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A highly practical and efficient preparation of 6-methy-4H-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 log10GI50 value of 4.55, 4.67 and 4.73 of compounds 9a, 9b and 9c, respectively.

international journal of organic chemistry

Efficient Synthesis of a New Class of &amp;lt;i&amp;gt;N&amp;lt;/i&amp;gt;-Nucleosides of 4&amp;lt;i&amp;gt;H&amp;lt;/i&amp;gt;-Thiochromeno[2,3-&amp;lt;i&amp;gt;d&amp;lt;/i&amp;gt;]pyrimidine-10-Sulfone as Potential Anticancer and Antibacterial Agents