Journal
MOLECULES
Volume 17, Issue 2, Pages 2000-2014Publisher
MDPI
DOI: 10.3390/molecules17022000
Keywords
synthesis; fluorescence spectroscopy; human serum albumin (HSA); DQL
Funding
- National Natural Science Foundation of China (NNSFC) [20972186, 21172256]
- National Basic Research Program of China [2010CB126104]
- Demonstration of R & D and Industrialization of Application of the Core Reagent and Intermediate for Scientific Research [2009BAK61B04]
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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.
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