178688-27-2Relevant academic research and scientific papers
Synthesis and characterization of a highly potent and selective isotopically labeled retinoic acid receptor ligand, ALRT1550
Bennani, Youssef L.,Marron, Kristin S.,Mais, Dale E.,Flatten, Karen,Nadzan, Alex M.,Boehm, Marcus F.
, p. 543 - 550 (2007/10/03)
The syntheses of two labeled homologues of (2E,4E,6E)-7-(3,5-di-tert- butylphenyl)-3-methylocta-2,4,6-trienoic acid (ALRT1550, 2), [13CD3]ALRT1550 (3) and [3H]ALRT1550 (4), are described in this report. ALRT1550 is an exceptionally potent antiproliferative agent which is currently in phase I/II clinical trials for acute chemotherapy. Both homologues were prepared from commercially available 3,5-di-tert-butylbenzoic acid. Homologue [13CD3]ALRT1550 was labeled at the 7-position of the trienoic acid chain via addition of [13CD3]MgI to a Weinreb amide precursor. The preparation of [3H]ALRT1550 utilized novel methodology to synthesize a sterically hindered and site-specific tritium-labeled tert- butyl group. Saturation binding and Scatchard analysis of this ligand at the retinoic acid receptors are also described, along with competition binding (K(i)) values for a series of known retinoids using [3H]ALRT1550 or [3H]ATRA as the labeled probes.
Trienoic retinoid compounds and methods
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, (2008/06/13)
Novel trienoic compounds having activity for retinoic acid receptors and retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such compounds and methods for their use.
Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells
Zhang, Lin,Nadzan, Alex M.,Heyman, Richard A.,Love, Deborah L.,Mais, Dale E.,Croston, Glenn,Lamph, William W.,Boehm, Marcus F.
, p. 2659 - 2663 (2007/10/03)
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-butylphen
