Synthesis and evaluation of novel naphthol diazenyl scaffold based Schiff bases as potential antimicrobial and cytotoxic agents against human colorectal carcinoma cell line (HT-29).

BACKGROUND

In search of new antimicrobial and cytotoxic agents, a series of new naphthol diazenyl scaffold based Schiff bases (-) was efficiently synthesized by condensation of 2-hydroxy naphthaldehyde azo dyes with various substituted aromatic/heteroaromatic/aliphatic amines.

METHODOLOGY

The synthesized derivatives were characterized by various physicochemical and spectral techniques and assessed for in vitro antimicrobial and cytotoxic potential against human colorectal carcinoma cell line (HT-29). The active derivatives were further evaluated for their apoptotic potential by Annexin-V/propidium iodide double staining assay using flow cytometer and analyzed for cell-cycle arrest studies.

RESULTS AND CONCLUSION

The derivative was found maximum active against . , and . The derivatives , , , and showed maximum antifungal activity against . The maximum cytotoxicity was observed from the derivatives , , , and towards HT-29 cell line with IC between 4 and 19 μg/ml. More than 90% and 62% of the cells were found in the apoptotic phase on treatment with and respectively in comparison to the 68% for doxorubicin. Further, these derivatives arrested the cell growth in S and G2/M phase of the cell cycle.