Synthesis, SAR, and antitumor properties of diamino-C,N-diarylpyrimidine positional isomers: inhibitors of lysophosphatidic acid acyltransferase-beta

  • Bioorg Med Chem Lett. 2004 May 3;14(9):2303-8. doi: 10.1016/j.bmcl.2004.01.104.
Baoqing Gong  1 ,  Feng Hong ,  Cory Kohm ,  Scott Jenkins ,  John Tulinsky ,  Rama Bhatt ,  Peter De Vries ,  Jack W Singer ,  Peter Klein
Affiliations
  • 1. Cell Therapeutics, Inc, 201 Elliott Ave W, Suite 400, Seattle, WA 98119, USA.
PMID: 15081029 DOI: 10.1016/j.bmcl.2004.01.104
Abstract

2,4-Diamino-N(4),6-diarylpyrimidines were identified as potent, isoform specific inhibitors of lysophosphatidic acid acyltransferase-beta (LPAAT-beta). Active inhibitors also blocked proliferation of tumor cell lines in vitro. The effect of 2j in an in vivo tumor model was investigated.

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