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<p>A series of novel pyrimidine and pyrimidopyrimidine analogs weresynthesized in good yield from 6-amino-4-aryl-2-oxo-pyrimidine-5-carbonitrile(<b>1a-d</b>). The synthesized compounds werecharacterized using various spectral studies, including FT-IR,<sup>1</sup>H NMR, <sup>13</sup>C NMR, massspectrometry, and elemental analysis. Newly synthesized pyrimidopyrimidines and2-(substituted-pyrazolyl)pyrimidine derivatives were assessed in vitro for theircytotoxic activities against three cancerous cell lines: colorectal carcinoma(<b>HCT-116</b>), mammary gland breast cancer(<b>MCF-7</b>), and hepatocellular carcinoma(<b>HEPG-2</b>), as well as normal fibroblasts(<b>W138</b>). The results indicated that compounds<b>3b</b>, <b>10b</b>, and<b>10c</b> exhibited the highest cytotoxic activities,with IC<sub>50</sub> values very close to those of the reference drug(doxorubicin) across all studied cancerous cell lines, while also demonstrating goodsafety effects on the normal human lung fibroblast cell line. Furthermore, all thesynthesized compounds were examined for their antimicrobial activity against twoGram-positive bacteria (<i>Staphylococcus aureus</i> and<i>Bacillus subtilis</i>), one Gram negativebacterium (<i>Escherichia coli</i>) and two fungalspecies (<i>Candida albicans</i> and <i>Aspergillus flavus</i>). The antimicrobial results of thesynthesized compounds, when compared with the reference drugs ampicillin andclotrimazole, revealed that compounds <b>3a</b>, <b>3b</b>, <b>3d</b>, <b>4a-d</b>, <b>9c</b> and <b>10b</b> exhibited excellent antimicrobial activities.Moreover, membrane stabilization or anti-hemolytic activity was employed as a methodto study the <i>in vitro</i> anti-inflammatory activityof the prepared heterocyclic compounds. Antioxidant activities were also assessed bymeasuring the percentage of free radical scavenging. Compounds <b>4b</b>, <b>10c</b> and <b>11a-c</b> demonstrated strong anti-hemolytic and antioxidant effects,which can be attributed to their ability to protect red blood cells fromhemolysis.</p>

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RETRACTED ARTICLE: Synthesis, antimicrobial, anti-inflammatory, antioxidant and cytotoxicity of new pyrimidine and pyrimidopyrimidine derivatives

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年3月18日

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  • Reda Mohammed Keshk,
  • Zeinab Ahmed Salama,
  • Samir Kamel Elsaedany,
  • Elsayed Mahmoud Abed ElRehim,
  • Doha Mohammad Beltagy

摘要

A series of novel pyrimidine and pyrimidopyrimidine analogs weresynthesized in good yield from 6-amino-4-aryl-2-oxo-pyrimidine-5-carbonitrile(1a-d). The synthesized compounds werecharacterized using various spectral studies, including FT-IR,1H NMR, 13C NMR, massspectrometry, and elemental analysis. Newly synthesized pyrimidopyrimidines and2-(substituted-pyrazolyl)pyrimidine derivatives were assessed in vitro for theircytotoxic activities against three cancerous cell lines: colorectal carcinoma(HCT-116), mammary gland breast cancer(MCF-7), and hepatocellular carcinoma(HEPG-2), as well as normal fibroblasts(W138). The results indicated that compounds3b, 10b, and10c exhibited the highest cytotoxic activities,with IC50 values very close to those of the reference drug(doxorubicin) across all studied cancerous cell lines, while also demonstrating goodsafety effects on the normal human lung fibroblast cell line. Furthermore, all thesynthesized compounds were examined for their antimicrobial activity against twoGram-positive bacteria (Staphylococcus aureus andBacillus subtilis), one Gram negativebacterium (Escherichia coli) and two fungalspecies (Candida albicans and Aspergillus flavus). The antimicrobial results of thesynthesized compounds, when compared with the reference drugs ampicillin andclotrimazole, revealed that compounds 3a, 3b, 3d, 4a-d, 9c and 10b exhibited excellent antimicrobial activities.Moreover, membrane stabilization or anti-hemolytic activity was employed as a methodto study the in vitro anti-inflammatory activityof the prepared heterocyclic compounds. Antioxidant activities were also assessed bymeasuring the percentage of free radical scavenging. Compounds 4b, 10c and 11a-c demonstrated strong anti-hemolytic and antioxidant effects,which can be attributed to their ability to protect red blood cells fromhemolysis.