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Discovery of novel 5-methyl-1H-pyrazole derivatives as potential anti-prostate cancer agents: design, synthesis, molecular modeling and biological evaluation
Key Laboratory of Chemical Biology (Ministry of Education)Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan, China.
Örebro University, School of Science and Technology. (Biology, The Life Science Center)
Key Laboratory of Chemical Biology (Ministry of Education)Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan, China.
Örebro University, School of Science and Technology. (Biology, The Life Science Center)ORCID iD: 0000-0001-7336-6335
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2018 (English)In: Chemical Biology and Drug Design, ISSN 1747-0277, E-ISSN 1747-0285, Vol. 91, no 6, p. 1113-1124Article in journal (Refereed) Published
Abstract [en]

Androgen receptor (AR) signaling functions as a core driving force for the progression of prostate cancer (PCa), and AR has been proved to be an effective therapeutic target even for castration resistant prostate cancer (CRPC). Herein, structural modification via a fragments splicing strategy was performed based on two lead compounds T3 and 10e, leading to the discovery of a series of 5-methyl-1H-pyrazole derivatives. AR reporter gene assay revealed compounds A13 and A14 as potent AR antagonists. Some of the compounds in this series inhibited growth of PCa LNCaP cells more efficiently than enzalutamide. A13 and A14 also showed improved metabolic stability comparing with 10e in human liver microsomes.

Place, publisher, year, edition, pages
John Wiley & Sons, 2018. Vol. 91, no 6, p. 1113-1124
Keywords [en]
androgen receptor, AR antagonist, luciferase reporter gene assay, prostate cancer, pyrazole derivative
National Category
Cancer and Oncology Cell and Molecular Biology
Identifiers
URN: urn:nbn:se:oru:diva-64844DOI: 10.1111/cbdd.13173ISI: 000431974400006PubMedID: 29388326Scopus ID: 2-s2.0-85042562810OAI: oai:DiVA.org:oru-64844DiVA, id: diva2:1181114
Note

Funding Agency:

National Natural Science Foundation of China  21272140

Available from: 2018-02-07 Created: 2018-02-07 Last updated: 2018-08-20Bibliographically approved

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Asnake, SolomonOlsson, Per-Erik

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