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

Demjén András | Zendy; Alföldi Róbert | Zendy; Angyal Anikó | Zendy; Gyuris Márió | Zendy; Hackler László | Zendy; Szebeni Gábor J. | Zendy; Wölfling János | Zendy; Puskás László G. | Zendy; Kanizsai Iván | Zendy

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

Author(s) -

Demjén András,

Alföldi Róbert,

Angyal Anikó,

Gyuris Márió,

Hackler László,

Szebeni Gábor J.,

Wölfling János,

Puskás László G.,

Kanizsai Iván

Publication year - 2018

Publication title -

archiv der pharmazie

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.468

H-Index - 61

eISSN - 1521-4184

pISSN - 0365-6233

DOI - 10.1002/ardp.201800062

Subject(s) - pyrazole , chemistry , in vitro , cytotoxic t cell , potency , stereochemistry , human breast , cytotoxicity , structure–activity relationship , ic50 , cell culture , combinatorial chemistry , cancer cell , cancer , biochemistry , medicine , biology , genetics

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 (IC 50 = 0.183 μM).

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