RESUMO
A range of 11 derivatives of flavone-8-acetic acid (FAA) in which the structure has been substantially altered in different ways have been prepared and their anti-tumour activity evaluated in vitro against a panel of human and murine tumour cell lines and in vivo against MAC 15A. The generally poor activity observed shows that the basic structure cannot be altered much without destroying the activity.
Assuntos
Antineoplásicos/síntese química , Flavonoides/síntese química , Animais , Antineoplásicos/farmacologia , Flavonoides/farmacologia , Humanos , Camundongos , Relação Estrutura-Atividade , Células Tumorais CultivadasRESUMO
A range of 14 derivatives of flavone-8-acetic acid (FAA) with a heterocyclic substituent in place of the 2-phenyl group have been prepared and their anti-tumour activity evaluated in vitro against a panel of human and murine tumour cell lines and in vivo against MAC 15A. Some of the compounds, notably 2c,d and s, showed significant in vivo activity and these require further studies in order to evaluate their potential for development.
Assuntos
Antineoplásicos/síntese química , Flavonoides/síntese química , Flavonoides/farmacologia , Compostos Heterocíclicos/síntese química , Animais , Antineoplásicos/farmacologia , Compostos Heterocíclicos/farmacologia , Humanos , Camundongos , Estrutura Molecular , Neoplasias Experimentais/tratamento farmacológico , Células Tumorais CultivadasRESUMO
A range of 18 derivatives of flavone-8-acetic acid (FAA) with substituents on the 2-phenyl group have been prepared and their anti-tumour activity evaluated in vitro against a panel of human and murine tumour cell lines and in vivo against MAC 15A. There was no clear-cut relationship between in vitro and in vivo activity but the activity in each situation was found to be very sensitive to the precise substitution pattern with closely related isomers giving widely different activities. Some of the compounds, notably 10b,c,j, and r, were active in vivo and these require further studies in order to evaluate their potential for development.
