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Molecules 2009, 14(10), 4166-4179; doi:10.3390/molecules14104166
Article

Design and Synthesis of Novel 2-Phenylaminopyrimidine (PAP) Derivatives and Their Antiproliferative Effects in Human Chronic Myeloid Leukemia Cells

1
, 1
, 1
, 2
 and 1,*
1 Shenyang Pharmaceutical University, Shenyang, 110016, China 2 Mount Sinai School of Medicine, New York, NY 10029, USA
* Author to whom correspondence should be addressed.
Received: 1 September 2009 / Revised: 30 September 2009 / Accepted: 12 October 2009 / Published: 19 October 2009
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Abstract

A series of novel 2-phenylaminopyrimidine (PAP) derivatives structurally related to STI-571 were designed and synthesized. The abilities of these compounds to inhibit proliferation were tested in human chronic myeloid leukemia K562 cells. (E)-3-(2-bromophenyl)-N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)phenyl]acrylamide(12d) was the most effective cell growth inhibitor and was 3-fold more potent than STI-571.
Keywords: 2-Phenylaminopyrimidine (PAP) derivative; STI-571; antiproliferative activity 2-Phenylaminopyrimidine (PAP) derivative; STI-571; antiproliferative activity
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Chang, S.; Yin, S.-L.; Wang, J.; Jing, Y.-K.; Dong, J.-H. Design and Synthesis of Novel 2-Phenylaminopyrimidine (PAP) Derivatives and Their Antiproliferative Effects in Human Chronic Myeloid Leukemia Cells. Molecules 2009, 14, 4166-4179.

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