Zhang L, Nadzan A M, Heyman R A, Love D L, Mais D E, Croston G, Lamph W W, Boehm M F
Department of Retinoid Chemistry, Ligand Pharmaceuticals, Inc., San Diego, California 92121, USA.
J Med Chem. 1996 Jul 5;39(14):2659-63. doi: 10.1021/jm960285j.
Retinoic acid receptor (RAR) active retinoids have proven therapeutically useful for treating certain cancers and dermatological diseases. Herein, we describe the discovery of two new RAR active trienoic acid retinoids, (2E,4E,6E)-7-(3,5-di-tert-butylphenyl)-3-methylocta-2, 4,6-trienoic acid (10a, ALRT1550) and (2E,4E,6Z)-7-(3,5-di-tert-butylphenyl)-3-methylocta-2, 4,6-trienoic acid (10b, LG100567). ALRT1550 is a RAR selective retinoid which exhibits exceptional potency in both competitive binding and cotransfection assays. Moreover, it is the most potent antiproliferative retinoid described to date and thus has implications for the treatment of certain cancers. LG100567 is a potent panagonist which activates both RARs and retinoid X receptors.
