Benzo[b]-1,8-naphthyridine derivatives: Synthesis and reversal activity on multidrug resistance

Houria Misbahi, Pierre Brouant, Aniko Hevér, A. Molnár, Krysztina Wolfard, G. Spengler, Hafid Mefetah, J. Molnár, Jacques Barbe

Research output: Contribution to journalArticle

16 Citations (Scopus)

Abstract

A series of benzo[b]-1,8-naphthyridine derivatives branched with various side-chains and substituents were prepared with the aim of being investigated as multidrug resistance (MDR) modulators. The syntheses were achieved from 2-halonicotinic acid and suitable aryl-amines according to a three-step procedure. All the derivatives were tested in vitro on mouse T-Lymphoma cell line L5178 transfected by MDR1 gene and the chemosensitizing properties of the compounds were compared to those of verapamil and propranolol, as well as to several other tricyclic derivatives like phenothiazines and acridines. Most of the compounds tested reversed the MDR of tumour cells more effectively than the reference drugs did and they showed more potent chemosensitizing activity than phenothiazine and acridine derivatives have.

Original languageEnglish
Pages (from-to)2097-2101
Number of pages5
JournalAnticancer Research
Volume22
Issue number4
Publication statusPublished - 2002

Fingerprint

Naphthyridines
Acridines
Multiple Drug Resistance
Phenothiazines
Verapamil
Propranolol
Amines
Lymphoma
Cell Line
Acids
Pharmaceutical Preparations
Genes
Neoplasms

Keywords

  • Benzonaphthyridine
  • Chemosensitizing activity
  • Multidrug resistance
  • P-glycoprotein

ASJC Scopus subject areas

  • Cancer Research
  • Oncology

Cite this

Misbahi, H., Brouant, P., Hevér, A., Molnár, A., Wolfard, K., Spengler, G., ... Barbe, J. (2002). Benzo[b]-1,8-naphthyridine derivatives: Synthesis and reversal activity on multidrug resistance. Anticancer Research, 22(4), 2097-2101.

Benzo[b]-1,8-naphthyridine derivatives : Synthesis and reversal activity on multidrug resistance. / Misbahi, Houria; Brouant, Pierre; Hevér, Aniko; Molnár, A.; Wolfard, Krysztina; Spengler, G.; Mefetah, Hafid; Molnár, J.; Barbe, Jacques.

In: Anticancer Research, Vol. 22, No. 4, 2002, p. 2097-2101.

Research output: Contribution to journalArticle

Misbahi, H, Brouant, P, Hevér, A, Molnár, A, Wolfard, K, Spengler, G, Mefetah, H, Molnár, J & Barbe, J 2002, 'Benzo[b]-1,8-naphthyridine derivatives: Synthesis and reversal activity on multidrug resistance', Anticancer Research, vol. 22, no. 4, pp. 2097-2101.
Misbahi, Houria ; Brouant, Pierre ; Hevér, Aniko ; Molnár, A. ; Wolfard, Krysztina ; Spengler, G. ; Mefetah, Hafid ; Molnár, J. ; Barbe, Jacques. / Benzo[b]-1,8-naphthyridine derivatives : Synthesis and reversal activity on multidrug resistance. In: Anticancer Research. 2002 ; Vol. 22, No. 4. pp. 2097-2101.
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