@article{e94a5aaa455c47288f550a31cb14e1aa,
title = "Fluorescent probes of the isoxazole-dihydropyridine scaffold: MDR-1 binding and homology model Dedicated to the memory of Professor Robert O. Hutchins, peerless mentor and good friend",
abstract = "Isoxazole-1,4-dihydropyridines (IDHPs) were tethered to fluorescent moieties using double activation via a lanthanide assisted Weinreb amidation. IDHP-fluorophore conjugate 3c exhibits the highest binding to date for IDHPs at the multidrug-resistance transporter (MDR-1), and IDHP-fluorophore conjugates 3c and 7 distribute selectively in SH-SY5Y cells. A homology model for IDHP binding at MDR-1 is presented which represents our current working hypothesis.",
keywords = "Dihydropyridine, Homology model, Isoxazole, Multidrug resistance transporter",
author = "Szabon-Watola, {Monika I.} and Ulatowski, {Sarah V.} and George, {Kathleen M.} and Hayes, {Christina D.} and Steiger, {Scott A.} and Natale, {Nicholas R.}",
note = "Funding Information: MDR1 data was generously provided by the National Institute of Mental Health{\textquoteright}s Psychoactive Drug Screening Program (NIMH PDSP) , Contract # HHSN-271-2008-00025-C (NIMH PDSP). The NIMH PDSP is Directed by Bryan L. Roth MD, Ph.D. at the University of North Carolina at Chapel Hill and Project Officer Jamie Driscoll at NIMH, Bethesda MD, USA. Funding Information: The authors thank NIH for grants NS038444 (N.N., M.I.S.), 5U01ES016102-02 (K.M.G., S.V.U.), and P20RR015583 (N.N., S.S.). C.D.H. thanks the NSF REU Award Number 0649306 . M.I.S. thanks the Malcolm and Carol Renfrew Scholarship. We thank Dr. Alex Blumenfeld for VT NMR and Dr. Gary Knerr for able assistance in FAB MS while at the University of Idaho. We thank Dr. Mike Braden and Dave Holley of the Core Facility for Molecular Computation (UM) for helpful discussions during pharmacophore modeling. ",
year = "2014",
month = jan,
day = "1",
doi = "10.1016/j.bmcl.2013.11.068",
language = "English",
volume = "24",
pages = "117--121",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Ltd",
number = "1",
}