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2005
Vitamins
U 0900
16- 197
9-cis-Retinoic Acid Analogues with Bulky Hydrophobic Rings: New RXR-Selective Agonists. — A stereoselective approach to retinoids (I) is achieved via Stille
cross-coupling and Horner—Wadsworth—Emmons reaction. The structure-based predictions are confirmed by transactivation studies and rexinoid-dependent leukemia cell
differentiation assays. Retinoids (I) exhibit selective binding and transactivation of
RXR, devoid of significant RAR activation. The combination of TTNPB and either (Ia)
or (Ib) strongly induces cell differentiation revealing a highly synergistic action of the
types of ligands. — (ALVAREZ, R.; VEGA, M. J.; KAMMERER, S.; ROSSIN, A.;
GERMAIN, P.; GRONEMEYER, H.; DE LERA*, A. R.; Bioorg. Med. Chem. Lett.
14 (2004) 24, 6117-6122; Dep. Quim. Org., Univ. Vigo, E-36200 Vigo, Spain; Eng.)
— H. Hoennerscheid
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