Biological evaluation, structure-activity relationships, and three-dimensional quantitative structure-activity relationship studies of dihydro-beta-agarofuran sesquiterpenes as modulators of P-glycoprotein-dependent multidrug resistance.

Biological evaluation, structure-activity relationships, and three-dimensional quantitative structure-activity relationship studies of dihydro-beta-agarofuran sesquiterpenes as modulators of P-glycoprotein-dependent multidrug resistance. Research Abstract Details 

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Biological evaluation, structure-activity relationships, and three-dimensional quantitative structure-activity relationship studies of dihydro-beta-agarofuran sesquiterpenes as modulators of P-glycoprotein-dependent multidrug resistance. Abstract Text:

Carolina P Reyes,Francisco ,Ivan R Torrecillas,Cristina R Mendoza,Francisco Gamarro,Isabel L Bazzocchi,Marvin J ,Leonardo Pardo,Santiago Castanys,Mercedes Campillo,Ignacio A ,

Multidrug resistance (MDR) is one of the main challenges in the chemotherapy of cancer, malaria, and other important diseases. Here, we report the inhibitory activity of a series of 76 dihydro-beta-agarofuran sesquiterpenes, tested on NIH-3T3 cells expressing the human P-glycoprotein (Pgp) multidrug transporter, to establish quantitative comparisons of their respective abilities to block the drug transport activity. The screening was performed on the basis of the ability of sesquiterpenes to modulate the intracellular accumulation of the classical Pgp substrate daunorubicin. To understand the structural basis for inhibitory activity and guide the design of more potent Pgp inhibitors, we have performed a three-dimensional quantitative structure-activity relationship model using the comparative molecular similarity indices analysis (CoMSIA). The most salient features of these requirements are in the region of the substituents at the C-2, C-3, and C-8 positions, which seem to be critical for determining the overall effectiveness of sesquiterpenes as Pgp inhibitors.

Biological evaluation, structure-activity relationships, and three-dimensional quantitative structure-activity relationship studies of dihydro-beta-agarofuran sesquiterpenes as modulators of P-glycoprotein-dependent multidrug resistance. Publishing Authors By Initials

CP Reyes,F ,IR Torrecillas,CR Mendoza,F Gamarro,IL Bazzocchi,MJ ,L Pardo,S Castanys,M Campillo,IA ,

For similar natural sciences: physics: thermodynamics research abstracts see: natural sciences: physics: thermodynamics research

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Biological evaluation, structure-activity relationships, and three-dimensional quantitative structure-activity relationship studies of dihydro-beta-agarofuran sesquiterpenes as modulators of P-glycoprotein-dependent multidrug resistance. Journal Published:

PUBLICATION TYPE: Research Support, Non-U.S. Gov

Journal: Journal of medicinal chemistry

VOLUME: 50

Page Numbers: 4808-17

Journal Abbreviation: J. Med. Chem.

ISSN: 0022-2623

DAY: 12

MONTH: 09

YEAR: 2007

Biological evaluation, structure-activity relationships, and three-dimensional quantitative structure-activity relationship studies of dihydro-beta-agarofuran sesquiterpenes as modulators of P-glycoprotein-dependent multidrug resistance. Information

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LANGUAGE: eng

NlmUniqueID: 9716531

Biological evaluation, structure-activity relationships, and three-dimensional quantitative structure-activity relationship studies of dihydro-beta-agarofuran sesquiterpenes as modulators of P-glycoprotein-dependent multidrug resistance. Keywords Mesh Terms:

KEYWORDS: Thermodynamics

MESH TERMS: pharmacology

Chemical & Substance for Abstract: Biological evaluation, structure-activity relationships, and three-dimensional quantitative structure-activity relationship studies of dihydro-beta-agarofuran sesquiterpenes as modulators of P-glycoprotein-dependent multidrug resistance. Information

Substance Name: Daunorubicin

Registry Number: 20830-81-3

Grant and Affiliation Information for Biological evaluation, structure-activity relationships, and three-dimensional quantitative structure-activity relationship studies of dihydro-beta-agarofuran sesquiterpenes as modulators of P-glycoprotein-dependent multidrug resistance.

AFFILIATION: Instituto Universitario de Bio-OrgAnica Antonio GonzAlez, Universidad de La Laguna and Instituto Canario de Investigación del CAncer, Avenida Astrofísico Francisco SAnchez, 2, 38206 La Laguna, Tenerife, Spain.

Country: United States

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MEDLINETA: J Med Chem

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