scholarly journals Discovery of Novel Non-Steroidal Cytochrome P450 17A1 Inhibitors as Potential Prostate Cancer Agents

2020 ◽  
Vol 21 (14) ◽  
pp. 4868
Author(s):  
Tomasz M. Wróbel ◽  
Oksana Rogova ◽  
Kasper L. Andersen ◽  
Rahul Yadav ◽  
Simone Brixius-Anderko ◽  
...  

The current study presents the design, synthesis, and evaluation of novel cytochrome P450 17A1 (CYP17A1) ligands. CYP17A1 is a key enzyme in the steroidogenic pathway that produces androgens among other steroids, and it is implicated in prostate cancer. The obtained compounds are potent enzyme inhibitors (sub µM) with antiproliferative activity in prostate cancer cell lines. The binding mode of these compounds is also discussed.

2019 ◽  
Vol 300 ◽  
pp. 63-72 ◽  
Author(s):  
Rossana Cocchiola ◽  
Mariangela Lopreiato ◽  
Raffaella Guazzo ◽  
Maria Margherita de Santi ◽  
Margherita Eufemi ◽  
...  

2011 ◽  
Vol 52 (7) ◽  
pp. 494 ◽  
Author(s):  
Chang Wook Jeong ◽  
Cheol Yong Yoon ◽  
Seong Jin Jeong ◽  
Sung Kyu Hong ◽  
Seok-Soo Byun ◽  
...  

2018 ◽  
Vol 42 (1) ◽  
pp. 50-53 ◽  
Author(s):  
Na Li ◽  
Nan Liu ◽  
Shu Tang ◽  
Duo-Lu Li ◽  
Xiao-Jian Zhang

Nine novel 1-(4′-sulfamoylphenyl)-1,2,3-triazole derivatives bearing an N-heterocycle moiety were designed using a molecular hybridisation approach and synthesised by alkyne/azide click chemistry. Most of the synthesised compounds exhibited good to moderate antiproliferative activity (IC50 values 3.7 to 77.1 μM) against stomach, oesophagus and prostate cancer cell lines, but a compound containing an S-(2-pyridyl)thiomethyl moiety showed 10-fold greater activity against the stomach cell line than 5-fluorouracil. These results demonstrate that N-heterocycle-1,2,3-triazolylsulfonamides could be promising lead compounds to develop new antitumour drugs.


2009 ◽  
Vol 52 (15) ◽  
pp. 4964-4967 ◽  
Author(s):  
Damian Plażuk ◽  
Anne Vessières ◽  
Elizabeth A. Hillard ◽  
Olivier Buriez ◽  
Eric Labbé ◽  
...  

2015 ◽  
Vol 23 (17) ◽  
pp. 5839-5845 ◽  
Author(s):  
Emmanuel S. Akinboye ◽  
Zebalda D. Bamji ◽  
Bernard Kwabi-Addo ◽  
David Ejeh ◽  
Robert L. Copeland ◽  
...  

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