Sorafenib Analogue and Its Rearranged Compound: Design, Synthesis, Their In Vitro Anticancer Activity and Crystal Structure of the Rearranged Compound Dichloromethane Solvate

Cancer is a devastating disease with female breast cancer becoming the leading cause of global cancer morbidity. Herein we report the design and synthesis of a sorafenib analog 1A and its base-promoted arranged compound 1A2. Their in vitro cytotoxicity and potencies in EFGR inhibition study revealed that compound 1A displayed good antiproliferative activity in MDA-MB-231 (breast) cells with an IC50 value of 16.18±1.42 μM. Crystallization 1A2 affored 1A2a as a solvate with dichloromethane which was explicitly confirmed by the single crystal X-ray diffraction analysis.