Search Results - "Rico, Alice"
-
1
Antitumor Properties of RAF709, a Highly Selective and Potent Inhibitor of RAF Kinase Dimers, in Tumors Driven by Mutant RAS or BRAF
Published in Cancer research (Chicago, Ill.) (15-03-2018)“…Resistance to the RAF inhibitor vemurafenib arises commonly in melanomas driven by the activated BRAF oncogene. Here, we report antitumor properties of RAF709,…”
Get full text
Journal Article -
2
Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: Synthesis and SAR studies
Published in Bioorganic & medicinal chemistry letters (15-08-2006)“…A series of 2-pyrimidyl-5-amidothiophenes has been synthesized and evaluated for AKT inhibition. Compound 2aa is a potent AKT inhibitor and showed cellular…”
Get full text
Journal Article -
3
Synthesis and Antibacterial Activity of Novel C12 Vinyl Ketolides
Published in Journal of medicinal chemistry (09-03-2006)“…A novel series of C12 vinyl erythromycin derivatives have been discovered which exhibit in vitro and in vivo potency against key respiratory pathogens. The C12…”
Get full text
Journal Article -
4
Synthesis and antibacterial activity of C12 des-methyl ketolides
Published in Bioorganic & medicinal chemistry letters (01-09-2006)“…Synthesis of C(12) des-methyl ketolide is developed featuring an intramolecular epoxide formation/elimination process to establish the C(12) stereocenter…”
Get full text
Journal Article -
5
Antihydrophobic Solvent Effects: An Experimental Probe for the Hydrophobic Contribution to Enzyme−Inhibitor Binding
Published in Journal of the American Chemical Society (17-04-2002)“…The hydrophobic component to the binding affinities of one acyclic phosphinate (4) and three macrocyclic phosphonamidate inhibitors (1−3) to the zinc peptidase…”
Get full text
Journal Article -
6
Design and Discovery of N‑(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic
Published in Journal of medicinal chemistry (12-03-2020)“…Direct pharmacological inhibition of RAS has remained elusive, and efforts to target CRAF have been challenging due to the complex nature of RAF signaling,…”
Get full text
Journal Article -
7
Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria
Published in Journal of medicinal chemistry (23-07-2020)“…Since their discovery over 5 decades ago, quinolone antibiotics have found enormous success as broad spectrum agents that exert their activity through dual…”
Get full text
Journal Article -
8
Application of Virtual Screening to the Identification of New LpxC Inhibitor Chemotypes, Oxazolidinone and Isoxazoline
Published in Journal of medicinal chemistry (25-10-2018)“…This report summarizes the identification and synthesis of novel LpxC inhibitors aided by computational methods that leveraged numerous crystal structures…”
Get full text
Journal Article -
9
Synthesis and Structure–Activity Relationship of Tetra-Substituted Cyclohexyl Diol Inhibitors of Proviral Insertion of Moloney Virus (PIM) Kinases
Published in Journal of medicinal chemistry (10-12-2020)“…Overexpression of PIM 1, 2, and 3 kinases is frequently observed in many malignancies. Previously, we discovered a potent and selective pan-PIM kinase…”
Get full text
Journal Article -
10
Design and Discovery of N‑(2-Methyl-5′-morpholino-6′-((tetrahydro‑2H‑pyran-4-yl)oxy)-[3,3′-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers
Published in Journal of medicinal chemistry (22-06-2017)“…RAS oncogenes have been implicated in >30% of human cancers, all representing high unmet medical need. The exquisite dependency on CRAF kinase in KRAS mutant…”
Get full text
Journal Article -
11
Abstract DDT01-04: Pharmacological profile and anti-tumor properties of LXH254, a highly selective RAF kinase inhibitor
Published in Cancer research (Chicago, Ill.) (01-07-2018)“…Abstract The mitogen-activated protein kinase (MAPK) signaling pathway is frequently activated in human cancers due to genetic alterations that can occur at…”
Get full text
Journal Article -
12
Abstract 330: Development of a highly selective BCRAF kinase inhibitor that exhibits antitumor activities in RAS and BRAF mutant tumors with minimal paradoxical activation
Published in Cancer research (Chicago, Ill.) (15-07-2016)“…The mitogen-activated protein kinase (MAPK) signaling pathway is frequently activated in human cancers due to genetic alterations that can occur at multiple…”
Get full text
Journal Article -
13
Abstract 330: Development of a highly selective B/CRAF kinase inhibitor that exhibits antitumor activities in RAS and BRAF mutant tumors with minimal paradoxical activation
Published in Cancer research (Chicago, Ill.) (15-07-2016)“…Abstract The mitogen-activated protein kinase (MAPK) signaling pathway is frequently activated in human cancers due to genetic alterations that can occur at…”
Get full text
Journal Article -
14
Design, Structure–Activity Relationship, and in Vivo Characterization of the Development Candidate NVP-HSP990
Published in Journal of medicinal chemistry (13-11-2014)“…Utilizing structure-based drug design, a novel dihydropyridopyrimidinone series which exhibited potent Hsp90 inhibition, good pharmacokinetics upon oral…”
Get full text
Journal Article -
15
Synthesis and antibacterial activity of C 12 des-methyl ketolides
Published in Bioorganic & medicinal chemistry letters (01-09-2006)“…Synthesis of C 12 des-methyl ketolides is developed featuring an intramolecular epoxide formation/elimination process to establish the C 12 stereocenter. These…”
Get full text
Journal Article -
16
Synthesis and Antibacterial Activity of Novel C 12 Vinyl Ketolides
Published in Journal of medicinal chemistry (09-03-2006)Get full text
Journal Article -
17
Synthesis and antibacterial activity of C sub(12) des-methyl ketolides
Published in Bioorganic & medicinal chemistry letters (01-09-2006)“…Synthesis of C sub(12) des-methyl ketolide is developed featuring an intramolecular epoxide formation/elimination process to establish the C sub(12)…”
Get full text
Journal Article