Tổng hợp và thử tác dụng ức chế protein kinase của một số dẫn chất dibenzofuran mới

Lượt tải về:

Đào Việt Hưng1,2, Hà Quang Lợi 1, Hà Thanh Hoà1, Hoàng Đức Luận1, Phạm Quốc Tuấn1, Trần Thị Vân Anh1, Isabelle Ourliac-Garnier2, Pascal Marchand1, Trần Phương Thảo3*

 1Trường cao đẳng Y Dược Phú Thọ

2Université de Nantes, Nantes Atlantique Universités, France

3Trường Đại học Dược Hà Nội

*Tác giả liên hệ: thaptp119@gmail.com

SUMMARY

Protein kinases play a predominant regulatory role in nearly every aspect of cell biology and they can modify the function of a protein. Protein phosphorylation can increase or decrease enzyme activity and it can alter other biological activities such as transcription and translation. A protein kinase inhibitor is a type of enzyme inhibitor that blocks the action of one or more protein kinases. Protein kinase inhibitors can be used to treat diseases due to hyperactive protein kinases or to modulate cell functions to overcome other disease drivers. The new dibenzofuran derivatives of ()-cercosporamid have been synthesized and evaluated for human protein kinases inhibitors. The compounds have been obtained via 4 to 6 steps with well-known reactions. Three synthesized compounds (5-7) showed potential and selective activity on MmCLK1 and HsPIM1 kinases (IC50 values of 0,13 – 1,22 μM).

Từ khóa: dibenzofuran, (-)-cercosporamid, protein kinsase, IC50

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