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- Title
Synthesis of Indole-Derived Allocolchicine Congeners through Pd-Catalyzed Intramolecular C-H Arylation Reaction.
- Authors
Sitnikov, Nikolay S.; Kokisheva, Antonina S.; Fukin, Georgy K.; Neudörfl, Jörg‐Martin; Sutorius, Hannah; Prokop, Aram; Fokin, Valery V.; Schmalz, Hans‐Günther; Fedorov, Alexey Yu.
- Abstract
The synthesis of several new heterocyclic structural analogs of the natural antimitotic agent allocolchicine is reported. As a key step an intramolecular Pd-catalyzed C--H arylation reaction was used to close the seven-membered ring fused with two electron-rich aryl fragments. The stereostructure of the target compounds was determined by X-ray crystal analysis. The primary biological assessment of the synthesized compounds was carried out on human lymphoma cells. Several allocolchicinoids were determined to possess antiproliferative and apoptosis-inducing activity in the micromolar concentration range.
- Subjects
CHEMICAL synthesis; HETEROCYCLIC compounds; ANTIMITOTIC agents; PALLADIUM catalysts; APOPTOSIS
- Publication
European Journal of Organic Chemistry, 2014, Vol 2014, Issue 29, p6481
- ISSN
1434-193X
- Publication type
Article
- DOI
10.1002/ejoc.201402850