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

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1 Department of Pharmaceutical Chemistry, College of Pharmacy, University of Kerbala, Karbala, Karbala, Iraq
2 Department of Chemistry and Biochemistry, College of Medicine, Al Nahrain University, Baghdad, Baghdad, Iraq
3 Department of Pharmaceutical Chemistry, Ashur University College, Baghdad, Baghdad, Iraq
4 Department of Pharmaceutical Chemistry, University of Mustansiriyah, Baghdad, Baghdad, Iraq
DOI
10.7287/peerj.preprints.27755v1
Published
Accepted
Subject Areas
Toxicology, Drugs and Devices, Global Health, Gynecology and Obstetrics, Oncology
Keywords
characterization, synthesis, colon cancer, breast cancer, tyrosine kinase inhibitor, MDCK, IC50, MCF-7, HCT116, cell lines
Copyright
© 2019 Al-Obaidi et al.
Licence
This is an open access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, reproduction and adaptation in any medium and for any purpose provided that it is properly attributed. For attribution, the original author(s), title, publication source (PeerJ Preprints) and either DOI or URL of the article must be cited.
Cite this article
Al-Obaidi ZMJ, Abdul-Rasheed OF, Mahdi MF, Raauf AMR. 2019. Synthesis, characterization, and biological evaluation of new spebrutinib analogues: potential candidates with enhanced activity and reduced toxicity profiles. PeerJ Preprints 7:e27755v1

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).

Author Comment

This is a submission to PeerJ for review.

Supplemental Information

MDCK normal kidney cell line

DOI: 10.7287/peerj.preprints.27755v1/supp-2

MCF-7 breast cancer cell line

DOI: 10.7287/peerj.preprints.27755v1/supp-3