We have previously reported of labeled reversible and irreversible EGFR inhibitors, such as 4-(3,4-dichloro-6-fluoroanilino)-6,7-dimethoxyquinazoline (ML01) and 6-acrylamido-4-(3,4-dichloro-6-fluoroanilino)quinazoline (ML03), to be suboptimal as imaging agents. On the basis of these studies, a new generation of novel, more chemically stable irreversible inhibitors was labeled with carbon-11 as ...

The design and synthesis of a quinazoline-based, multi-kinase inhibitor for the treatment of acute myeloid leukemia (AML) and other malignancies is reported. Based on the previously reported furanopyrimidine 3, quinazoline core containing lead 4 was synthesized and found to impart dual FLT3/AURKA inhibition (IC50 = 127/5 nM), as well as improved physicochemical properties. A detailed structure-...

The present work describes convenient synthesis of the novel Schiff bases 4, 5 and 6 by reaction each previously synthesized quinazolinones 1, 2 3 with p-methoxybenzaldehyde. [2+2] Cycloaddition Reaction former within phenylisothiocyanate affording azatedine derivatives 7 8. Also, quinazolines 1 could be reacted α-bromoglucose tetraacetate giving peracetylated N-glycosides 9 10 which were then ...