Synthesis 2016; 48(22): 3907-3916
DOI: 10.1055/s-0035-1562497
paper
© Georg Thieme Verlag Stuttgart · New York

Multicomponent Approach to Bioactive Peptide–Ecdysteroid Conjugates: Creating Diversity at C6 by Means of the Ugi Reaction

Giordano Lesma
a   Dipartimento di Chimica, Università di Milano, via Golgi 19, Milano, 20133, Italy
,
Andrea Luraghi
a   Dipartimento di Chimica, Università di Milano, via Golgi 19, Milano, 20133, Italy
,
Giulia Rainoldi
a   Dipartimento di Chimica, Università di Milano, via Golgi 19, Milano, 20133, Italy
,
Elena Mattiuzzo
b   Dipartimento di salute della Donna e del Bambino, Università di Padova, Via Giustiniani 3, Padova, 35128, Italy   Email: alessandra.silvani@unimi.it
,
Roberta Bortolozzi
b   Dipartimento di salute della Donna e del Bambino, Università di Padova, Via Giustiniani 3, Padova, 35128, Italy   Email: alessandra.silvani@unimi.it
,
Giampietro Viola
b   Dipartimento di salute della Donna e del Bambino, Università di Padova, Via Giustiniani 3, Padova, 35128, Italy   Email: alessandra.silvani@unimi.it
,
Alessandra Silvani*
a   Dipartimento di Chimica, Università di Milano, via Golgi 19, Milano, 20133, Italy
› Author Affiliations
Further Information

Publication History

Received: 16 March 2016

Accepted after revision: 17 May 2016

Publication Date:
01 July 2016 (online)


Abstract

An efficient multicomponent protocol has been developed to access two different kinds of peptide–ecdysteroid conjugates. The approach exploits the reactivity of the 6-keto-7-ene group of 20-OH-ecdysone, allowing the unprecedented preparation of 6-amino and 6-isocyanide derivatives. The ecdysteroid derivatives were further employed in the Ugi reaction, together with formaldehyde and various structurally diverse carboxylic acids, isocyanides and amines, to afford a small family of potential multidrug-resistance modulators.

Supporting Information