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The Evaluation of Antiproliferative Effect of Imatinib Derivatives against Breast and Colon Cell-Lines
Author(s) -
Omar F. AbdulRasheed,
Ali N. Hussein,
Monther F. Mahdi,
Ayad M.R. Raauf
Publication year - 2020
Publication title -
international journal of pharmaceutical quality assurance
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.114
H-Index - 7
ISSN - 0975-9506
DOI - 10.25258/ijpqa.11.1.22
Subject(s) - imatinib , cytotoxic t cell , cell culture , tyrosine kinase , ic50 , chemistry , cytotoxicity , pharmacology , cancer cell lines , cancer research , tyrosine kinase inhibitor , biological activity , cancer , medicine , in vitro , cancer cell , biology , biochemistry , receptor , myeloid leukemia , genetics
Background: Cancer is considered as one of the major leading causes of death. Tyrosine kinase inhibitors are recognized for their potential antiproliferative effects.Materials and methods: In the previous study, the authors designed, synthesized, and characterized two imatinib derivatives. These derivatives were biologically evaluated with the utilization of MCF-7, HCT116, and MDCK cell lines.Results: In respect to the imatinib standard, compound 2b has superior activity against HCT116 cell line (IC50; 15.88 μg/mL against 18.52 μg/mL for imatinib) and an improved cytotoxic activity on MDCK cell line (IC50; 0.654 mg/mL against 0.272 mg/mL for imatinib).Conclusion: The two synthesized compounds showed biological activity against cancerous cell lines and improved cytotoxic activity against normal non-cancerous cell line with respect to the imatinib standard.

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