Discovery of Novel Retinoic Acid Receptor Agonists Having Potent Antiproliferative Activity in Cervical Cancer Cells
| Autor: | William W. Lamph, Alex M. Nadzan, Richard A. Heyman, Deborah L. Love, Dale E. Mais, Lin Zhang, Glenn Croston, Marcus F. Boehm |
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| Rok vydání: | 1996 |
| Předmět: |
Receptors
Retinoic Acid medicine.drug_class Retinoic acid Uterine Cervical Neoplasms Antineoplastic Agents Retinoid X receptor Retinoids chemistry.chemical_compound Drug Discovery Tumor Cells Cultured medicine Humans Retinoid Molecular Structure Retinoid X receptor alpha Chemistry Retinoid X receptor gamma Retinoic acid receptor Retinoid X Receptors Biochemistry Retinoic acid receptor alpha Cancer research Molecular Medicine Female Drug Screening Assays Antitumor Retinoid X receptor beta Cell Division Thymidine Transcription Factors |
| Zdroj: | Journal of Medicinal Chemistry. 39:2659-2663 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm960285j |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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