Zunyi Medical Univ. EGFR compound 6q

Zunyi Medical Univ. EGFR compound 6q: sourced facts only. name: "Starting from the binding mode of allosteric EGFR inhibitor JBJ-04-125-02 and the key pharmacophore of the third-generation EGFR inhibitors, we designed and synthesized a novel series of EGFR inhibitors, represented by (R)-N-(4-((2-aminopyrimidin-4-yl)amino)phenyl)-2-(5-(4-(4-methylpiperazin-1-yl)phenyl)-1-oxoisoindolin-2-yl)-2-phenylacetamide (6q)." [PMID:38142512]; target: "Starting from the binding mode of allosteric EGFR inhibitor JBJ-04-125-02 and the key pharmacophore of the third-generation EGFR inhibitors, we designed and synthesized a novel series of EGFR inhibitors, represented by (R)-N-(4-((2-aminopyrimidin-4-yl)amino)phenyl)-2-(5-(4-(4-methylpiperazin-1-yl)phenyl)-1-oxoisoindolin-2-yl)-2-phenylacetamide (6q)." [PMID:38142512]; developer: "School of Bioengineering, Zunyi Medical University, Zhuhai, 519041, China; Key Laboratory of Biocatalysis&Chiral Drug Synthesis of Guizhou Province, Zunyi Medical University, Zunyi, 563000, China." [PMID:38142512]; stage: "Furthermore, compound 6q showed excellent activity against mutant NSCLC cell line NCI-H1975-EGFRL858R/T790M/C797S cells, with IC50 value of 0.82 μM which was superior to that of osimertinib (IC50 = 2.94 μM), JBJ-04-125-02 (IC50 = 3.66 μM), and coadministration of JBJ-04-125-02 and osimertinib (IC50 = 1.25 μM)." [PMID:38142512]