3.8 Article

Synthesis and Antitumor Evaluation of a Novel Class of 4-Substituted-1,4-Dihydroisoquinolin-3-ones

Journal

JOURNAL OF COMBINATORIAL CHEMISTRY
Volume 12, Issue 4, Pages 488-490

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/cc100021t

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Funding

  1. National Natural Science Foundation of China [30772652, 90813026]
  2. National Science & Technology Major Project Key New Drug Creation and Manufacturing Program of China [2009ZX09501-010]

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An efficient method for the solution-phase parallel synthesis of 4-substituted-1,4-dihydroisoquinolin-3-ones is developed. The isoquinolinones were constructed employing an intramolecular Heck reaction, providing full regio- and stereoselectivity. Most of the synthesized compounds showed potent antiproliferative activities against tumor cell lines.

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