PT  - JOURNAL ARTICLE
AU  - TOSHIKI WADA
AU  - RYOTA MARUYAMA
AU  - YUTA IRIE
AU  - MASASHI HASHIMOTO
AU  - HIDETSUGU WAKABAYASHI
AU  - NORIYUKI OKUDAIRA
AU  - YOSHIHIRO UESAWA
AU  - HAJIME KAGAYA
AU  - HIROSHI SAKAGAMI
TI  - <em>In Vitro</em> Anti-tumor Activity of Azulene Amide Derivatives
DP  - 2018 May 01
TA  - In Vivo
PG  - 479--486
VI  - 32
IP  - 3
4099  - http://iv.iiarjournals.org/content/32/3/479.short
4100  - http://iv.iiarjournals.org/content/32/3/479.full
SO  - In Vivo2018 May 01; 32
AB  - Background/Aim: There exist few research articles regarding the anticancer activity of azulene-related compounds. We investigated here the relative cytotoxicity of 10 azulene amide derivatives against cancer and normal cells. Materials and Methods: Cytotoxicity against four human oral squamous cell carcinoma (OSCC) cell lines and three human oral normal cells (gingival fibroblasts, periodontal ligament fibroblasts and pulp cells) was determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetra-zolium bromide method. Antitumor activity was evaluated by tumor-specificity (TS) (ratio of mean 50% cytotoxic concentration (CC50) against normal cells to that against OSCC cell lines) and potency-selectivity expression (PSE) (ratio of TS to CC50 against tumor cells). Apoptosis-inducing activity was evaluated by cleavage of poly ADP-ribose polymerase and caspase-3 with western blot analysis. Results. N-Propylguaiazulenecarboxamide [1] showed the highest TS and PSE values, compared to that of doxorubicin, and induced apoptosis in two OSCC cell lines. QSAR analysis demonstrated that their tumor-specificity of azulene amide derivatives was correlated with hydrophobicity and molecular shape. Conclusion: Compound [1] can be considered as a lead compound for manufacturing new anticancer drug candidates.