Identification of 4‐methoxythieno[2,3‐d]pyrimidines as FGFR1 Inhibitors
Aim. To identify novel FGFR1 inhibitors using virtual screening approach. Methods. We used methods of organic synthesis, molecular docking via the Autodock 4.2.6 program package and in vitro biochemical tests with γ-32P. Results. In vitro experiments showed that 9 of 23 tested compounds possess inhi...
Збережено в:
| Дата: | 2019 |
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| Автори: | , , , , , , , |
| Формат: | Стаття |
| Мова: | English |
| Опубліковано: |
Інститут молекулярної біології і генетики НАН України
2019
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| Назва видання: | Вiopolymers and Cell |
| Теми: | |
| Онлайн доступ: | http://dspace.nbuv.gov.ua/handle/123456789/154386 |
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| Назва журналу: | Digital Library of Periodicals of National Academy of Sciences of Ukraine |
| Цитувати: | Identification of 4‐methoxythieno[2,3‐d]pyrimidines as FGFR1 Inhibitors / I.M. Kotey, M.V. Protopopov, S.A. Starosyla, A.O. Balanda, L.V. Pletnova, A.O. Prykhod'ko, V.G. Bdzhola, S.M. Yarmoluk // Вiopolymers and Cell. — 2019. — Т. 35, № 2. — С. 152-162. — Бібліогр.: 17 назв. — англ. |
Репозитарії
Digital Library of Periodicals of National Academy of Sciences of Ukraine| Резюме: | Aim. To identify novel FGFR1 inhibitors using virtual screening approach. Methods. We used methods of organic synthesis, molecular docking via the Autodock 4.2.6 program package and in vitro biochemical tests with γ-32P. Results. In vitro experiments showed that 9 of 23 tested compounds possess inhibitory activity against FGFR1 with IC50 values in the range from 0.9 to 5.6 μM. Conclusions. Nine FGFR1 inhibitors were developed. The mode of compounds binding with the ATP-acceptor site was determined using molecular docking methods and the dependence of the compounds’ activity on the substituents R1, R4 and R5 was evaluated |
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