Régis Millet - Academia.edu (original) (raw)
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Papers by Régis Millet
Bioorganic & Medicinal Chemistry, 2002
Exploration of SAR around dual NK 1 /NK 2 antagonist Cbz-Gly-Leu-Trp-OBzl(CF 3 ) 2 and its deriva... more Exploration of SAR around dual NK 1 /NK 2 antagonist Cbz-Gly-Leu-Trp-OBzl(CF 3 ) 2 and its derivatives disclosed the essential requirements for more potent dual NK 1 /NK 2 binding. We report here the synthesis and the biological properties of a novel series of indolizine including pharmacophoric elements. #
J Med Chem, 2004
We recently described a novel series of CA 1 A 2 X peptidomimetics as farnesyl transferase inhibi... more We recently described a novel series of CA 1 A 2 X peptidomimetics as farnesyl transferase inhibitors (FTIs). These compounds possess an N-(4-piperidinyl)benzamide scaffold mimicking A 1 A 2 residue. Extensive exploration of structure-activity relationships revealed that replacement of cysteine by substituted benzylimidazoles provided nanomolar FTIs with in vitro activities (18e, IC 50 ) 4.60 nM on isolated enzyme, EC 50 ) 20.0 nM for growth inhibition on a tumor cell line). The molecular docking of 18e and 19e in the active site of the enzyme provided details of key interactions with the protein and showed that the methionine or phenylalanine residue fits into the aryl binding site.
Letters in Organic Chemistry, 2010
ABSTRACT Reaction between aryl 1,3-diketoesters 2a-e and hydroxylamine hydrochloride has been inv... more ABSTRACT Reaction between aryl 1,3-diketoesters 2a-e and hydroxylamine hydrochloride has been investigated under different experimental conditions. Whereas acid conditions gave principally 3,5-isoxazole esters (3a-e), reactions under neutral and basic conditions led to different 4,5 and 2,3-dihydro-hydroxy-isoxazoles 4a-e and 5a-e.
Bioorganic & Medicinal Chemistry, 2002
Exploration of SAR around dual NK 1 /NK 2 antagonist Cbz-Gly-Leu-Trp-OBzl(CF 3 ) 2 and its deriva... more Exploration of SAR around dual NK 1 /NK 2 antagonist Cbz-Gly-Leu-Trp-OBzl(CF 3 ) 2 and its derivatives disclosed the essential requirements for more potent dual NK 1 /NK 2 binding. We report here the synthesis and the biological properties of a novel series of indolizine including pharmacophoric elements. #
J Med Chem, 2004
We recently described a novel series of CA 1 A 2 X peptidomimetics as farnesyl transferase inhibi... more We recently described a novel series of CA 1 A 2 X peptidomimetics as farnesyl transferase inhibitors (FTIs). These compounds possess an N-(4-piperidinyl)benzamide scaffold mimicking A 1 A 2 residue. Extensive exploration of structure-activity relationships revealed that replacement of cysteine by substituted benzylimidazoles provided nanomolar FTIs with in vitro activities (18e, IC 50 ) 4.60 nM on isolated enzyme, EC 50 ) 20.0 nM for growth inhibition on a tumor cell line). The molecular docking of 18e and 19e in the active site of the enzyme provided details of key interactions with the protein and showed that the methionine or phenylalanine residue fits into the aryl binding site.
Letters in Organic Chemistry, 2010
ABSTRACT Reaction between aryl 1,3-diketoesters 2a-e and hydroxylamine hydrochloride has been inv... more ABSTRACT Reaction between aryl 1,3-diketoesters 2a-e and hydroxylamine hydrochloride has been investigated under different experimental conditions. Whereas acid conditions gave principally 3,5-isoxazole esters (3a-e), reactions under neutral and basic conditions led to different 4,5 and 2,3-dihydro-hydroxy-isoxazoles 4a-e and 5a-e.