One-Pot Multicomponent Synthesis and Cytotoxic Evaluation of Novel 7-Substituted-5-(1<i>H</i>-Indol-3-yl)Tetrazolo[1,5-a] Pyrimidine-6-Carbonitrile

• Main Authors: Mohamed A. A. Radwan, Fahad M. Alminderej, Hanem M. Awad
• Format: Article
• Language: English
• Published: MDPI AG 2020-01-01
• Series: Molecules
• Subjects: indole; tetrazole; pyrimidine; multicomponent reaction (mcrs); cytotoxicity; hct-116; mcf-7; mda-mb-231; a549
• Online Access: https://www.mdpi.com/1420-3049/25/2/255
• ISSN: 1420-3049

A series of novel 7-substituted-5-(1<i>H</i>-indol-3-<i>yl</i>)tetrazolo[1,5-a]pyrimidine-6-carbonitrile was synthesized via a one-pot, three-multicomponent reaction of appropriate aldehydes, 1<i>H</i>-tetrazole-5-amine and 3-cyanoacetyl indole in catalytic triethylamine. The cytotoxic activity of the new synthesized tetrazolopyrimidine-6-carbonitrile compounds was investigated against HCT-116, MCF-7, MDA-MB-231, A549 human cancer cell lines and one human healthy normal cell line (RPE-1) using the MTT cytotoxicity assay. Compounds <b>4h</b>, <b>4b</b>, <b>4c</b>, <b>4i</b> and <b>4a</b> showed potent anticancer activities against human colon cancer. Additionally, all the compounds showed potent anticancer activities on human lung cancer.