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Title of Journal: Res Chem Intermed

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Abbravation: Research on Chemical Intermediates

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Springer Netherlands

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DOI

10.1007/bf02355293

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ISSN

1568-5675

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Synthesis of novel Emphasis Type="Italic"S/Emph

Authors: Makaram M Said Azza T Taher Hala B ElNassan Eman A ElKhouly
Publish Date: 2016/03/11
Volume: 42, Issue: 8, Pages: 6643-6662
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Abstract

Two series of 4phenyl5cyanopyrimidin6one derivatives bearing various Salkyl or Sacyl moieties at position 2 were prepared as cytotoxic agents All compounds were tested for possible anticancer activity on two cell lines MCF7 and HCT116 The MCF7 cell line was found to be more sensitive than the HCT116 cell line to the action of the compounds Compound 8g was the most potent on the MCF7 cell line with IC50 183 nM/mL whereas its IC50 on the normal cell line MRC5 was 6438 nM/mL indicating its safety and selectivity towards the MCF7 cell line On the other hand compound 8d was the most potent compound on the HCT116 cell line with IC50 238 nM/mL Compound 8g was screened against five kinases The compound showed selective inhibitory activity against pim1 kinase with IC50 1162 µMThe authors are grateful to all members of the department of Cancer Biology National Cancer Institute Cairo Egypt for carrying out the cytotoxicity testing The authors are grateful to Kinexus lab Canada for performing the kinase inhibitory assays

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