androstane has been researched along with Prostatic-Neoplasms* in 2 studies
2 other study(ies) available for androstane and Prostatic-Neoplasms
| Article | Year |
|---|---|
17(E)-picolinylidene androstane derivatives as potential inhibitors of prostate cancer cell growth: antiproliferative activity and molecular docking studies.
We report a rapid and efficient synthesis of A-ring modified 17α-picolyl and 17(E)-picolinylidene androstane derivatives from dehydroepiandrosterone. Compounds were validated spectroscopically and structurally characterized by X-ray crystallography. Virtual screening by molecular docking against clinical targets of steroidal anticancer drugs (ERα, AR, Aromatase and CYP17A1) suggests that 17(E)-picolinylidene, but not 17α-picolyl androstanes could specifically interact with CYP17A1 (17α-hydroxylase) with similar geometry and affinity as Abiraterone, a 17-pyridinyl androstane drug clinically used in the treatment of prostate cancer. In addition, several 17(E)-picolinylidene androstanes demonstrated selective antiproliferative activity against PC3 prostate cancer cells, which correlates with Abiraterone antiproliferative activity and predicted CYP17A1 binding affinities. Based on these preliminary results, 17(E)-picolinylidene androstane derivatives could be a promising starting point for the development of new compounds for the treatment of prostate cancer. Topics: Androstanes; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Crystallography, X-Ray; Humans; Male; Molecular Docking Simulation; Prostate; Prostatic Neoplasms; Protein Binding; Steroid 17-alpha-Hydroxylase | 2013 |
Synthesis, antiproliferative activity, acute toxicity and assessment of the antiandrogenic activities of new androstane derivatives.
A number of 17-oxo-5-androsten-3β-yl esters (9a-9f) and 3β-alkoxy-5-androsten-17-ones (11a-11e) were synthesized from commercially available (25R)-5-spirosten-3β-ol (Diosgenin) (4) as starting material. The synthesized compounds were evaluated for their antiproliferative activity against the prostate-specific cancer cell line DU-145, acute toxicity and effect on serum androgen levels, and compared with finasteride as positive control. Some of the compounds exhibited better cytotoxicity and antiandrogenic activity than the reference control. The detailed synthesis, spectroscopic data and biological activity of the synthesized compounds are reported. Topics: Androgen Antagonists; Androgens; Androstanes; Androstenes; Androstenols; Animals; Antineoplastic Agents; Cell Line; Cell Line, Tumor; Cell Proliferation; Diosgenin; Dose-Response Relationship, Drug; Finasteride; Humans; Inhibitory Concentration 50; Lethal Dose 50; Macrophages; Male; Mice; Prostatic Neoplasms; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship | 2011 |