Subhas S Karki, Chudamani B, Sujeet Kumar, Hiroshi Sakagami, Yoshiko Masuda, Satoshi Yokose, Yoshihiro Uesawa, Hajime Kagaya, Erik De Clercq and Dominique Schols
KLE University, India
Meikai University Japan
Meiji Pharmaceutical University, Japan
Rega Institute for Medical Research, Belgium
Posters & Accepted Abstracts: Med Chem (Los Angeles)
A number of imidazo[2,1-b][1,3,4]thiadiazole derivatives having aralkyl and aryl moieties attached to positions 2 and 6 of imidazo[2,1-b][1,3,4]thiadiazole nucleus, respectively, were prepared and characterized by IR, NMR and mass spectrometry. The cytotoxic activity of a new series of 2-naphthyl-imidazo[2,1-b][1,3,4]thiadiazoles against different human and murine cancer cell lines is reported. Among the tested compounds, five derivatives namely CH17, 24, 34, 37 and 39 emerged as the most potent against all the cell lines. To investigate the mechanism of action, we selected compounds CH34, 37 and 39. These compounds induced PARP and caspase-3 cleavages in HSC-2 cells, suggesting the apoptosis induction.
Email: subhasskarki@gmail.com
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