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HeLa cervical adenocarcinoma, A375 malignant mela-
noma and HCT-116 colon carcinoma cells with IC50
values of 1.7, 0.87 and 0.55 lM, respectively. Finally,
1b was evaluated for its ability to inhibit VEGFR-2 ki-
nase, a receptor tyrosine kinase implicated in angio-
genesis, another important mechanism for tumour
progression.17 Compound 1b inhibited VEGFR-2 ki-
nase with an IC50 value of 1.46 lM, revealing approx-
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inhibition.
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In summary, a novel heterocyclic compound was discov-
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tential use for anticancer therapy, this CDK1 inhibitor
may also be useful for the treatment of other indications
such as restenosis, psoriasis, retinopathy and allopecia.8
An efficient chemistry was developed for the synthesis,
with key steps including Pd(II) catalyzed Stille coupling
reaction and sulfur(0) induced benzimidazole formation.
A detailed structure–activity relationship (SAR) study
and pharmacokinetic properties for this series will be
reported in due course.
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Acknowledgments
We are grateful to Robert H. Gruninger and Angel
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