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Abstract <p><i>N</i>-(2,5-Dimethylphenyl)-4-(pyridin-3-yl)pyrimidin-2-amine is the key intermediate product for the synthesis of imatinib and is the key structural feature which is likely to be responsible for its inhibitory effect against BCR-ABL kinase. In the present study, sixteen compounds were designed as possible alternatives to Imatinib to overcome the resistant cases. These compounds were synthesized by reactions of <i>N</i>-(2,5-dimethyl­phenyl)-4-(pyridin-3-yl)pyrimidin-2-amine with substituted benzoyl chlorides, chlorobenzenes, benzyl chlorides, and benzaldehydes under appropriate reaction condition. The new derivatives were characterized by spectral techniques such as FT-IR and NMR spectroscopy and mass spectrometry to confirm their structures. The novel imatinib analogues were then screened for their in vitro cytotoxicity against A549 and MCF7 cancer cell lines via MTT assay protocol. The compounds showed moderate antiproliferative activity at a concentration of 10 μM; among them, two derivatives exhibited antiproliferative activity at cell viability of 19.23±3.26 and 25.77±1.52 for A549 and 20.44±3.11 and 26.17±3.64 for MCF7.</p>

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Design, Synthesis, and Characterization of Some Novel Imatinib Derivatives as Promising Anticancer Agents

  • 期刊论文

  • 发表日期：

    2025年10月1日

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  • K. Sangwan,
  • G. Agarwal,
  • S. Kumar

摘要

Abstract

N-(2,5-Dimethylphenyl)-4-(pyridin-3-yl)pyrimidin-2-amine is the key intermediate product for the synthesis of imatinib and is the key structural feature which is likely to be responsible for its inhibitory effect against BCR-ABL kinase. In the present study, sixteen compounds were designed as possible alternatives to Imatinib to overcome the resistant cases. These compounds were synthesized by reactions of N-(2,5-dimethyl­phenyl)-4-(pyridin-3-yl)pyrimidin-2-amine with substituted benzoyl chlorides, chlorobenzenes, benzyl chlorides, and benzaldehydes under appropriate reaction condition. The new derivatives were characterized by spectral techniques such as FT-IR and NMR spectroscopy and mass spectrometry to confirm their structures. The novel imatinib analogues were then screened for their in vitro cytotoxicity against A549 and MCF7 cancer cell lines via MTT assay protocol. The compounds showed moderate antiproliferative activity at a concentration of 10 μM; among them, two derivatives exhibited antiproliferative activity at cell viability of 19.23±3.26 and 25.77±1.52 for A549 and 20.44±3.11 and 26.17±3.64 for MCF7.