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Identification of New 4-N-substituted 6-aryl-7H-pyrrolo[2,3-d]pyrimidine-4-amines as Highly Potent EGFR-TK Inhibitors With Src-family Activity

Identification of New 4-N-substituted 6-aryl-7H-pyrrolo[2,3-d]pyrimidine-4-amines as Highly Potent EGFR-TK Inhibitors With Src-family Activity

Svein Jacob Kaspersen, Jin Han, Kristin G Nørsett, Line Rydså, Eli Kjøbli, Steffen Bugge, Geir Bjørkøy, Eirik Sundby, Bård Helge Hoff

Eur J Pharm Sci. 2014 Aug 1;59:69-82.

PMID: 24769040

Abstract:

The epidermal growth factor receptor is an important target in molecular cancer therapy. Herein, the enzymatic inhibition potential of a series of chiral and non chiral pyrrolopyrimidine based derivatives have been investigated and optimised. Overall, seven new compounds were identified having enzymatic IC50 values comparable to or better than the commercial drug Erlotinib. High activity was also confirmed towards the epidermal growth factor receptor L858R and L861Q mutants. Based on calculated druglike properties, eight compounds were further evaluated towards a panel of 52 other kinases revealing interesting Src-family kinase and colony stimulating factor 1 receptor kinase inhibitory activity. Cell proliferation studies with the cell lines A431, C-33A, AU-565, K-562 and genetically engineered Ba/F3-EGFR(L858R) cells also showed several molecules to be more active than Erlotinib, and thus confirming these pyrrolopyrimidines as attractive drug candidates or lead structures.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP87199153	3-(Hydroxymethyl)phenylboronic acid		87199-15-3	Price

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