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. 2010 Mar 15;20(6):2038-43.
doi: 10.1016/j.bmcl.2009.09.071. Epub 2009 Sep 22.

Synthesis and characterization of a novel iNOS/Akt inhibitor Se,Se'-1,4-phenylenebis(1,2-ethanediyl)bisisoselenourea (PBISe)--against colon cancer

Dhimant Desai  1 , SubbaRao V Madhunapantula, Krishnegowda Gowdahalli, Arati Sharma, Raghavendragowda Chandagaludoreswamy, Karam El-Bayoumy, Gavin P Robertson, Shantu Amin
Affiliations

Synthesis and characterization of a novel iNOS/Akt inhibitor Se,Se'-1,4-phenylenebis(1,2-ethanediyl)bisisoselenourea (PBISe)--against colon cancer

Dhimant Desai et al. Bioorg Med Chem Lett. .

Abstract

Our studies demonstrate that substitution of sulfur with selenium in known iNOS inhibitor increases the compound's potency by several folds in variety of different cancers cell lines tested. Hence, this approach may be used as a strategy to increase the efficacy of the anticancer agents.

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Figures

Figure 1
Figure 1
Structures of PBIT, PBISe, PEIT, and PEISe
Figure 2
Figure 2
In vitro therapeutic efficacy of PBISe and PBIT in Caco-2 cancer cell viability study - IC50 value (μM)
Figure 3
Figure 3
PBISe inhibit cancer cell survival more effectively compared to normal cells - IC50 value (μM)
Figure 4
Figure 4
Effect of PBIT and PBISe on total nitrite production by Caco-2 cells
Figure 5
Figure 5
Effect of PBISe on vital pathways regulating colon cancer development.
Scheme 1
Scheme 1
Reagents and condition: (a), LiAlH4, RT, 91%; (b) CBr4/PPh3, 74%; (c) NH2CSNH2 or NH2CSeNH2/EtOH, 78–69%.
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