Bioorganic & Medicinal Chemistry 26 (2018) 2958–2964 Contents lists available at ScienceDirect Bioorganic & Medicinal Chemistry journal homepage: www.elsevier.com/locate/bmc A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line Mekala Gunaratnam, Gavin W. Collie , Anthony P. Reszka, Alan K. Todd, Gary N. Parkinson, Stephen Neidle UCL School of Pharmacy, University College London, 29-39 Brunswick Square, London WC1N 1AX, UK ar ti c l e i nf o ab stra ct Article history: Gastro-intestinal tumours (GISTs) are driven by aberrant expression of the c-KIT oncoprotein. They can be Received 27 February 2018 effectively treated by the kinase inhibitor imatinib, which locks the c-KIT kinase domain into an inactive Revised 23 April 2018 conformation. However resistance to imatinib, driven by active-site mutations, is a recurrent clinical Accepted 25 April 2018 challenge, which has been only partly met by the subsequent development of second and third-genera- Available online 26 April 2018 tion c-KIT inhibitors. It is reported here that a tetra-substituted naphthalene diimide derivative, which is a micromolar inhi- Keywords: bitor of cell growth in a wild-type patient-derived GIST cell line, has a sub-micromolar activity in two Cancer distinct patient-derived imatinib-resistant cell
Bioorganic & Medicinal Chemistry – Elsevier
Published: Jul 15, 2018
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