Cargando…

Biaryl Sulfonamides Based on the 2-Azabicycloalkane Skeleton—Synthesis and Antiproliferative Activity

In a search for new, selective antitumor agents, we prepared a series of sulfonamides built on bicyclic scaffolds of 2-azabicyclo(2.2.1)heptane and 2-azabicyclo(3.2.1)octane. To this end, aza-Diels–Alder cycloadducts were converted into amines bearing 2-azanorbornane or a bridged azepane skeleton; t...

Descripción completa

Detalles Bibliográficos
Autores principales: Iwan, Dominika, Kamińska, Karolina, Wojaczyńska, Elżbieta, Psurski, Mateusz, Wietrzyk, Joanna, Daszkiewicz, Marek
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7664408/
https://www.ncbi.nlm.nih.gov/pubmed/33172089
http://dx.doi.org/10.3390/ma13215010
Descripción
Sumario:In a search for new, selective antitumor agents, we prepared a series of sulfonamides built on bicyclic scaffolds of 2-azabicyclo(2.2.1)heptane and 2-azabicyclo(3.2.1)octane. To this end, aza-Diels–Alder cycloadducts were converted into amines bearing 2-azanorbornane or a bridged azepane skeleton; their treatment with sulfonyl chlorides containing biaryl moieties led to the title compounds. The study of antiproliferative activity of the new agents showed that some of them inhibited the growth of chosen cell lines with the IC(50) values comparable with cisplatin, and some derivatives were found considerably less toxic for nonmalignant cells.