Bioorganic & medicinal chemistry, 2010-05, Vol.18 (9), p.3159-3168
2010
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Details
- Autor(en) / Beteiligte
- Titel
- Structure–activity relationships of bioisosteric replacement of the carboxylic acid in novel androgen receptor pure antagonists
- Ist Teil von
- Bioorganic & medicinal chemistry, 2010-05, Vol.18 (9), p.3159-3168
- Ort / Verlag
- Amsterdam: Elsevier Ltd
- Erscheinungsjahr
- 2010
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- We designed and synthesized novel AR pure antagonists for the treatment of hormone refractory prostate cancer. CH4933468 with a sulfonamide side chain showed higher activities than lead compound 5. A series of 5,5-dimethylthiohydantoin derivatives were synthesized and evaluated for androgen receptor pure antagonistic activities for the treatment of hormone refractory prostate cancer. CH4933468 (32d) with a sulfonamide side chain not only exhibited antagonistic activity with no agonistic activity in the reporter gene assay but also inhibited the growth of bicalutamide-resistant cell lines. This compound also inhibited tumor growth of the LNCaP xenograft in mice dose-dependently.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0968-0896eISSN: 1464-3391DOI: 10.1016/j.bmc.2010.03.036Titel-ID: cdi_proquest_miscellaneous_733933677
- Format
- –
- Schlagworte
- Androgen Antagonists - chemical synthesis, Androgen Antagonists - chemistry, Androgen Antagonists - pharmacology, Androgen receptor, Animals, Antineoplastic agents, Antineoplastic Agents, Hormonal - chemical synthesis, Antineoplastic Agents, Hormonal - chemistry, Antineoplastic Agents, Hormonal - pharmacology, Bioisostere, Biological and medical sciences, Carboxylic Acids - chemical synthesis, Carboxylic Acids - chemistry, Carboxylic Acids - pharmacology, Cell Line, Tumor, Dose-Response Relationship, Drug, General aspects, Hormones. Endocrine system, Inhibitory Concentration 50, Male, Medical sciences, Mice, Mice, SCID, Molecular Structure, Nitriles - chemical synthesis, Nitriles - chemistry, Nitriles - therapeutic use, Pharmacology. Drug treatments, Prostate cancer, Prostatic Neoplasms - drug therapy, Pure antagonist, Sulfonamide, Sulfonamides - chemical synthesis, Sulfonamides - chemistry, Sulfonamides - therapeutic use, Thiohydantoins - chemical synthesis, Thiohydantoins - chemistry, Thiohydantoins - pharmacology, Urinary system, Xenograft Model Antitumor Assays