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<p>A panel of 27 new compounds was prepared, starting from N-propargyl-3,4-dichloromaleimide where one chlorine atom was first replaced with either morpholine or piperidine. Then, the acetylenic moiety was subjected to a copper-catalyzed Mannich-type reaction to afford aminoacetylenic derivatives of maleimide. The prepared compounds' structures were characterized using IR, NMR, MS, and X-ray analysis (for compound 4&#xa0;h). The newly synthesized compounds were evaluated for their cytotoxic activities against three cancer cell lines: MCF-7, MDA-MB-231, and K562. Ten compounds exhibited cytotoxic activity against one or two cell lines, among which <b>4c</b> and <b>5c</b> were active against all three cancer cell lines. Compounds <b>5e, 5 h,</b> and <b>5c</b> demonstrated excellent cytotoxicity against MCF-7 breast cancer cells. Compounds <b>5a, 5e, 5c,</b> and <b>5d</b> displayed moderate activity against leukemia (K562) cell lines, while compounds <b>4c</b> and <b>4a</b> showed good activity against metastatic breast cancer (MDA-MB-231) Additionally, compounds <b>5c</b> and <b>4h</b> exhibited moderate activity against MDA-MB-231.</p>

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Synthesis and anti-cancer evaluation of aminoacetylene maleimide hybrids

  • 期刊论文

  • 发表日期：

    2025年7月8日

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  • Bader A. Salameh,
  • Ahmad M. Al-malkawi,
  • Iman A. Mansi,
  • Kayed Abu-Safieh,
  • Murad A. AlDamen,
  • Bashaer Abu-Irmaileh

摘要

A panel of 27 new compounds was prepared, starting from N-propargyl-3,4-dichloromaleimide where one chlorine atom was first replaced with either morpholine or piperidine. Then, the acetylenic moiety was subjected to a copper-catalyzed Mannich-type reaction to afford aminoacetylenic derivatives of maleimide. The prepared compounds' structures were characterized using IR, NMR, MS, and X-ray analysis (for compound 4 h). The newly synthesized compounds were evaluated for their cytotoxic activities against three cancer cell lines: MCF-7, MDA-MB-231, and K562. Ten compounds exhibited cytotoxic activity against one or two cell lines, among which 4c and 5c were active against all three cancer cell lines. Compounds 5e, 5 h, and 5c demonstrated excellent cytotoxicity against MCF-7 breast cancer cells. Compounds 5a, 5e, 5c, and 5d displayed moderate activity against leukemia (K562) cell lines, while compounds 4c and 4a showed good activity against metastatic breast cancer (MDA-MB-231) Additionally, compounds 5c and 4h exhibited moderate activity against MDA-MB-231.