公开(公告)号：US20200330449A1

公开(公告)日：2020-10-22

申请号：US16831346

申请日：2020-03-26

Applicant: Academia Sinica

Inventor： Rong-Jie CHEIN ,  Pan-Chyr YANG ,  Chi-Huey WONG ,  Ming-Shiu LIN ,  Ting-Jen CHENG ,  Ting-Hung CHOU

IPC: A61K31/47 ,  C07D215/233 ,  A61K45/06 ,  A61P35/00

Abstract: Compounds of Formula (I) and methods for treating, delaying, and/or preventing the adverse effects of proliferative diseases, such as cancers including, for example, lung cancer, breast cancer, ovarian cancer, prostate cancer, head cancer, neck cancer, head and neck cancer, or leukemia (e.g., cancer resistant to treatment by one or more microtubule-targeting agents, e.g., cancer resistant to multiple drugs associated with P-glycoprotein (P-gp) overexpression). Methods of inhibiting polymerization of a cancer cell microtubule in a subject in need thereof or a cell, tissue, or biological sample, binding p-tubulin, inhibiting microtubule assembly and, inducing apoptosis in a cancer cell resistant to multiple drugs in a tissue, biological sample, or subject. Pharmaceutical compositions, kits, and methods of using the compounds for treating any of the target diseases described herein.