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Front Cover: Alkynylnicotinamide‐Based Compounds as ABL1 Inhibitors with Potent Activities against Drug‐Resistant CML Harboring ABL1(T315I) Mutant Kinase (ChemMedChem 12/2018)
Author(s) -
Larocque Elizabeth A.,
Nagan.,
OpokuTemeng Clement,
Lambrecht Alyssa M.,
Sintim Herman O.
Publication year - 2018
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201800278
Subject(s) - ponatinib , imatinib , dasatinib , myeloid leukemia , imatinib mesylate , chronic myelogenous leukemia , pharmacology , homoharringtonine , drug , medicine , cancer research , leukemia , immunology
The Front Cover shows the facile synthesis (via Sonogashira cross‐coupling) of alkynyl aminoisoquinoline and aminonaphthyridine compounds that potently inhibit chronic myeloid leukemia (CML) cell lines, including the imatinib‐resistant KCL22‐IR CML cell line. KCL22‐IR harbors drug‐resistant BCR‐ABL1, which contains the T315I mutation. Currently, only Ponatinib, a CML drug with some cardiovascular safety liabilties, has been approved for the treatment of CML harboring BCR‐ABL1(T315I). More information can be found in the Full Paper by Herman O. Sintim et al. on page 1172 in Issue 12, 2018 (DOI: 10.1002/cmdc.201700829).