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Discovery of colon tumor cell growth inhibitory agents through a combinatorial approach.

Abstract：

:Two series with the general formula of 4,6-diaryl-2-oxo-1,2 dihydropyridine-3-carbonitriles and their isosteric 4,6-diaryl-2-imino-1,2-dihydropyridine-3-carbonitrile were synthesized through one pot reaction of the appropriate acetophenone, aldehyde, ammonium acetate with ethyl cyanoacetate or malononitrile, respectively. The synthesized compounds were evaluated for their tumor cell growth inhibitory activity against the human HT-29 colon tumor cell line, as well as their PDE3 inhibitory activity. Compound 4-(2-Ethoxyphenyl)-2-oxo-6-thiophen-3-yl-1,2-dihydropyridine-3 carbonitrile (21) showed tumor cell growth inhibitory activity with an IC50 value of 1.25 microM. Meanwhile, 4-(4-Ethoxyphenyl)-2-imino-6-(thiophen-3-yl)-1,2-dihydropyridine-3-carbonitrile (26) showed inhibitory effect upon PDE3 using cAMP or cGMP as substrate. No correlation exists between PDE3 inhibition and the tumor cell growth inhibitory activity. Docking compound 21 to other possible molecular targets showed the potential to bind PIM1 Kinase.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Abadi AH,Abouel-Ella DA,Lehmann J,Tinsley HN,Gary BD,Piazza GA,Abdel-Fattah MA

doi

10.1016/j.ejmech.2009.09.029

subject

Has Abstract

pub_date

2010-01-01 00:00:00

pages

90-7

issue

1

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(09)00461-9

journal_volume

45

pub_type

杂志文章

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