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Syntheses and evaluation of quinoline derivatives as novel retinoic acid receptor alpha antagonists.
One of the quinoline derivatives, 4-[5-[8-(1-methylethyl)-4-phenyl- 2-quinolinyl]-1H-2-pyrrolyl]benzoic acid (12f) shows potent RARalpha-selective antagonistic activity.
Discovery of novel and potent retinoic acid receptor alpha agonists: syntheses and evaluation of benzofuranyl-pyrrole and benzothiophenyl-pyrrole derivatives.
A series of benzofuran and benzothiophene derivatives markedly inhibited LPS-induced B-lymphocyte proliferation and exerted RARalpha selectivity in studies on retinoic acid receptor (RAR) agonists.
Syntheses and evaluation of quinoline derivatives as novel retinoic acid receptor α antagonists
Syntheses and structure-activity relationships of 5,6,7, 8-tetrahydro-5,5,8,8-tetramethyl-2-quinoxaline derivatives with retinoic acid receptor alpha agonistic activity.
A series of quinoxaline derivatives designed and synthesized showed selectivity for the RARalpha receptor and exerted highly potent cell-differentiating activity on HL-60 cells.
E6201 [(3S,4R,5Z,8S,9S,11E)-14-(Ethylamino)-8, 9,16-trihydroxy-3,4-dimethyl-3,4,9,19-tetrahydro-1H-2-benzoxacyclotetradecine-1,7(8H)-dione], a Novel Kinase Inhibitor of Mitogen-Activated Protein…
- M. Goto, Jesse C. Chow, F. Gusovsky
- Biology, ChemistryJournal of Pharmacology and Experimental…
- 1 November 2009
The in vitro activities of E6201 are characterized and it is discovered that the compound inhibits lipopolysaccharide-activated TNFα reporter activity in THP-1-33 cells with an IC50 value of 50 nM and selectively inhibits mitogen-activated protein kinase/extracellular signal-regulated kinase kinase (MEK)-1 and MEK kinase-1 in cell-free biochemical assays.
Novel retinoic acid receptor α agonists: syntheses and evaluation of pyrazole derivatives
Syntheses and structure-activity relationships of novel retinoid X receptor agonists.
- S. Hibi, K. Kikuchi, H. Yoshimura, M. Nagai, K. Tai, T. Hida
- Chemistry, BiologyJournal of medicinal chemistry
- 25 July 1998
Compound 14b (ER-35794), which possesses an ethyl substituent at the 7-position and fluorine at the 6-position of the triene moiety, is one of the most potent and selective RXR agonists reported to date.
Existence of retinoic acid-receptor-independent retinoid X-receptor-dependent pathway in myeloid cell function.
The results strongly suggest the existence of a pharmacological RXR-dependent pathway that is activated by a ligand that can bind to RXR.
Syntheses and evaluation of naphthalenyl- and chromenyl-pyrrolyl-benzoic acids as potent and selective retinoic acid receptor alpha agonists.