Efficient Synthesis of a New Class of <i>N</i>-Nucleosides of 4<i>H</i>-Thiochromeno[2,3-<i>d</i>]pyrimidine-10-Sulfone as Potential Anticancer and Antibacterial Agents — Oak Academic Publishing
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Efficient Synthesis of a New Class of <i>N</i>-Nucleosides of 4<i>H</i>-Thiochromeno[2,3-<i>d</i>]pyrimidine-10-Sulfone as Potential Anticancer and Antibacterial Agents
Department of Chemistry, Al-Imam Mohammad Ibn Saud Islamic University (IMSIU), Faculty of Science, Riyadh, KSA
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Department of Chemistry, Al-Imam Mohammad Ibn Saud Islamic University (IMSIU), Faculty of Science, Riyadh, KSA Photochemistry Department, Heterocyclic & Nucleosides Unit, National Research Centre, Cairo, Egypt
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Department of Chemistry, Al-Imam Mohammad Ibn Saud Islamic University (IMSIU), Faculty of Science, Riyadh, KSA Photochemistry Department, Heterocyclic & Nucleosides Unit, National Research Centre, Cairo, Egypt
1 Department of Chemistry, Al-Imam Mohammad Ibn Saud Islamic University (IMSIU), Faculty of Science, Riyadh, KSA
2 Department of Chemistry, Al-Imam Mohammad Ibn Saud Islamic University (IMSIU), Faculty of Science, Riyadh, KSA Photochemistry Department, Heterocyclic & Nucleosides Unit, National Research Centre, Cairo, Egypt
3 Department of Chemistry, Al-Imam Mohammad Ibn Saud Islamic University (IMSIU), Faculty of Science, Riyadh, KSA Photochemistry Department, Heterocyclic & Nucleosides Unit, National Research Centre, Cairo, Egypt
A highly practical and efficient preparation of 6-methy-4 H -thiochromene and 7-methyl-thiochromene[2,3- d ]pyrimidine derivatives was developed via a multi-component reaction of 3-methyl-thiophenol ( 1 ), aldehydes ( 2 ), and malononitrile ( 3 ). A series of pyrimidine nucleoside, thiochromene[2,3- d ]pyrimidine and thiochromene[2,3- d ]pyrimidine-10-sulfone was efficiently obtained. These hybrid compounds were evaluated as potential antibacterial and anticancer agents and showed encouraging biological activities. Some of these derivatives showed broad-spectrum antitumour activity against the nine tumour subpanels tested, and demonstrated significant activity in the in vitro antitumour screening expressed by MG-MID log 10 GI 50 value of － 4.55, －4.67 and －4.73 of compounds 9a , 9b and 9c , respectively.
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