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<p>Three libraries containing pyrrolo[2,3-d]pyrimidine moiety linked to diazospiro[3.5]nonane, diazospiro[5.5]undecane and piperazine - piperidine hybrid derivatives were synthesized involving various <i>N</i>-deprotection and acid amine coupling reactions. They were tested for their invitro cytotoxicity against triple negative human breast cancer cells MDA-MB-231 and BT-549. Promising results were obtained by pyrrolo[2,3-d]pyrimidine linked diazospiro[3.3]nonane compounds (<b>7a</b> and <b>7c</b>) containing <i>ortho</i>-trifluoro and <i>meta</i>-bromo functional groups against MDA-MB-231 cells. Their dose response curves were plotted and their IC<sub>50</sub> value found to be <b>11.66 µM</b> (<b>7a</b>) and <b>10.37 µM (7b)</b>. Additionally, performed acridine orange and rhodamine 123 straining tests to study the cell deformation at various dosages, which garnered promising results.</p><p></p>

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Design and synthesis of pyrrolo[2,3-d]pyrimidine linked diazospiro and piperazine – piperidine libraries as anticancer agents

  • 期刊论文

  • 发表日期：

    2026年7月17日

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  • Sridhar Guda,
  • Srilakshmi V Patri,
  • Krishna Reddy V,
  • Vishnu Thumma,
  • Santosh Kumar Guru

摘要

Three libraries containing pyrrolo[2,3-d]pyrimidine moiety linked to diazospiro[3.5]nonane, diazospiro[5.5]undecane and piperazine - piperidine hybrid derivatives were synthesized involving various N-deprotection and acid amine coupling reactions. They were tested for their invitro cytotoxicity against triple negative human breast cancer cells MDA-MB-231 and BT-549. Promising results were obtained by pyrrolo[2,3-d]pyrimidine linked diazospiro[3.3]nonane compounds (7a and 7c) containing ortho-trifluoro and meta-bromo functional groups against MDA-MB-231 cells. Their dose response curves were plotted and their IC50 value found to be 11.66 µM (7a) and 10.37 µM (7b). Additionally, performed acridine orange and rhodamine 123 straining tests to study the cell deformation at various dosages, which garnered promising results.