SYNTHESIS, DOCKING STUDIES AND EVALUATION OF ANTIMICROBIAL AND IN VITRO ANTIPROLIFERATIVE ACTIVITY OF 5H-CHROMENO 4,3-D PYRIMIDIN-2-AMINE DERIVATIVES
Objective: Docking studies and synthesis of 4-aryl-5H-chromeno [4,3 -d]pyrimidine-2-amine derivatives to evaluate antimicrobial and in vitro cytotoxicity activity.
Methods: Docking studies were performed on Autodock Vina. Computational work was carried out with UCSF Chimera, Argus lab, Marvin beans. Antimicrobial activity was carried out with the agar cup plate method on two gram-positive organisms viz. Bacillus Subtilis and Staphylococcus Aureus and two gram-negative organisms viz. Escherichia Coli and Pseudomonas Aeruginosa. In vitro cytotoxicity was performed on HeLa cell lines with Sulfo Rhodamine B (SRB) assay method.
Results: In docking studies compounds CHR 7, CHR 8 and CHR 9 gave highest docking score (binding free energy) and moderate antimicrobial activity against gram positive organisms. All the synthesized compounds showed poor antimicrobial activity against gram negative organisms. In vitro cytotoxicity activity, in terms of growth inhibitory concentration 50 % (GI50) was in the range 37.9 - 57.1 ÂµM. Though synthesised compounds possess moderate GI50, in comparison to standard Adrinamycin the compounds are inactive.
Conclusion: A series of 4-aryl-5H-chromeno[4,3 -d]pyrimidine-2-amine derivatives were synthesized and evaluated for antimicrobial and in vitro cytotoxicity studies. The compound CHR 9 was found most active among all the synthesised compounds.
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