Oxazoline derivatives of [17(20)E]-21-norpregnene – inhibitors of CYP17A1 activity and proliferation of prostate carcinoma cells
- Авторлар: Kostin V.1, Latysheva A.1, Zolottsev V.1, Tkachev Y.2, Timofeev V.2, Kuzikov A.1, Shumyantseva V.1, Morozevich G.1, Misharin A.1
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Мекемелер:
- V. N. Orekhovich Research Institute of Biomedical Chemistry, Russian Academy of Medical Sciences
- V. A. Engel’gardt Institute of Molecular Biology, Russian Academy of Sciences
- Шығарылым: Том 67, № 4 (2018)
- Беттер: 682-687
- Бөлім: Full Article
- URL: https://journals.rcsi.science/1066-5285/article/view/242433
- DOI: https://doi.org/10.1007/s11172-018-2122-7
- ID: 242433
Дәйексөз келтіру
Аннотация
Nine new oxazolinyl derivatives of [17(20)E]-21-norpregnene, differing in the structure of steroid moiety, were investigated for their potency to inhibit the CYP17A1 catalytic activity, as well as growth and proliferation of LNCaP and PC-3 prostate carcinoma cell lines. The activity of one of the investigated compounds, 2´-{[(E)3β-hydroxyandrost-5-en-17-ylidene]methyl}-4´,5´-dihydro-1´,3´-oxazole (1), was found to be comparable with that of Abiraterone, a known inhibitor of CYP17A1 used for treatment of prostate cancer. A model of the interaction of oxazoline 1 with the active site of CYP17A1 was constructed by the molecular dynamics method. A correlation was found between the structure and the biological activity in the series of [17(20)E]-21-norpregnene oxazolinyl derivatives.
Авторлар туралы
V. Kostin
V. N. Orekhovich Research Institute of Biomedical Chemistry, Russian Academy of Medical Sciences
Email: vazolottsev@mail.ru
Ресей, Build. 8, 10 Pogodinskaya ul., Moscow, Russian Federation, 119121
A. Latysheva
V. N. Orekhovich Research Institute of Biomedical Chemistry, Russian Academy of Medical Sciences
Email: vazolottsev@mail.ru
Ресей, Build. 8, 10 Pogodinskaya ul., Moscow, Russian Federation, 119121
V. Zolottsev
V. N. Orekhovich Research Institute of Biomedical Chemistry, Russian Academy of Medical Sciences
Хат алмасуға жауапты Автор.
Email: vazolottsev@mail.ru
Ресей, Build. 8, 10 Pogodinskaya ul., Moscow, Russian Federation, 119121
Ya. Tkachev
V. A. Engel’gardt Institute of Molecular Biology, Russian Academy of Sciences
Email: vazolottsev@mail.ru
Ресей, 32 ul. Vavilova, Moscow, Russian Federation, 119991
V. Timofeev
V. A. Engel’gardt Institute of Molecular Biology, Russian Academy of Sciences
Email: vazolottsev@mail.ru
Ресей, 32 ul. Vavilova, Moscow, Russian Federation, 119991
A. Kuzikov
V. N. Orekhovich Research Institute of Biomedical Chemistry, Russian Academy of Medical Sciences
Email: vazolottsev@mail.ru
Ресей, Build. 8, 10 Pogodinskaya ul., Moscow, Russian Federation, 119121
V. Shumyantseva
V. N. Orekhovich Research Institute of Biomedical Chemistry, Russian Academy of Medical Sciences
Email: vazolottsev@mail.ru
Ресей, Build. 8, 10 Pogodinskaya ul., Moscow, Russian Federation, 119121
G. Morozevich
V. N. Orekhovich Research Institute of Biomedical Chemistry, Russian Academy of Medical Sciences
Email: vazolottsev@mail.ru
Ресей, Build. 8, 10 Pogodinskaya ul., Moscow, Russian Federation, 119121
A. Misharin
V. N. Orekhovich Research Institute of Biomedical Chemistry, Russian Academy of Medical Sciences
Email: vazolottsev@mail.ru
Ресей, Build. 8, 10 Pogodinskaya ul., Moscow, Russian Federation, 119121