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).
