New imidazo[1,2-b]pyrazoles as anticancer agents: Synthesis, biological evaluation and structure activity relationship analysis

作者：Grosse Sandrine; Mathieu Veronique; Pillard Christelle; Massip Stephane; Marchivie Mathieu; Jury Christian; Bernard Philippe; Kiss Robert; Guillaumet Gerald^*

来源：European Journal of Medicinal Chemistry, 2014, 84: 718-730.

DOI：10.1016/j.ejmech.2014.07.057

• Imidazo[1,2-b]pyrazoles
• Anticancer activity
• Structure-activity relationship

Synthesis and functionalization strategies of the imidazo[1,2-b]pyrazole core were developed giving a rapid access to three series of novel imidazo[1,2-b]pyrazole type derivatives: C-2/C-61C-7 trisubstituted, C-2/C-3/C-6 tri(hetero)arylated and C-2/C-3/C-6/C-7 tetrasubstituted imidazo[1,2-b]pyrazoles. 39 of the synthetized products were evaluated for in vitro anticancer activity using the MTT colorimetric assay against 5 human and 1 murine cancer cell lines. Promising in vitro growth inhibitory activities were exhibited by some of the target compounds. Of the 39 evaluated products, 4 displayed an IC50 %26lt;= 10 mu M in the 6 cell lines analyzed (compounds 4d, 4g, 9a, ha). A structure activity relationship analysis is also reported in this paper.

• 出版日期2014-9-12