Retinoic acid and analogs as potent inducers of differentiation and apoptosis. New promising chemopreventive and chemotherapeutic agents in oncology

Author:

Simoni Daniele1,Rondanin Riccardo1,Baruchello Riccardo1,Roberti Marinella2,Rossi Marcello1,Grimaudo Stefania3,D'Alessandro Natale4,Invidiata Francesco Paolo5,Tolomeo Manlio3

Affiliation:

1. 1Dipartimento di Scienze Farmaceutiche, Via Fossato di Mortara 17-19, Università di Ferrara, 44100 Ferrara, Italy

2. 2Dipartimento di Scienze Farmaceutiche, Università di Bologna, Italy

3. 3Divisione di Ematologia e Servizio AIDS, Policlinico di Palermo, Italy

4. 4Dipartimento di Scienze Farmacologiche, Università di Palermo, Italy

5. 5Dipartimento Farmacochimico Tossicologico e Biologico, Università di Palermo, Italy

Abstract

In this report we will describe the preparation and the biological activity of a novel class of heterocyclic arotinoids endowed with potent cytotoxic and apoptotic acitivity. Structure­activity relationship studies revealed that the different stereochemistry at the C9 double bond of retinoids seems associated with a different biological activity: potent apoptotic activity for the cis-isomers, whereas differentiating activity for the trans structures. An interesting modified Wittig procedure that allows easily to arotinoids will also be described. The substitution of the alkenyl portion with a more flexible oxymethyl or aminomethyl moiety gave compounds with poor activity, whereas isoxazole-bridged arotinoids allowed compounds active also on multidrug-resistant (MDR) leukemia cell lines.

Publisher

Walter de Gruyter GmbH

Subject

General Chemical Engineering,General Chemistry

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