Next Article in Journal
3D-QSAR Studies of Dihydropyrazole and Dihydropyrrole Derivatives as Inhibitors of Human Mitotic Kinesin Eg5 Based on Molecular Docking
Previous Article in Journal
Allylic Alkylations Catalyzed By Palladium-Bis(oxazoline) Complexes Derived From Heteroarylidene Malonate Derivatives
Molecules 2012, 17(2), 2000-2014; doi:10.3390/molecules17022000
Article

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

, , , , ,  and *
Received: 16 December 2011; in revised form: 26 January 2012 / Accepted: 27 January 2012 / Published: 17 February 2012
Download PDF [583 KB, uploaded 18 June 2014]
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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Export to BibTeX |
EndNote


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.

AMA 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(2):2000-2014.

Chicago/Turabian Style

Liu, Feng; Wang, Yi; Lv, Cong; Wang, Lei; Ou, Junjun; Wang, Min; Liu, Shangzhong. 2012. "Impact of Halogen Substituents on Interactions between 2-Phenyl-2,3-dihydroqulinazolin-4(1H)-one Derivatives and Human Serum Albumin." Molecules 17, no. 2: 2000-2014.


Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert