Novel Insight in Structure−Activity Relationship and Bioanalysis of P-Glycoprotein Targeting Highly Potent Tetrakishydroxymethyl Substituted 3,9-Diazatetraasteranes

2008 ◽  
Vol 51 (18) ◽  
pp. 5871-5874 ◽  
Author(s):  
Claudius Coburger ◽  
Jörg Wollmann ◽  
Christiane Baumert ◽  
Martin Krug ◽  
Josef Molnár ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity ◽  
P Glycoprotein

Structure–Activity Relationship Study of Permethyl Ningalin B Analogues as P-Glycoprotein Chemosensitizers

2013 ◽  
Vol 56 (22) ◽  
pp. 9057-9070 ◽  
Author(s):  
Jin Wen Bin ◽  
Iris L. K. Wong ◽  
Xuesen Hu ◽  
Zhang Xiao Yu ◽  
Li Fu Xing ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity ◽  
P Glycoprotein ◽  
Relationship Study

Cytocompatibility and P-glycoprotein Inhibition of Block Copolymers: Structure–Activity Relationship

2013 ◽  
Vol 10 (8) ◽  
pp. 3232-3241 ◽  
Author(s):  
A. Cambón ◽  
J. Brea ◽  
M. I. Loza ◽  
C. Alvarez-Lorenzo ◽  
A. Concheiro ◽  
...  
Keyword(s):  
Block Copolymers ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity ◽  
P Glycoprotein ◽  
Glycoprotein Inhibition

scholarly journals High-Speed Screening and Structure-Activity Relationship Analysis for the Substrate Specificity of P-Glycoprotein (ABCB1)

2003 ◽  
Vol 3 ◽  
pp. 175-193 ◽  
Author(s):  
Yuko Onishi ◽  
Hiroyuki Hirano ◽  
Kunio Nakata ◽  
Keisuke Oosumi ◽  
Makoto Nagakura ◽  
...  
Keyword(s):  
Substrate Specificity ◽  
High Speed ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Relationship Analysis ◽  
Structure Activity ◽  
P Glycoprotein

scholarly journals Antioxidant and Chemosensitizing Effects of Flavonoids with Hydroxy and/or Methoxy Groups and Structure-Activity Relationship

2007 ◽  
Vol 10 (4) ◽  
pp. 537 ◽  
Author(s):  
Ju-Mi Jeong ◽  
Cheol-Hee Choi ◽  
Su-Kyeong Kang ◽  
In-Hwa Lee ◽  
Ji-Yoon Lee ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Oh Groups ◽  
Structure Activity ◽  
P Glycoprotein ◽  
Ic50 Values

Purpose. Flavonoids have been used as antioxidant, chemopreventive and chemosensitizing agents. In this study, eleven flavonoids containing a variety of hydroxy (OH) and/or methoxy (OMe) groups were evaluated for their antioxidant, cytotoxic and chemosensitizing effects to create a structure-activity relationship (SAR). Methods. 1,1-Diphenyl-2-picrylhydrazyl (DPPH) radical solution-based chemical assay and and 2',7'-dichlorofluorescin diacetate (DCFH-DA) cellular-based assay were used to compare the free radical scavenging activity on the same molar concentration basis using the AML-2/DX100 cells which are characterized by the down-regulated expression of catalase and resulting supersensitiviy to hydrogen peroxide. The chemosensitization and cytotoxicity were determined by the MTT assay in the presence or absence of an anticancer drug using the P-glycoprotein-overexpressing AML-2 subline AML-2/D100 cells. Results. The antioxidant activity of the flavonoid (3,5,7,3’,4’-OH) was higher than that of the flavonoid (5,7,3’,4’-OH). Flavonoids substituted with the various number of OMe decreased antioxidant activity. Flavonoids with 7-OH or 5,7-OH groups have the highest cytotoxicity, and flavonoids with 5,7-OMe group intermediate cytotoxicity. The IC50 values of flavonoid (5,7-OMe, 3’,4’,5’-OMe) and flavonoid (5,7-OMe, 4’-OMe), 0.4 M and 1.4 M. The IC50 values of flavonoid (5,6,7-OMe, 3’,4’-OMe) and flavonoid (5,6,7-OMe, 3’,4’,5’-OMe), 3.2 uM and 0.9 M, respectively, and those of flavonoid (5,6,7-OMe, 3’,4’,5’-OMe) and flavonoid (5,7-OMe,3’,4’,5’-OMe) were 0.9 M and 0.4 M, respectively. Conclusions. These results suggest that flavonoids with 3-OH group play a positive role in antioxidant activities, flavonoids with 5-OH and/or 7-OH groups show the higher cytotoxicity, and flavonoids with 3’-OMe and/or 5’-OMe groups plays positive but 6-OMe groups negative roles in the P-glycoprotein (Pgp) inhibition. It is believed that these SAR results can be taken into account for the development of flavonoids with high therapeutic index.

Structure–activity relationship of natural and synthetic coumarins inhibiting the multidrug transporter P-glycoprotein

2006 ◽  
Vol 14 (20) ◽  
pp. 6979-6987 ◽  
Author(s):  
Imad Raad ◽  
Raphael Terreux ◽  
Pascal Richomme ◽  
Eva-Laure Matera ◽  
Charles Dumontet ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Multidrug Transporter ◽  
Structure Activity ◽  
P Glycoprotein ◽  
Relationship Of ◽  
Natural And Synthetic
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