Discovery of Novel Retinoic Acid Receptor Agonists Having Potent Antiproliferative Activity in Cervical Cancer Cells

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, AL...

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Bibliographic Details
Published in:	Journal of medicinal chemistry Vol. 39; no. 14; pp. 2659 - 2663
Main Authors:	Zhang, Lin, Nadzan, Alex M, Heyman, Richard A, Love, Deborah L, Mais, Dale E, Croston, Glenn, Lamph, William W, Boehm, Marcus F
Format:	Journal Article
Language:	English
Published:	Washington, DC American Chemical Society 05-07-1996
Subjects:	Antineoplastic agents Antineoplastic Agents - pharmacology Biological and medical sciences Cell Division - drug effects Drug Screening Assays, Antitumor Female General aspects Humans Medical sciences Molecular Structure Pharmacology. Drug treatments Receptors, Retinoic Acid - agonists Receptors, Retinoic Acid - metabolism Retinoid X Receptors Retinoids - chemistry Retinoids - pharmacology Thymidine - metabolism Transcription Factors - metabolism Tumor Cells, Cultured Uterine Cervical Neoplasms Antineoplastic agent Cell proliferation Stereoisomer Conjugated polyenic compound Aliphatic compound Retinoids In vitro Biological activity Biological fixation Carboxylic acid Established cell line Benzenic compound Inhibitor Chemical synthesis Carotenoid Retinoic acid Tumor cell Biological receptor
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Summary:	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.
Bibliography:	Abstract published in Advance ACS Abstracts, June 15, 1996. istex:6DEE7712F216B4639CDF361EA5686E8E303B3E4F ark:/67375/TPS-3X4KRX7V-X ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm960285j