1454306-41-2Relevant academic research and scientific papers
Synthesis and biological evaluation of a post-synthetically modified Trp-based diketopiperazine
Preciado, Sara,Mendive-Tapia, Lorena,Torres-Garcia, Carolina,Zamudio-Vazquez, Rubi,Soto-Cerrato, Vanessa,Perez-Tomas, Ricardo,Albericio, Fernando,Nicolas, Ernesto,Lavilla, Rodolfo
, p. 1171 - 1174 (2013/08/23)
A series of C2-arylated analogues of the diketopiperazine brevianamide F has been synthesized using a mild Pd-catalyzed CH-activation procedure. Biological evaluation of the new derivatives in different cell lines shows that this modification is responsible for the remarkable change in activity, turning a mild antibiotic and antifungal natural product (brevianamide F) into novel antitumoral compounds. Furthermore, the approach stated represents a new straightforward and versatile methodology with promising applications in peptidomimetics and medicinal chemistry.
