Structural antitumoral activity relationships of synthetic chalcones

Cesar Echeverria; Juan Francisco Santibañez; Oscar Donoso-Tauda; Carlos A. Escobar; Rodrigo Ramirez-Tagle

doi:10.3390/ijms10010221

Structural antitumoral activity relationships of synthetic chalcones

Cesar Echeverria
, Juan Francisco Santibañez
, Oscar Donoso-Tauda
, Carlos A. Escobar
, Rodrigo Ramirez-Tagle

Research output: Contribution to journal › Article › peer-review

130 Scopus citations

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.

Original language	English
Pages (from-to)	221-231
Number of pages	11
Journal	International Journal of Molecular Sciences
Volume	10
Issue number	1
DOIs	https://doi.org/10.3390/ijms10010221
State	Published - Jan 2009
Externally published	Yes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Antitumoral activity
DFT
Structure-activity relationships

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10.3390/ijms10010221

Cite this

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title = "Structural antitumoral activity relationships of synthetic chalcones",

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",

author = "Cesar Echeverria and Santiba{\~n}ez, \{Juan Francisco\} and Oscar Donoso-Tauda and Escobar, \{Carlos A.\} and Rodrigo Ramirez-Tagle",

year = "2009",

month = jan,

doi = "10.3390/ijms10010221",

language = "English",

volume = "10",

pages = "221--231",

journal = "International Journal of Molecular Sciences",

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T1 - Structural antitumoral activity relationships of synthetic chalcones

AU - Echeverria, Cesar

AU - Santibañez, Juan Francisco

AU - Donoso-Tauda, Oscar

AU - Escobar, Carlos A.

AU - Ramirez-Tagle, Rodrigo

PY - 2009/1

Y1 - 2009/1

N2 - 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.

AB - 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.

KW - Antitumoral activity

KW - DFT

KW - Structure-activity relationships

UR - https://www.scopus.com/pages/publications/59649100854

U2 - 10.3390/ijms10010221

DO - 10.3390/ijms10010221

M3 - Article

C2 - 19333443

AN - SCOPUS:59649100854

SN - 1661-6596

VL - 10

SP - 221

EP - 231

JO - International Journal of Molecular Sciences

JF - International Journal of Molecular Sciences

IS - 1

ER -

Structural antitumoral activity relationships of synthetic chalcones

Abstract

UN SDGs

Keywords

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