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

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

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
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MDPI and ACS Style

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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