Synthesis, characterization, and biological evaluation of new spebrutinib analogues: potential candidates with enhanced activity and reduced toxicity profiles

Abstract

Background: Cancer is regarded as an undoubtable major concern for both researchers and the general public because of its high mortality rates. While breast cancer has the highest incidence of malignancy globally, colon cancer also has high morbidity and mortality rates. Currently, researchers are working on designing, synthesizing, and biologically investigating the effects of some potential anticancer candidates. Methods: The authors successfully synthesized and characterized two potential spebrutinib analogues. These analogues were evaluated with the employment of MCF-7, HCT116, and MDCK cell lines. Results: With respect to the spebrutinib standard, one of these analogues had superior activity against the MCF-7 cell line (IC50; 10.744 µg/mL against 13.566 µg/mL for spebrutinib) and an enhanced toxicity profile on the MDCK cell line (IC50; 8.653 mg/mL against 4.011 mg/mL for spebrutinib).