Synthesis, biological evaluation and docking studies of 4-amino-tetrahydroquinazolino[3,2-e]purine derivatives

The synthesis of new 4-amino-tetrahydroquinazolino[3,2-e]purine derivatives along with their activity in cell-free enzymatic assays on Src is reported. Some compounds emerged as moderately active inhibitors of the enzyme and showed antiproliferative effects on the murine leukemia L1210 cell line. Docking studies have been also performed to analyze the binding mode of compounds under study and to identify the structural determinants of their interaction. Therefore, this study provides a new promising scaffold with moderate enzymatic inhibitory activities for further development of new anticancer drugs targeting Src tyrosine kinase.

Graphical abstractA series of 4-amino-tetrahydroquinazolino[3,2-e]purine derivatives was synthesized and evaluated for its Src cell-free enzymatic inhibitory and antiproliferative activity on the murine leukemia L1210 cell line.Figure optionsDownload full-size imageDownload as PowerPoint slide