Novel approach to bis(indolyl)methanes: de novo synthesis of 1-hydroxyiminomethyl derivatives with anti-cancer properties. | - CCMAR -

Journal Article

TitleNovel approach to bis(indolyl)methanes: de novo synthesis of 1-hydroxyiminomethyl derivatives with anti-cancer properties.
Publication TypeJournal Article
AuthorsGrosso, C, Cardoso, ALúcia, Lemos, A, Varela, J, Rodrigues, MJoão, Custódio, L, Barreira, L, Melo, TMVDPinh
Year of Publication2015
JournalEur J Med Chem
Volume93
Date Published2015 Mar 26
Pagination9-15
ISSN1768-3254
KeywordsAnimals, Antineoplastic Agents, Cell Culture Techniques, Cell Line, Tumor, Cell Survival, Cycloaddition Reaction, Drug Design, Humans, Indoles, Macrophages, Microglia, Oximes, Structure-Activity Relationship
Abstract

A versatile and broad range approach to previously unknown bis(indolyl)methane oximes based on two consecutive hetero Diels-Alder cycloaddition reactions of electrophilic conjugated nitrosoalkenes with indoles is disclosed. The cytotoxic properties and selectivity of some adducts against several human cancer cell lines pointing to a promising role in the development of anti-tumoural drugs, in particular for leukaemia and lymphoma.

DOI10.1016/j.ejmech.2015.01.050
Sapientia

http://www.ncbi.nlm.nih.gov/pubmed/25644672?dopt=Abstract

Alternate JournalEur J Med Chem
PubMed ID25644672