Structural Antitumoral Activity Relationships of Synthetic Chalcones

doi:10.3390/ijms10010221

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Int. J. Mol. Sci. 2009, 10(1), 221-231; doi:10.3390/ijms10010221

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Structural Antitumoral Activity Relationships of Synthetic Chalcones

Cesar Echeverria¹, Juan Francisco Santibañez¹, Oscar Donoso-Tauda², Carlos A. Escobar² and Rodrigo Ramirez-Tagle^2,*

¹ Instituto de Nutrición y Tecnología de los Alimentos, Universidad de Chile, El Líbano 5524, Macul, Santiago, Chile ² Universidad Andres Bello, Departamento de Ciencias Químicas, Av. República 275, Santiago, Chile

* Author to whom correspondence should be addressed.

Received: 30 September 2008; in revised form: 31 December 2008 / Accepted: 4 January 2009 / Published: 9 January 2009

(This article belongs to the Section Biochemistry, Molecular Biology and Biophysics)

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Abstract: Relationships between the structural characteristic of synthetic chalcones and their antitumoral activity were studied. Treatment of HepG2 cells for 24 h with synthetic 2’-hydroxychalcones resulted in apoptosis induction and dose-dependent inhibition of cell proliferation. The calculated reactivity indexes and the adiabatic electron affinities using the DFT method including solvent effects, suggest a structure-activity relationship between the Chalcones structure and the apoptosis in HepG2 cells. The absence of methoxy substituents in the B ring of synthetic 2’-hydroxychalcones, showed the mayor structure-activity pattern along the series.

Keywords: Antitumoral activity; DFT; structure-activity relationships

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MDPI and ACS Style

Echeverria, C.; Santibañez, J.F.; Donoso-Tauda, O.; Escobar, C.A.; Ramirez-Tagle, R. Structural Antitumoral Activity Relationships of Synthetic Chalcones. Int. J. Mol. Sci. 2009, 10, 221-231.

AMA Style

Echeverria C, Santibañez JF, Donoso-Tauda O, Escobar CA, Ramirez-Tagle R. Structural Antitumoral Activity Relationships of Synthetic Chalcones. International Journal of Molecular Sciences. 2009; 10(1):221-231.

Chicago/Turabian Style

Echeverria, Cesar; Santibañez, Juan Francisco; Donoso-Tauda, Oscar; Escobar, Carlos A.; Ramirez-Tagle, Rodrigo. 2009. "Structural Antitumoral Activity Relationships of Synthetic Chalcones." Int. J. Mol. Sci. 10, no. 1: 221-231.

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