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 and Szebeni, Gábor J. and Wölfling, János and Puskás, László G. and Kanizsai, Iván (2018) Synthesis, cytotoxic characterization, and SAR study of imidazo[1,2-b]pyrazole-7-carboxamides. ARCHIV DER PHARMAZIE, 351 (7). pp. 1-21. ISSN 0365-6233

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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=0.183M).

Item Type: Article
Uncontrolled Keywords: IN-VIVO; MULTICOMPONENT REACTIONS; BIOLOGICAL EVALUATION; multicomponent reaction; Anticancer agents; kinase inhibitors; Cytotoxic; Aurora Kinases; Groebke-Blackburn-Bienayme reaction; LEAD OPTIMIZATION; ANTITUMOR EVALUATION; ANTIMICROBIAL EVALUATION; PYRAZOLE DERIVATIVES; 2-b]pyrazole; imidazo[1;
Subjects: R Medicine / orvostudomány > RS Pharmacy and materia medica / gyógyszerészet, gyógyászati eszközök
Depositing User: MTMT SWORD
Date Deposited: 31 Jan 2019 07:27
Last Modified: 31 Jan 2019 07:27

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