Nicole Bozza

TL;DR: The findings suggest that the insertion of a chloroacetamide warhead on a suitable scaffold, as exemplified by UPR1376, is a valuable strategy to develop a novel generation of FGFR inhibitors for the treatment of SQCLC patients with FGFR alterations.

TL;DR: A synthetic route was reported that allowed us to characterize and unambiguously identify the structure of the active compound by a combination of NMR spectroscopy and in silico conformational analysis and sustain experiments aimed at assessing its therapeutic potential for the treatment of FGF-dependent lung cancers.

TL;DR: UPR1444 (compound 11) is a new sulfonyl fluoride derivative which potently and irreversibly inhibits EGFRL858R/T790M/C797S through the formation of a sulfonamide bond with the catalytic residue Lys745.

TL;DR: This work synthesized a 2-chloro-N-(4-(phenylamino)quinazolin-6-yl)acetamide (8) derivative as a prototype of EGFR inhibitor potentially able to react with Cys797 by nucleophilic substitution and tuned the reactivity of the acetamide fragment by replacing the chlorine leaving group with (hetero)-aromatic thiols or carboxylate esters.

TL;DR: The studies provide the evidence for using NSC12 as a specific FGF/FGFR system inhibitor, thus representing a novel therapeutic strategy in WM, and demonstrate significant inhibition of WM cell growth, induction ofWM cell apoptosis, halting MAPK, JAK/STAT3 and PI3K-Akt pathways.