論文 - 詳細
| RRC ID | 63036 |
|---|---|
| 著者 | Teratani M, Nakamura S, Sakagami H, Fujise M, Hashimoto M, Okudaira N, Bandow K, Iijima Y, Nagai J, Uesawa Y, Wakabayashi H. |
| タイトル | Antitumor Effects and Tumor-specificity of Guaiazulene-3-Carboxylate Derivatives Against Oral Squamous Cell Carcinoma In Vitro. |
| ジャーナル | Anticancer Res |
| Abstract |
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. |
| 巻・号 | 40(9) |
| ページ | 4885-4894 |
| 公開日 | 2020-9-1 |
| DOI | 10.21873/anticanres.14491 |
| PII | 40/9/4885 |
| PMID | 32878776 |
| MeSH | Antineoplastic Agents / chemical synthesis Antineoplastic Agents / chemistry* Antineoplastic Agents / pharmacology* Apoptosis / drug effects Azulenes / chemical synthesis Azulenes / chemistry* Azulenes / pharmacology* Carcinoma, Squamous Cell / drug therapy* Carcinoma, Squamous Cell / pathology Cell Cycle / drug effects Cell Line Cell Line, Tumor Cell Survival / drug effects Humans Molecular Structure Mouth Neoplasms / drug therapy* Mouth Neoplasms / pathology Quantitative Structure-Activity Relationship Sesquiterpenes, Guaiane / chemical synthesis Sesquiterpenes, Guaiane / chemistry* Sesquiterpenes, Guaiane / pharmacology* |
| IF | 1.994 |
| リソース情報 | |
| ヒト・動物細胞 | Ca9-22(RCB1976) HSC-2(RCB1945) HSC-3(RCB1975) HSC-4(RCB1902) |