3,5-Diacetyl-1,4-dihydropyridines: Synthesis and MDR reversal in tumor cells

Anamik Shah, Harsukh Gaveriya, Noboru Motohashi, Masami Kawase, Setsuo Saito, Hiroshi Sakagami, Kazue Satoh, Yukio Tada, Agnes Solymosi, Kristina Walfard, Joseph Molnar

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35 Citations (Scopus)

Abstract

Eleven 4-phenyl-3,5-diacetyl-1,4-dihydropyridines (AcDHPs) [G1-11] substituted at the phenyl ring were synthesized and compared for their cytotoxic activity and multidrug resistance (MDR)-reversing activity in in vitro assay systems. Among them, compound [G7] showed the highest cytotoxic activity against human promyelocytic leukemia HL-60 and human squamous cell carcinoma HSC-2 cells. However, no compounds tested produced radicals at pH 7.4-12.5. The activity of P-glycoprotein (Pgp) responsible for MDR in tumor cells was reduced by compounds [G2, 3, 6, 5, 8, 1, 11], verapamil [VP] and nifedipine [NP]. However, compounds [G4, 7, 10] were hardly active while G9 did not show a MDR reversing effect at 2.0-20.0 μg/mL. These data show a relationship between chemical structures and MDR-reversing effect on tumor cells.

Original languageEnglish
Pages (from-to)373-377
Number of pages5
JournalAnticancer research
Volume20
Issue number1 A
Publication statusPublished - 2000

Keywords

  • Cytotoxic activity
  • Dihydropyridines
  • ESR
  • MDR reversal on tumor cells

ASJC Scopus subject areas

  • Oncology
  • Cancer Research

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    Shah, A., Gaveriya, H., Motohashi, N., Kawase, M., Saito, S., Sakagami, H., Satoh, K., Tada, Y., Solymosi, A., Walfard, K., & Molnar, J. (2000). 3,5-Diacetyl-1,4-dihydropyridines: Synthesis and MDR reversal in tumor cells. Anticancer research, 20(1 A), 373-377.