Letters in Drug Design & Discovery

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

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Design, Synthesis and Anti Colon Cancer Activity Evaluation of Phosphorylated Derivatives of Lamivudine (3TC)

Author(s): Valasani Koteswara Rao, Sanapalli S. Reddy, Balam S. Krishna, Cirandur S. Reddy, Nimmanapalli P. Reddy, Tamatam C.M. Reddy, Chamarthi N. Raju, S. K. Ghosh.

Abstract:

The novel phosphorylated derivatives of Lamivudine (5a-5l) as potential anti colon cancer agents are synthesized. These title compounds are designed based on the basic pyrimidine derivative lamivudine as a starting compound and reacted with various phosphorodichloridates followed by the introduction of bioactive groups at the phosphorus. Their structures were characterized by IR, 1H, 13C, 31P NMR and mass spectral analyses. All the compounds were evaluated for their anti colon cancer activity against COLO-205 cell lines in vitro studies. Among them 5a and 5b emerged as lead compounds with 0.003 μM and 0.0001 μM values.

Keywords: Anti colon cancer activity, COLO- 205 cell lines, MTT assay, Phosphorylated derivatives of lamivudine, anti colon cancer agents, pyrimidine derivative, NMR, mass spectral analyses, Nucleoside analogs, HIV-1, antiretroviral effect, AIDS, HBVDNA, HBeAg, ALT, FT-IR spectrophotometer, TMS, COLO-205 cells, FBS, Cell proliferation, MTT, IC50, TEA, THF, TLC, COLO-205 cell line, 3TC

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Article Details

VOLUME: 8
ISSUE: 1
Year: 2011
Page: [59 - 64]
Pages: 6
DOI: 10.2174/157018011793663921