Abstract
A series of novel fluoroaminophosphates 4a-4j were synthesized by one-pot method in presence of tetramethylguanidine (TMG) as a catalyst and were characterized by elemental analysis, FTIR, 1H, 13C, 31P, 19F NMR, and mass spectra. All the title compounds were evaluated for in vitro cytotoxicity against leukemic cell line derived from Tcells of leukemia patient (CEM cells) by Trypan blue exclusion and MTT assays, and these were found to exert concentration dependent cytotoxic effects. Among them 4f, 4g & 4j possessed marked cytotoxicity. 4g (with IC50 value of 6 iM) had emerged as lead compound.
Keywords: Aminophosphonate, Fluorine, TMG, Synthesis, Leukmia, CEM cell, Cytotoxicity
Letters in Drug Design & Discovery
Title: Synthesis, Characterization and Evaluation of Cytotoxicity of New Aminophosphonic Acid Diesters in Human Leukemia Cells
Volume: 7 Issue: 4
Author(s): Avula Balakrishna, Kishore K. Chiruvella, Mudumala V.N. Reddy, Rajesh Reddy, Sandip K. Nayak, Sathees C. Raghavan and Cirandur S. Reddy
Affiliation:
Keywords: Aminophosphonate, Fluorine, TMG, Synthesis, Leukmia, CEM cell, Cytotoxicity
Abstract: A series of novel fluoroaminophosphates 4a-4j were synthesized by one-pot method in presence of tetramethylguanidine (TMG) as a catalyst and were characterized by elemental analysis, FTIR, 1H, 13C, 31P, 19F NMR, and mass spectra. All the title compounds were evaluated for in vitro cytotoxicity against leukemic cell line derived from Tcells of leukemia patient (CEM cells) by Trypan blue exclusion and MTT assays, and these were found to exert concentration dependent cytotoxic effects. Among them 4f, 4g & 4j possessed marked cytotoxicity. 4g (with IC50 value of 6 iM) had emerged as lead compound.
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Balakrishna Avula, Chiruvella K. Kishore, Reddy V.N. Mudumala, Reddy Rajesh, Nayak K. Sandip, Raghavan C. Sathees and Reddy S. Cirandur, Synthesis, Characterization and Evaluation of Cytotoxicity of New Aminophosphonic Acid Diesters in Human Leukemia Cells, Letters in Drug Design & Discovery 2010; 7 (4) . https://dx.doi.org/10.2174/157018010790945841
DOI https://dx.doi.org/10.2174/157018010790945841 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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