Novel structurally varied N-Alkyl 1,4-dihydropyridines as ABCB1 inhibitors

Structure-activity relationships, biological activity and first bioanalytical evaluation

Andreas Hilgeroth, Christiane Baumert, Claudius Coburger, Marianne Seifert, Sören Krawczyk, Cornelius Hempel, Felix Neubauer, Martin Krug, J. Molnár, Hermann Lage

Research output: Contribution to journalArticle

7 Citations (Scopus)

Abstract

Series of structurally varied N-alkyl 1,4-dihydropyridines and novel benzo-annelated derivatives as 1,4- dihydroquinolines have been characterized as ABCB1 inhibitors. Structure-activity relationships (SARs) are discussed. Cytotoxic activities of selected compounds have been determined. A first bioanalysis of ABCB1 substrate properties has been carried out in a cell-based model. Compounds with highest ABCB1 inhibiting activities were no substrates of ABCB1 and not transported by the efflux pump, thus profiling the new ABCB1 inhibitors.

Original languageEnglish
Pages (from-to)487-493
Number of pages7
JournalMedicinal Chemistry
Volume9
Issue number4
DOIs
Publication statusPublished - Jun 2013

Fingerprint

Structure-Activity Relationship
1,4-dihydropyridine
1,4-dihydroquinoline

Keywords

  • ABCB1 inhibitor
  • ABCB1 substrate properties
  • Structure-activity relationships

ASJC Scopus subject areas

  • Drug Discovery

Cite this

Novel structurally varied N-Alkyl 1,4-dihydropyridines as ABCB1 inhibitors : Structure-activity relationships, biological activity and first bioanalytical evaluation. / Hilgeroth, Andreas; Baumert, Christiane; Coburger, Claudius; Seifert, Marianne; Krawczyk, Sören; Hempel, Cornelius; Neubauer, Felix; Krug, Martin; Molnár, J.; Lage, Hermann.

In: Medicinal Chemistry, Vol. 9, No. 4, 06.2013, p. 487-493.

Research output: Contribution to journalArticle

Hilgeroth, Andreas ; Baumert, Christiane ; Coburger, Claudius ; Seifert, Marianne ; Krawczyk, Sören ; Hempel, Cornelius ; Neubauer, Felix ; Krug, Martin ; Molnár, J. ; Lage, Hermann. / Novel structurally varied N-Alkyl 1,4-dihydropyridines as ABCB1 inhibitors : Structure-activity relationships, biological activity and first bioanalytical evaluation. In: Medicinal Chemistry. 2013 ; Vol. 9, No. 4. pp. 487-493.
@article{86b5711128b5474eb8a7df37103a52ad,
title = "Novel structurally varied N-Alkyl 1,4-dihydropyridines as ABCB1 inhibitors: Structure-activity relationships, biological activity and first bioanalytical evaluation",
abstract = "Series of structurally varied N-alkyl 1,4-dihydropyridines and novel benzo-annelated derivatives as 1,4- dihydroquinolines have been characterized as ABCB1 inhibitors. Structure-activity relationships (SARs) are discussed. Cytotoxic activities of selected compounds have been determined. A first bioanalysis of ABCB1 substrate properties has been carried out in a cell-based model. Compounds with highest ABCB1 inhibiting activities were no substrates of ABCB1 and not transported by the efflux pump, thus profiling the new ABCB1 inhibitors.",
keywords = "ABCB1 inhibitor, ABCB1 substrate properties, Structure-activity relationships",
author = "Andreas Hilgeroth and Christiane Baumert and Claudius Coburger and Marianne Seifert and S{\"o}ren Krawczyk and Cornelius Hempel and Felix Neubauer and Martin Krug and J. Moln{\'a}r and Hermann Lage",
year = "2013",
month = "6",
doi = "10.2174/1573406411309040002",
language = "English",
volume = "9",
pages = "487--493",
journal = "Medicinal Chemistry",
issn = "1573-4064",
publisher = "Bentham Science Publishers B.V.",
number = "4",

}

TY - JOUR

T1 - Novel structurally varied N-Alkyl 1,4-dihydropyridines as ABCB1 inhibitors

T2 - Structure-activity relationships, biological activity and first bioanalytical evaluation

AU - Hilgeroth, Andreas

AU - Baumert, Christiane

AU - Coburger, Claudius

AU - Seifert, Marianne

AU - Krawczyk, Sören

AU - Hempel, Cornelius

AU - Neubauer, Felix

AU - Krug, Martin

AU - Molnár, J.

AU - Lage, Hermann

PY - 2013/6

Y1 - 2013/6

N2 - Series of structurally varied N-alkyl 1,4-dihydropyridines and novel benzo-annelated derivatives as 1,4- dihydroquinolines have been characterized as ABCB1 inhibitors. Structure-activity relationships (SARs) are discussed. Cytotoxic activities of selected compounds have been determined. A first bioanalysis of ABCB1 substrate properties has been carried out in a cell-based model. Compounds with highest ABCB1 inhibiting activities were no substrates of ABCB1 and not transported by the efflux pump, thus profiling the new ABCB1 inhibitors.

AB - Series of structurally varied N-alkyl 1,4-dihydropyridines and novel benzo-annelated derivatives as 1,4- dihydroquinolines have been characterized as ABCB1 inhibitors. Structure-activity relationships (SARs) are discussed. Cytotoxic activities of selected compounds have been determined. A first bioanalysis of ABCB1 substrate properties has been carried out in a cell-based model. Compounds with highest ABCB1 inhibiting activities were no substrates of ABCB1 and not transported by the efflux pump, thus profiling the new ABCB1 inhibitors.

KW - ABCB1 inhibitor

KW - ABCB1 substrate properties

KW - Structure-activity relationships

UR - http://www.scopus.com/inward/record.url?scp=84877973849&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84877973849&partnerID=8YFLogxK

U2 - 10.2174/1573406411309040002

DO - 10.2174/1573406411309040002

M3 - Article

VL - 9

SP - 487

EP - 493

JO - Medicinal Chemistry

JF - Medicinal Chemistry

SN - 1573-4064

IS - 4

ER -