In this section, you can access to the latest technical information related to the FUTURE project topic.

Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors

A series of thirty two anilinopyrimidines derived from WZ4002 has been synthesized and evaluated for percentage inhibition of six different EGFR kinases using LanthaScreen binding assay method (EGFR d746 â?? 750) or Zâ??LYTE assay method (EGFR-WT, EGFR d746 - 750, EGFR T790M, EGFR T790M L858R, EGFR C797S and EGFR T790M L858R C797S). Ortho-hydroxyacetamide 10 exhibited complete inhibition of all the six kinases at 10 µM. Against the triple mutant, EGFR T790M C797S L858R, compounds 9-12 exhibited complete inhibition at 10 µM and nearly complete inhibition at 1 µM. The target compounds were also evaluated using the MTT assay to determine their cytotoxic activity against human non-small cell lung cancer cells (PC9, PC9GR and H460) and mouse leukemic cells (Ba/F3 WT and Ba/F3 T 3151). Overall, 7, 9 â?? 12, 30 and 31 were found to be the most potent compounds across all five cell lines.

» Author: Aireen A. Romu, Zining Lei, Bin Zhou, Zhe-Sheng Chen, Vijaya Korlipara

» Reference: Bioorganic & Medicinal Chemistry Letters

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