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azastene

inhibitor of ovarian & adrenal steroidogenesis in rats; progesterone antagonist
Also Known As:
Win 17,625; Win-17625; isoxazol; (17 beta)-4,4,17-trimethylandrosta-2,5-diene(3,2-d)isoxazol-17-ol
Networked: 44 relevant articles (4 outcomes, 5 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Experts

1. Wang, Yong-Xiang: 4 articles (12/2015 - 03/2012)
2. Gong, Nian: 3 articles (12/2015 - 03/2012)
3. Wang, Chao: 2 articles (10/2022 - 01/2020)
4. Xu, Yong: 2 articles (10/2022 - 01/2020)
5. Zhang, Cheng: 2 articles (10/2022 - 01/2020)
6. Zhang, Yan: 2 articles (10/2022 - 01/2020)
7. Averina, Elena B: 2 articles (05/2022 - 05/2022)
8. Gracheva, Yulia A: 2 articles (05/2022 - 05/2022)
9. Grishin, Yuri K: 2 articles (05/2022 - 05/2022)
10. Milaeva, Elena R: 2 articles (05/2022 - 05/2022)

Related Diseases

1. Neoplasms (Cancer)
01/01/2020 - "Discovery and optimization of novel N-benzyl-3,6-dimethylbenzo[d]isoxazol-5-amine derivatives as potent and selective TRIM24 bromodomain inhibitors with potential anti-cancer activities."
11/18/2009 - "The present data showed that a novel synthesized compound, N-acetyl-N-(4-(4-methoxyphenyl-3-(3,4,5-trimethoxyphenyl)isoxazol-5-yl)acetamide (XN05), exhibited potent antitumor activity against various cancer cells in vitro. "
11/01/2012 - "Subcutaneous and intrathecal injection of the specific DAAO inhibitor CBIO (5-chloro-benzo[d]isoxazol-3-ol) blocked mechanical allodynia in a dose- and time-dependent manner in tumor-bearing rats, with maximum inhibition of 40-50 %. "
10/01/1986 - "Based on our recent findings that danazol, an isoxazol derivative of ethinyltestosterone, has a profound growth-inhibitory effect on an established human endometrial adenocarcinoma cell line, the effects of danazol on cancer cells from human endometrial adenocarcinomas obtained by hysterectomy were investigated in the present study. "
05/01/2022 - "The cytotoxicity of 3-methyl-N-[5-methyl-3-(3,4,5-trimethoxyphenyl)isoxazol-4-yl]benzamide (1ab) to the androgen-sensitive human prostate adenocarcinoma cancer cell line LNCaP (IC50  = 0.301 µM) was approximately one order of magnitude higher than that to the conditionally normal cells lines WI-26 VA4 (IC50  = 2.26 µM) and human umbilical vein endothelial cells (IC50  = 5.58 µM) and significantly higher than that to primary fibroblasts (IC50  > 75 µM)."
2. Prostatic Neoplasms (Prostate Cancer)
10/01/2017 - "Inhibition of Androgen Receptor Function and Level in Castration-Resistant Prostate Cancer Cells by 2-[(isoxazol-4-ylmethyl)thio]-1-(4-phenylpiperazin-1-yl)ethanone."
10/01/2017 - "Through a high-throughput/high-content screening of a 220,000-member small molecule library, we have previously identified 2-[(isoxazol-4-ylmethyl)thio]-1-(4-phenylpiperazin-1-yl)ethanone (IMTPPE) (SID 3712502) as a novel small molecule capable of inhibiting AR transcriptional activity and protein level in C4-2 prostate cancer cells. "
04/25/2014 - "The preclinical profiles of two most potent compounds of our recently published cycloalkane[d]isoxazole pharmacophore-based androgen receptor (AR) modulators, FL442 (4-(3a,4,5,6,7,7a-hexahydro-benzo[d]isoxazol-3-yl)-2-(trifluoromethyl)benzonitrile) and its nitro analog FL425 (3-(4-nitro-3-(trifluoromethyl)phenyl)-3a,4,5,6,7,7a-hexahydrobenzo[d]isoxazole), were explored to evaluate their druggability for the treatment of AR dependent prostate cancer. "
07/26/2012 - "The most potent compound, 4-(3a,4,5,6,7,7a-hexahydrobenzo[d]isoxazol-3-yl)-2-(trifluoromethyl)benzonitrile (6a), exhibits antiandrogenic activity significantly greater than that of the most widely used antiandrogenic prostate cancer drugs bicalutamide (1) and hydroxyflutamide (2) in reporter gene assays measuring the transcriptional activity of AR (decreasing approximately 90% of the total AR activity) and in competitive AR ligand-binding assays (showing over four times higher potency to inhibit radioligand binding in comparison to bicalutamide). "
3. Rheumatoid Arthritis
4. Autoimmune Diseases (Autoimmune Disease)
5. Pain (Aches)

Related Drugs and Biologics

1. Leflunomide (Arava)
2. Immunomodulating Agents
3. benzonitrile
4. Phosphotransferases (Kinase)
5. Ligands
6. linifanib
7. benzocycloheptapyridine
8. tyrosine receptor (receptor, tyrosine)
9. bicalutamide (Casodex)
10. hydroxyflutamide

Related Therapies and Procedures

1. Hysterectomy
2. Analgesia
3. Subcutaneous Injections
4. Spinal Injections
5. Castration