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Molecules 2012, 17(2), 2000-2014; doi:10.3390/molecules17022000

Impact of Halogen Substituents on Interactions between 2-Phenyl-2,3-dihydroqulinazolin-4(1H)-one Derivatives and Human Serum Albumin

Department of Applied Chemistry, China Agricultural University, Beijing 100193, China
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Received: 16 December 2011 / Revised: 26 January 2012 / Accepted: 27 January 2012 / Published: 17 February 2012
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Abstract

A novel type of 2-(un)substituted phenyl-2,3-dihydroquinazolin-4(1H)-one (DQL) derivatives were designed and synthesized to study the impact of halogen substituents on interactions between DQL and human serum albumin (HSA) by comparison methodology. The interactions between DQL and HSA were studied by fluorescence spectroscopy. The intrinsic fluorescence of human serum albumin was quenched by DQL through a static quenching mechanism. Site marker competitive experiments showed that DQL bound to HSA in site II (subdomain IIIA). The binding constants, the numbers of binding sites and the thermodynamic parameters were measured too. The results indicated that the interactions were spontaneous, mainly through hydrophobic forces, and the substitution by halogen atoms in the benzene ring could increase the interactions between DQL and HSA. Furthermore, the binding affinity was enhanced gradually with the increasing of halogen atomic number.
Keywords: synthesis; fluorescence spectroscopy; human serum albumin (HSA); DQL synthesis; fluorescence spectroscopy; human serum albumin (HSA); DQL
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Liu, F.; Wang, Y.; Lv, C.; Wang, L.; Ou, J.; Wang, M.; Liu, S. Impact of Halogen Substituents on Interactions between 2-Phenyl-2,3-dihydroqulinazolin-4(1H)-one Derivatives and Human Serum Albumin. Molecules 2012, 17, 2000-2014.

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