Synthesis and anticancer activity evaluation of 2(4-alkoxyphenyl)cyclopropyl hydrazides and triazolo phthalazines.
Bioorg Med Chem
; 18(7): 2537-48, 2010 Apr 01.
Article
em En
| MEDLINE
| ID: mdl-20303278
ABSTRACT
A series of new 2(4-alkoxyphenyl)cyclopropyl hydrazide- and triazolo-derivatives were synthesized starting from 4-hydroxycinnamic acid (1) in a clean, mild, efficient and straightforward synthetic protocol. These compounds consisting of different alkoxy substitution, phenylcyclopropyl backbone and different heterocyclic groups were evaluated for in vitro anticancer activity against 4 cell lines displaying certain levels of resistance to pro-apoptotic stimuli and 2 cell lines sensitive to pro-apoptotic compounds. Compounds 7f and 8e were most active and displaying moderate in vitro cytostatic effect through different mechanisms. Significantly, chemically modified derivatives could be obtained in order to develop novel types of compounds aiming to combat apoptosis-resistant cancers, for example, those cancers associated with dismal prognoses.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Ftalazinas
/
Hidrazinas
/
Antineoplásicos
Limite:
Humans
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article