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<p>The reaction of ethyl 4′-amino-1′H-spiro[cycloheptane-1,2′-naphthalene]-3′-carboxylate with <i>m</i>-tolyl isothiocyanate and subsequent cyclization of the intermediate thiourea derivative synthesized 2-thioxo-3-(<i>m</i>-tolyl)-2,3-dihydro-1<i>H</i>-spiro[benzo[<i>h</i>]quinazoline-5,1′-cycloheptane]-4(6<i>H</i>)-one. The last was alkylated by various halides in the presence of alkali to form 2-thiosubstituted 3-(<i>m</i>-tolyl)-3<i>H</i>-spiro[benzo[<i>h</i>]-quinazoline-5,1′-cycloheptane]-4(6<i>H</i>)-ones. The antibacterial activity of the synthesized compounds was studied by the agar diffusion method using Gram-positive strains <i>Staphylococcus aureus</i> 209p and <i>Bacillus subtilis</i> ATCC 6633 and Gram-negative strains <i>Shigella flexneri</i> 6858 and <i>Escherichia coli</i> 0-55. The antitumor properties of the synthesized compounds were studied on a transplantable mouse tumor sarcoma 180 model. It was established that the studied compounds possessed antibacterial and antitumor activity. A comparative evaluation of the results indicated that the activities of the studied compounds were noticeably inferior to that of the reference antimicrobial drug furazolidone. The studied compounds at doses of 145-170 mg/kg exhibited antitumor activity against sarcoma 180, inhibiting tumor growth by 31-56%.</p>

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Synthesis and Antitumor and Antibacterial Activity of Sulfanyl-Substituted 3-(m-tolyl)-3H-spiro[benzo[h]quinazoline-5,1′-Cycloheptane]-4(6H)-ones

  • 期刊论文

  • 发表日期：

    2025年8月1日

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  • A. I. Markosyan,
  • S. M. Vardapetyan,
  • A. M. Hovhannisyan,
  • R. A. Bekjanyan,
  • Kh. S. Hakopyan,
  • S. H. Gabrielyan,
  • M. Yu. Dangyan,
  • H. H. Arakelyan,
  • F. H. Arsenyan,
  • A. S. Sagyan

摘要

The reaction of ethyl 4′-amino-1′H-spiro[cycloheptane-1,2′-naphthalene]-3′-carboxylate with m-tolyl isothiocyanate and subsequent cyclization of the intermediate thiourea derivative synthesized 2-thioxo-3-(m-tolyl)-2,3-dihydro-1H-spiro[benzo[h]quinazoline-5,1′-cycloheptane]-4(6H)-one. The last was alkylated by various halides in the presence of alkali to form 2-thiosubstituted 3-(m-tolyl)-3H-spiro[benzo[h]-quinazoline-5,1′-cycloheptane]-4(6H)-ones. The antibacterial activity of the synthesized compounds was studied by the agar diffusion method using Gram-positive strains Staphylococcus aureus 209p and Bacillus subtilis ATCC 6633 and Gram-negative strains Shigella flexneri 6858 and Escherichia coli 0-55. The antitumor properties of the synthesized compounds were studied on a transplantable mouse tumor sarcoma 180 model. It was established that the studied compounds possessed antibacterial and antitumor activity. A comparative evaluation of the results indicated that the activities of the studied compounds were noticeably inferior to that of the reference antimicrobial drug furazolidone. The studied compounds at doses of 145-170 mg/kg exhibited antitumor activity against sarcoma 180, inhibiting tumor growth by 31-56%.