4-Isoxazolyl-1,4-dihydropyridines exhibit binding at the multidrug-resistance transporter

Victoria Hulubei; Scott B. Meikrantz; David A. Quincy; Tina Houle; John I. McKenna; Mark E. Rogers; Scott Steiger; N. R. Natale

doi:10.1016/j.bmc.2012.09.022

4-Isoxazolyl-1,4-dihydropyridines exhibit binding at the multidrug-resistance transporter

Victoria Hulubei, Scott B. Meikrantz, David A. Quincy, Tina Houle, John I. McKenna, Mark E. Rogers, Scott Steiger, N. R. Natale

Research output: Contribution to journal › Article › peer-review

17 Scopus citations

Abstract

The 4-isoxazolyl-dihydropyridines (IDHPs) exhibit inhibition of the multidrug-resistance transporter (MDR-1), and exhibit an SAR distinct from their activity at voltage gated calcium channels (VGCC). Among the four most active IDHPs, three were branched at C-5 of the isoxazole, including the most active analog, 1k.

Original language	English
Pages (from-to)	6613-6620
Number of pages	8
Journal	Bioorganic and Medicinal Chemistry
Volume	20
Issue number	22
DOIs	https://doi.org/10.1016/j.bmc.2012.09.022
State	Published - Nov 15 2012

Funding

MDR1 data was generously provided by the National Institute of Mental Health’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, PhD at the University of North Carolina at Chapel Hill and Project Officer Jamie Driscoll at NIMH, Bethesda MD, USA. The authors thank the NIH for grants GM42029, NS038444, and P20RR015583.

Funder number
GM42029, NS038444
HHSN-271-2008-00025-C
P20RR015583

Keywords

Adjuvant
Dihydropyridine
Isoxazole
Lateral metalation
Multidrug transporter

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10.1016/j.bmc.2012.09.022

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@article{3295d8452fba440a82af1c11fe96fb34,

title = "4-Isoxazolyl-1,4-dihydropyridines exhibit binding at the multidrug-resistance transporter",

abstract = "The 4-isoxazolyl-dihydropyridines (IDHPs) exhibit inhibition of the multidrug-resistance transporter (MDR-1), and exhibit an SAR distinct from their activity at voltage gated calcium channels (VGCC). Among the four most active IDHPs, three were branched at C-5 of the isoxazole, including the most active analog, 1k.",

keywords = "Adjuvant, Dihydropyridine, Isoxazole, Lateral metalation, Multidrug transporter",

author = "Victoria Hulubei and Meikrantz, \{Scott B.\} and Quincy, \{David A.\} and Tina Houle and McKenna, \{John I.\} and Rogers, \{Mark E.\} and Scott Steiger and Natale, \{N. 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, PhD at the University of North Carolina at Chapel Hill and Project Officer Jamie Driscoll at NIMH, Bethesda MD, USA. Funding Information: The authors thank the NIH for grants GM42029, NS038444, and P20RR015583. ",

year = "2012",

month = nov,

day = "15",

doi = "10.1016/j.bmc.2012.09.022",

language = "English",

volume = "20",

pages = "6613--6620",

journal = "Bioorganic and Medicinal Chemistry",

issn = "0968-0896",

publisher = "Elsevier Ltd",

number = "22",

}

TY - JOUR

T1 - 4-Isoxazolyl-1,4-dihydropyridines exhibit binding at the multidrug-resistance transporter

AU - Hulubei, Victoria

AU - Meikrantz, Scott B.

AU - Quincy, David A.

AU - Houle, Tina

AU - McKenna, John I.

AU - Rogers, Mark E.

AU - Steiger, Scott

AU - Natale, N. R.

N1 - Funding Information: MDR1 data was generously provided by the National Institute of Mental Health’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, PhD at the University of North Carolina at Chapel Hill and Project Officer Jamie Driscoll at NIMH, Bethesda MD, USA. Funding Information: The authors thank the NIH for grants GM42029, NS038444, and P20RR015583.

PY - 2012/11/15

Y1 - 2012/11/15

N2 - The 4-isoxazolyl-dihydropyridines (IDHPs) exhibit inhibition of the multidrug-resistance transporter (MDR-1), and exhibit an SAR distinct from their activity at voltage gated calcium channels (VGCC). Among the four most active IDHPs, three were branched at C-5 of the isoxazole, including the most active analog, 1k.

AB - The 4-isoxazolyl-dihydropyridines (IDHPs) exhibit inhibition of the multidrug-resistance transporter (MDR-1), and exhibit an SAR distinct from their activity at voltage gated calcium channels (VGCC). Among the four most active IDHPs, three were branched at C-5 of the isoxazole, including the most active analog, 1k.

KW - Adjuvant

KW - Dihydropyridine

KW - Isoxazole

KW - Lateral metalation

KW - Multidrug transporter

UR - https://www.scopus.com/pages/publications/84867884475

U2 - 10.1016/j.bmc.2012.09.022

DO - 10.1016/j.bmc.2012.09.022

M3 - Article

C2 - 23063517

AN - SCOPUS:84867884475

SN - 0968-0896

VL - 20

SP - 6613

EP - 6620

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 22

ER -

4-Isoxazolyl-1,4-dihydropyridines exhibit binding at the multidrug-resistance transporter

Abstract

Funding

Keywords

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