| Literature DB >> 24844756 |
Khalid Mohammed Khan1, Syed Muhammad Saad2, Nimra Naveed Shaikh2, Shafqat Hussain2, Muhammad Imran Fakhri2, Shahnaz Perveen3, Muhammad Taha4, Muhammad Iqbal Choudhary5.
Abstract
2-Arylquinazolin-4(3H)-ones 1-25 were synthesized by reacting anthranilamide with various benzaldehydes using CuCl2·2H2O as a catalyst in ethanol under reflux. Synthetic 2-arylquinazolin-4(3H)-ones 1-25 were evaluated for their β-glucuronidase inhibitory potential. A trend of inhibition IC50 against the enzyme in the range of 0.6-198.2μM, was observed and compared with the standard d-saccharic acid 1,4-lactone (IC50=45.75±2.16μM). Compounds 13, 19, 4, 12, 14, 22, 23, 25, 15, 8, 17, 11, 21, 1, 3, 18, 9, 2, and 24 with the IC50 values within the range of 0.6-44.0μM, indicated that the compounds have superior activity than the standard. The compounds showed no cytotoxic effects against PC-3 cells. A structure-activity relationship is established.Entities:
Keywords: 2-Arylquinazolin-4(3H)-ones; Cytotoxicity; Structure–activity relationship; β-Glucuronidase inhibition
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Year: 2014 PMID： 24844756 DOI： 10.1016/j.bmc.2014.04.039
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641