烯已被披露。这些化合物激活PP2A,抑制致癌激酶信号传导,并在癌症中负调节MYC和MYCN。这些化合物还通过调节PP2A诱导FOXO转录因子转位到细胞核,从而表现出抗增殖效应。它们在治疗各种疾病中很有用,包括作为单药治疗癌症,或与其他药物联合使用以恢复对化疗的敏感性,尤其是在出现耐药性的情况下。