Synthesis, cytotoxic characterization, and SAR study of imidazo[1,2-b]pyrazole-7-carboxamides

András Demjén, Róbert Alföldi, Anikó Angyal, Márió Gyuris, László Hackler, Gábor J. Szebeni, J. Wölfling, L. Puskás, Iván Kanizsai

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4 Citations (Scopus)

Abstract

The synthesis and in vitro cytotoxic characteristics of new imidazo[1,2-b]pyrazole-7-carboxamides were investigated. Following a hit-to-lead optimization exploiting 2D and 3D cultures of MCF-7 human breast, 4T1 mammary gland, and HL-60 human promyelocytic leukemia cancer cell lines, a 67-membered library was constructed and the structure–activity relationship (SAR) was determined. Seven synthesized analogues exhibited sub-micromolar activities, from which compound 63 exerted the most significant potency with a remarkable HL-60 sensitivity (IC50 = 0.183 μM).

Original languageEnglish
Article number1800062
JournalArchiv der Pharmazie
Volume351
Issue number7
DOIs
Publication statusPublished - Jul 1 2018

Keywords

  • anticancer agents
  • cytotoxic
  • Groebke–Blackburn–Bienaymé reaction
  • imidazo[1,2-b]pyrazole
  • multicomponent reaction

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery

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    Demjén, A., Alföldi, R., Angyal, A., Gyuris, M., Hackler, L., Szebeni, G. J., Wölfling, J., Puskás, L., & Kanizsai, I. (2018). Synthesis, cytotoxic characterization, and SAR study of imidazo[1,2-b]pyrazole-7-carboxamides. Archiv der Pharmazie, 351(7), [1800062]. https://doi.org/10.1002/ardp.201800062