Preprint Communication Version 1 Preserved in Portico This version is not peer-reviewed

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

Version 1 : Received: 23 January 2024 / Approved: 24 January 2024 / Online: 24 January 2024 (09:52:57 CET)

How to cite: Yu, Q. Sorafenib Analogue and Its Rearranged Compound: Design, Synthesis, Their In Vitro Anticancer Activity and Crystal Structure of the Rearranged Compound Dichloromethane Solvate. Preprints 2024, 2024011715. https://doi.org/10.20944/preprints202401.1715.v1 Yu, Q. Sorafenib Analogue and Its Rearranged Compound: Design, Synthesis, Their In Vitro Anticancer Activity and Crystal Structure of the Rearranged Compound Dichloromethane Solvate. Preprints 2024, 2024011715. https://doi.org/10.20944/preprints202401.1715.v1

Abstract

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.

Keywords

Sorafenib analogue; crystal structure; rearranged compound; anticancer activity

Subject

Chemistry and Materials Science, Medicinal Chemistry

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