Our earlier research has shown that mono-substituted N-phenyl-2, 2-dichloroacetamide exhibited much higher anti-cancer activity than the lead compound sodium dichloroacetate (DCA). In this paper, a variety of multi-substituted N-phenyl-2, 2-dichloroacetamides were synthesized and biologically evaluated. The results showed that 3, 5-disubstituted N-phenyl-2, 2-dichloroacetamide analogues had satisfactory potency. Among them, N-(3, 5-diiodophenyl)-2, 2-dichloroacetamide had an IC50 of 2.84 micromol x L(-1) against non-small cell lung cancer cell line A549 and could induce cancer cell apoptosis.
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Design, synthesis and biological evaluation of N-arylphenyl-2,2-dichloroacetamide analogues as anti-cancer agents.
Bioorg Med Chem Lett
December 2012
Key Laboratory of Bioorganic Phosphorus and Chemical Biology, The Ministry of Education, Department of Chemistry, Tsinghua University, Beijing 100084, PR China.
Our earlier research has shown that N-phenyl-2,2-dichloroacetamide analogues had much higher anti-cancer activity than the lead compound sodium dichloroacetate (DCA). In this current study, a variety of N-arylphenyl-2,2-dichloroacetamide analogues were synthesized via Suzuki coupling reaction and their anti-cancer activity was evaluated. The results showed that N-terphenyl-2,2-dichloroacetamide analogues had satisfactory anti-cancer activity.
View Article and Find Full Text PDFMulti-substituted N-phenyl-2, 2-dichloroacetamide analogues as anti-cancer drugs: design, synthesis and biological evaluation.
Yao Xue Xue Bao
March 2012
Key Laboratory of Bioorganic Phosphorus and Chemical Biology, Ministry of Education, Department of Chemistry, Tsinghua University, Beijing 100084, China.
Our earlier research has shown that mono-substituted N-phenyl-2, 2-dichloroacetamide exhibited much higher anti-cancer activity than the lead compound sodium dichloroacetate (DCA). In this paper, a variety of multi-substituted N-phenyl-2, 2-dichloroacetamides were synthesized and biologically evaluated. The results showed that 3, 5-disubstituted N-phenyl-2, 2-dichloroacetamide analogues had satisfactory potency.
View Article and Find Full Text PDFNovel N-phenyl dichloroacetamide derivatives as anticancer reagents: design, synthesis and biological evaluation.
Eur J Med Chem
September 2010
Key laboratory of Bioorganic Phosphorus and Chemical Biology, The Ministry of Education, Department of Chemistry, Tsinghua University, Beijing, 100084, PR China.
A current study shows that sodium dichloroacetate (DCA) can induce cancer cell apoptosis and inhibit tumor growth, but its cytotoxic activity is low (IC(50) > 1000 microM for A549). In this paper, a variety of DCA derivatives were synthesized, and their cytotoxic activities were evaluated. The result showed that the N-phenyl-2,2-dichloroacetamide analogues had satisfactory potencies.
View Article and Find Full Text PDFSynthesis, Fourier transform infrared and Raman spectra, assignments and analysis of N-(phenyl)- and N-(chloro substituted phenyl)-2,2-dichloroacetamides.
Spectrochim Acta A Mol Biomol Spectrosc
April 2004
Department of Chemistry, Tagore Arts College, Pondicherry 605008, India.
N-(phenyl)-2,2-dichloroacetamide (NPA) and N-(chloro substituted phenyl)-2,2-dichloroacetamides of the configuration XyC6H(5-y)-NHCO-CHCl2 (where, X = Cl and y = 1, 2 and 3) were synthesised and the Fourier transform infrared (FTIR) and Fourier transform Raman (FT-Raman) spectra of the compounds were recorded and analysed. The FTIR spectra of all the compounds were recorded in a Bruker IFS 66V spectrometer in the range of 4000-400 cm(-1) and the FT-Raman spectra were also recorded in the same instrument in the region 3500-100 cm(-1). The variation of an amide bond (-NHCO-) parameters with the substitution of the chlorine atom in the phenyl group and the mixing of different normal modes are discussed with the help of potential energy distribution (PED) calculated through normal co-ordinate analysis.
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