Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


Synthesis and Antitumor Properties of N1-(Hydroxymethyl Phenylmethyl) Pyrimidine Derivatives and their Intermediates

Author(s): Liying Chen, Nageswara Kode, Devangachinta Murthy, Shashikant Phadtare.


A series of ortho- meta- and para-N1-[(chloromethylphenyl)methyl]pyrimidines and N1- [(hydroxymethylphenyl)methyl]pyrimidines 4-27 were prepared by the alkylation of various pyrimidine nucleic acid bases with α,α-dichloroxylenes followed by acid catalyzed hydrolysis. Compounds 4-27 were evaluated for the cytotoxic activity against a panel NCI-H460 (lung), MCF7 (breast) and SF-268 (CNS) cancer cell lines. The ‘active’ compounds which reduced growth of cancer cells to ca. 32% or less have been evaluated in the full panel of 60 human cancer cell lines over a 5-log dose range at the National Cancer Institute. Specifically, the ortho-N1-[(chloromethylphenyl)methyl]pyrimidines in this series (5, 6 and 7) have demonstrated growth inhibitory effects (GI50) on the leukemia (CCRF-CEM, HL-60, K562, MOLT-4, SR) and other cancer cell lines at 10-5 to 10-7 M concentrations.

Keywords: Arylpyrimidines, N1-[(chloromethylphenyl)methyl]pyrimidines, GI50, Antitumor activity

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Article Details

Year: 2007
Page: [249 - 256]
Pages: 8
DOI: 10.2174/157018007784620022
Price: $58