Design, Synthesis and Antiproliferative Activity of Novel 2-Substituted-4-amino-6-halogenquinolines

Two series of novel 2-substituted-4-amino-6-halogenquinolines 8a–l and 13a–h were designed, synthesized and evaluated for their antiproliferative activity against H-460, HT-29, HepG2 and SGC-7901 cancer cell lines in vitro. The pharmacological results indicated that most compounds with 2-arylvinyl s...

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Detalles Bibliográficos
Autores principales: Jiang, Nan, Zhai, Xin, Li, Ting, Liu, Difa, Zhang, Tingting, Wang, Bin, Gong, Ping
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2012
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268466/
https://www.ncbi.nlm.nih.gov/pubmed/22592090
http://dx.doi.org/10.3390/molecules17055870
Descripción
Sumario:Two series of novel 2-substituted-4-amino-6-halogenquinolines 8a–l and 13a–h were designed, synthesized and evaluated for their antiproliferative activity against H-460, HT-29, HepG2 and SGC-7901 cancer cell lines in vitro. The pharmacological results indicated that most compounds with 2-arylvinyl substituents exhibited good to excellent antiproliferative activity. Among them, compound 8e was a considered promising lead for further structural modifications with IC(50) values of 0.03 μM, 0.55 μM, 0.33 μM and 1.24 μM, which was 2.5- to 186-fold more active than gefitinib and compound 1.

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