Synthesis and biological activity of retinoic acid receptor-alpha specific amides

  • Bioorg Med Chem Lett. 2002 Nov 4;12(21):3145-8. doi: 10.1016/s0960-894x(02)00647-9.
Richard L Beard  1 ,  Tien T Duong ,  Min Teng ,  Elliott S Klein ,  Andrew M Standevan ,  Roshantha A S Chandraratna
Affiliations
  • 1. Retinoid Research, Department of Chemistry, Allergan Inc., Irvine, CA 92623-9534, USA. [email protected]
PMID: 12372520 DOI: 10.1016/s0960-894x(02)00647-9
Abstract

Retinoids are analogues of all-trans-retinoic acid, a powerful hormone that mediates many fundamental biological processes. Cancer and Other serious hyperproliferative diseases are attractive therapeutic targets for retinoids, but the therapeutic use of retinoids is limited due to severe toxicity. We report here the design of retinoid receptor-alpha specific ligands with growth inhibitory activity in breast Cancer cell lines, and which do not cause the cutaneous toxicity associated with the currently available nonselective retinoid agonists.

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