Impact of Halogen Substituents on Interactions between 2-Phenyl-2,3-dihydroqulinazolin-4(1H)-one Derivatives and Human Serum Albumin
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...
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| Format: | Article |
| Language: | English |
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MDPI AG
2012-02-01
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| Series: | Molecules |
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| Online Access: | http://www.mdpi.com/1420-3049/17/2/2000/ |
| _version_ | 1828812190984962048 |
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| author | Shangzhong Liu Min Wang Junjun Ou Lei Wang Cong Lv Yi Wang Feng Liu |
| author_facet | Shangzhong Liu Min Wang Junjun Ou Lei Wang Cong Lv Yi Wang Feng Liu |
| author_sort | Shangzhong Liu |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-12-12T09:39:49Z |
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| id | doaj.art-dbd560d1384d483db7a2f89c4074fe42 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-12T09:39:49Z |
| publishDate | 2012-02-01 |
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| series | Molecules |
| spelling | doaj.art-dbd560d1384d483db7a2f89c4074fe422022-12-22T00:28:37ZengMDPI AGMolecules1420-30492012-02-011722000201410.3390/molecules17022000Impact of Halogen Substituents on Interactions between 2-Phenyl-2,3-dihydroqulinazolin-4(1H)-one Derivatives and Human Serum AlbuminShangzhong LiuMin WangJunjun OuLei WangCong LvYi WangFeng LiuA 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.http://www.mdpi.com/1420-3049/17/2/2000/synthesisfluorescence spectroscopyhuman serum albumin (HSA)DQL |
| spellingShingle | Shangzhong Liu Min Wang Junjun Ou Lei Wang Cong Lv Yi Wang Feng Liu Impact of Halogen Substituents on Interactions between 2-Phenyl-2,3-dihydroqulinazolin-4(1H)-one Derivatives and Human Serum Albumin Molecules synthesis fluorescence spectroscopy human serum albumin (HSA) DQL |
| title | Impact of Halogen Substituents on Interactions between 2-Phenyl-2,3-dihydroqulinazolin-4(1H)-one Derivatives and Human Serum Albumin |
| title_full | Impact of Halogen Substituents on Interactions between 2-Phenyl-2,3-dihydroqulinazolin-4(1H)-one Derivatives and Human Serum Albumin |
| title_fullStr | Impact of Halogen Substituents on Interactions between 2-Phenyl-2,3-dihydroqulinazolin-4(1H)-one Derivatives and Human Serum Albumin |
| title_full_unstemmed | Impact of Halogen Substituents on Interactions between 2-Phenyl-2,3-dihydroqulinazolin-4(1H)-one Derivatives and Human Serum Albumin |
| title_short | Impact of Halogen Substituents on Interactions between 2-Phenyl-2,3-dihydroqulinazolin-4(1H)-one Derivatives and Human Serum Albumin |
| title_sort | impact of halogen substituents on interactions between 2 phenyl 2 3 dihydroqulinazolin 4 1h one derivatives and human serum albumin |
| topic | synthesis fluorescence spectroscopy human serum albumin (HSA) DQL |
| url | http://www.mdpi.com/1420-3049/17/2/2000/ |
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