Novel Class of Fluorinated Pyrazolo[1,5‐a]pyrimidines as CDK5 and Bcl2 Inhibitors: Design, Synthesis, Biological Evaluation, Molecular Docking and ADME Studies
Mona Said Mohamed,
Zinab Atwa Saad,
Nadia Hanafy Metwally
Abstract:New pyrazolo[1,5‐a]pyrimidines were designed and synthesized based on the structural analysis of known CDK5 inhibitors. Biological evaluations showed that the IC50 of the most potent compounds 3 c and 5 b targeting normal WI38 (human lung cells) were 74.13±4.0 and 56.19±3.5 μM, respectively and showed safety profile in normal cells compared to doxorubicin with IC50 of 6.27±0.5 μM. Compounds 3 c and 5 b, demonstrated potent CDK5 inhibitory activity with IC50=0.36±0.02 and 0.226±0.01 μM, respectively compared to… Show more
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