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- W2563224463 abstract "In the last few years, several pyrrolo-pyrimidine derivatives have been either approved by the US FDA and in other countries for the treatment of different diseases or are currently in phase I/II clinical trials. Herein we present the synthesis and the characterization of a novel series of pyrrolo[2,3-d]pyrimidines, compounds 8a-j, and their activity against Glioblastoma multiforme (GBM). Docking studies and MM-GBSA analysis revealed the ability of such compounds to efficiently interact with the ATP binding site of Src. Enzymatic assays against a mini-panel of kinases (Src, Fyn, EGFR, Kit, Flt3, Abl, AblT315I) have been performed, showing an unexpected selectivity of our pyrrolo[2,3-d]pyrimidines for Src. Finally, the derivatives were tested for their antiproliferative potency on U87 GBM cell line. Compound 8h showed a considerable cytotoxicity effect against U87 cell line with an IC50 value of 7.1 μM." @default.
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- W2563224463 date "2017-02-01" @default.
- W2563224463 modified "2023-10-17" @default.
- W2563224463 title "Identification of new pyrrolo[2,3- d ]pyrimidines as Src tyrosine kinase inhibitors in vitro active against Glioblastoma" @default.
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- W2563224463 doi "https://doi.org/10.1016/j.ejmech.2016.12.036" @default.
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