Literature DB >> 17512729

Antiproliferative and apoptosis inducing properties of pyrano[3,2-c]pyridones accessible by a one-step multicomponent synthesis.

Igor V Magedov1, Madhuri Manpadi, Nikolai M Evdokimov, Eerik M Elias, Elena Rozhkova, Marcia A Ogasawara, Jennifer D Bettale, Nikolai M Przheval'skii, Snezna Rogelj, Alexander Kornienko.   

Abstract

4-Arylpyrano-[3,2-c]-pyridones have been prepared by a one-step cyclocondensation of 4-hydroxy-1,6-dimethylpyridin-2(1H)-one with various substituted benzaldehydes and malononitrile. These heterocycles exhibit micromolar and submicromolar antiproliferative activity in HeLa and induce apoptosis in Jurkat cell lines. Structure-activity studies performed on a small library of these compounds show a pronounced cytotoxicity enhancing effect of the bromo substituent at the meta position of the C4 aromatic moiety.

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Year:  2007        PMID: 17512729      PMCID: PMC3383048          DOI: 10.1016/j.bmcl.2007.05.004

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  8 in total

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Journal:  Mol Cancer Ther       Date:  2004-11       Impact factor: 6.261

  8 in total
  10 in total

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4.  Structural simplification of bioactive natural products with multicomponent synthesis. 3. Fused uracil-containing heterocycles as novel topoisomerase-targeting agents.

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5.  Structural simplification of bioactive natural products with multicomponent synthesis. 2. antiproliferative and antitubulin activities of pyrano[3,2-c]pyridones and pyrano[3,2-c]quinolones.

Authors:  Igor V Magedov; Madhuri Manpadi; Marcia A Ogasawara; Adriana S Dhawan; Snezna Rogelj; Severine Van Slambrouck; Wim F A Steelant; Nikolai M Evdokimov; Pavel Y Uglinskii; Eerik M Elias; Erica J Knee; Paul Tongwa; Mikhail Yu Antipin; Alexander Kornienko
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6.  Cerium ammonium nitrate (CAN)-catalyzed four-component one-pot synthesis of multi-substituted pyrano[2,3-c] pyrazoles under ultrasound irradiation.

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Journal:  Bioorg Med Chem Lett       Date:  2008-01-11       Impact factor: 2.823

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  10 in total

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