AI Article Synopsis
- A new method was developed for creating 3,4-diaminopyrazolo[3,4-]pyrimidines using a three-component reaction involving 3,5-diaminopyrazole-4-carbonitriles, primary amines, and orthoesters.
- This method was efficient, especially under microwave heating, allowing for the rapid synthesis of 116 different compounds, which didn’t require complex purification steps.
- The most effective compound showed significant anti-leukemic activity, inhibiting Jurkat T cells at just 0.5 μM while being highly selective over non-cancerous cells.
Article Abstract
A convenient method for the synthesis of ,-disubstituted 3,4-diaminopyrazolo[3,4-]pyrimidines was developed using a three-component reaction of 3,5-diaminopyrazole-4-carbonitriles with primary amines and orthoesters. The preparation of 116 examples demonstrated the good scope of the reaction, which tolerated variations in the substrate structure and was particularly efficient under microwave irradiation. The short reaction time and chromatography-free product isolation add practicality to this method. The anti-leukemic activity was assessed using K562 and Jurkat T cells, and the selectivity of the most active compounds was evaluated using non-cancerous MRC5 cells. The most promising compound inhibited Jurkat T cells with a GI value of 0.5 μM and a selectivity index of 65.
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| http://dx.doi.org/10.1039/d3ob00350g | DOI Listing |
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