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

Demjén, András and Alföldi, Róbert and Angyal, Anikó and Gyuris, Márió and Hackler, László, Jr. and Szebeni, Gábor J. and Wölfling, János and Kanizsai, Iván and Puskás, László G. (2018) Synthesis, cytotoxic characterization, and SAR study of imidazo[1,2-b]pyrazole-7-carboxamides. ARCHIV DER PHARMAZIE. pp. 1-21. ISSN 0365-6233

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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).

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