Cytotoxic activity and QSAR of N,N'-diarylalkanediamides.
The one- and two-step syntheses of N,N'-(dinitrophenyl)alkanediamides and N,N'-(diaminophenyl)alkanediamides from 4-nitroaniline were carried out. These compounds were subjected to cytotoxic evaluation against different tumoural cell lines. A QSAR analysis for the aminated series, introducing a QSAR descriptor (D(CL)) designed herein for groove binders, reveals that the activity in the K562 cell line is related to the charge, polarisability, volume and length of the molecules.
Chacón-García
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Instituto de Química, Universidad Nacional Autónoma de México, Circuito Interior, Ciudad Universitaria, Coyoacán, 04510 Mexico DF, Mexico.
Martínez
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R
D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity*; D000814:Aniline Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D021281:Quantitative Structure-Activity Relationship; D014407:Tumor Cells, Cultured / Q000187:drug effects
D000577:Amides; D000814:Aniline Compounds