TY - JOUR T1 - Antitumor Effects and Tumor-specificity of Guaiazulene-3-Carboxylate Derivatives Against Oral Squamous Cell Carcinoma <em>In Vitro</em> JF - Anticancer Research JO - Anticancer Res SP - 4885 LP - 4894 DO - 10.21873/anticanres.14491 VL - 40 IS - 9 AU - MICHITO TERATANI AU - SHOUTA NAKAMURA AU - HIROSHI SAKAGAMI AU - MASAKAZU FUJISE AU - MASASHI HASHIMOTO AU - NORIYUKI OKUDAIRA AU - KENJIRO BANDOW AU - YOSUKE IIJIMA AU - JUNKO NAGAI AU - YOSHIHIRO UESAWA AU - HIDETSUGU WAKABAYASHI Y1 - 2020/09/01 UR - http://ar.iiarjournals.org/content/40/9/4885.abstract N2 - Aim: The aim of this study was to investigate the antitumor potential of guaiazulene-3-carboxylate derivatives against oral malignant cells. Materials and Methods: Twelve guaiazulene-3-carboxylate derivatives were synthesized by introduction of either with alkyl group [1-5], alkoxy group [6, 7], hydroxyl group [8, 9] or primary amine [10-12] at the end of sidechains. Tumor-specificity (TS) was calculated by the ratio of mean 50% cytotoxic concentration (CC50) against 3 human oral mesenchymal cell lines to that against 4 human oral squamous cell carcinoma (OSCC) cell lines. Potency-selectivity expression (PSE) was calculated by dividing TS value by CC50value against OSCC cell lines. Cell cycle analysis was performed by cell sorter. Results: [6, 7] showed the highest TS and PSE values, and induced the accumulation of both subG1 and G2/M cell populations in HSC-2 OSCC cells. Quantitative structure-activity relationship analysis demonstrated that their tumor-specificity was correlated with chemical descriptors that explain the 3D shape, electric state and ionization potential. Conclusion: Alkoxyl guaiazulene-3-carboxylates [6, 7] can be potential candidates of lead compound for developing novel anticancer drugs. ER -