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Design and synthesis of new potent anticancer pyrazoles with high FLT3 kinase inhibitory selectivity.

Abstract：

:A new series of 1H- and 2H-pyrazole derivatives (35 final compounds) has been designed and synthesized in this study. A selected group (13 compounds) was then tested over a panel of 60 cancer cell lines at a single dose concentration of 10microM. At this concentration, six compounds have showed moderate to strong mean inhibitions, and were further tested at five-dose testing mode to determine their IC(50) over the 60 cell lines. The IC(50) values of the tested compounds indicated high potency (as for compound 10f) as well as high efficacy (as for compound 11e). Accordingly, compound 10f was then tested at a single dose concentration of 10microM over a panel of 54 kinases to determine its kinase inhibitory profile. The compound has showed good selectivity towards FLT3 kinase, associated with a moderate potency, with an IC(50) value of 1.74microM.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

El-Deeb IM,Lee SH

doi

10.1016/j.bmc.2010.04.029

subject

Has Abstract

pub_date

2010-06-01 00:00:00

pages

3961-73

issue

11

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(10)00333-0

journal_volume

18

pub_type

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