DOI: 10.36347/sjams.2013.v01i03.014

Pages: 219-225

Abstract: DNA intercalatiors are one of the most important and widely used classes of anti-cancer drugs. Based on the essentially required structural features hereby we have proposed to synthesize a novel series of dimeric compounds which would be capable of intercalating DNA in the minor groove and could serve as a model for developing a novel class of anti-cancer agents. It is evident from the literature review that benzothiazoles possess wide range of biological & pharmacological properties including anticancer properties. In present investigations we have attempted to design a novel series of compounds which contained N1, N3 Bis (6-chlorobenzo (d) thiazol-2-yl) 2 – substituted methyl malonamide molecular framework of possible Bis-DNA intercalators. Based on this hypothesis and the proposed model a new series of N1, N3 Bis (6-chlorobenzo (d) thiazol-2-yl) 2–substituted methyl malonamides were developed and screened for their anticancer activity by Wheat rootlet growth inhibition assay Antimitotic studies using onion root model. The compounds were characterized by FT-IR and 1H-NMR spectral studies. Solubulity studies, Rf value determination, Percentage yield determination were done. In wheat rootlet growth inhibition assay Compounds IVg (Fluoro) and Vie (Chloro) were most active with percentage inhibition of 50 and 54 respectively. Compounds IVg (Fluoro) and Vie (Chloro) were most active with percentage inhibition of 50 and 54 respectively. In antimitotic studies using onion root model the series compounds IVj (Nitro) was found to be more potent with 54 and 74% inhibition of mitosis at 10 and 20µg/ml respectively. It was followed by the compounds IVc (Aniline) & IVe (Chloro) which showed about 70% inhibition at 20µg/ml concentration.