6533b856fe1ef96bd12b308f
RESEARCH PRODUCT
Retinoid acid and analogs as potent inducers of differentiation and apoptosis. New promising chemopreventive and chemotherapeutic agents in oncology
Marinella RobertiNatale D'alessandroManlio TolomeoRiccardo RondaninFrancesco Paolo InvidiataDaniele SimoniMarcello RossiRiccardo BaruchelloStefania Grimaudosubject
chemistry.chemical_compoundchemistryBiochemistryApoptosisGeneral Chemical EngineeringWittig reactionRetinoic acidCytotoxic T cellInducerBiological activityGeneral ChemistryLeukemia cell linedescription
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.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2001-09-01 |