論文 - 詳細
| RRC ID | 57855 |
|---|---|
| 著者 | Imanari K, Hashimoto M, Wakabayashi H, Okudaira N, Bandow K, Nagai J, Tomomura M, Tomomura A, Uesawa Y, Sakagami H. |
| タイトル | Quantitative Structure-Cytotoxicity Relationship of Azulene Amide Derivatives. |
| ジャーナル | Anticancer Res |
| Abstract |
BACKGROUND/AIM:Very few studies of anticancer activity of azulene amides led us to investigate the cytotoxicity of 21 N-alkylazulene-1-carboxamides introduced either with 3-methyl [1-7], 7-isopropyl-3-methyl [8-14] or 2-methoxy group [15-21] Materials and Methods: Tumor-specificity (TS) was calculated by the ratio of mean 50% cytotoxic concentration (CC50) against three normal human oral mesenchymal cells to that against four human oral squamous cell carcinoma (OSCC) cell lines. Potency-selectivity expression (PSE) was calculated by dividing TS value by CC50 value against OSCC cell lines. Apoptosis-inducing activity was evaluated by caspase-3 activation and appearance of subG1 cell population. RESULTS:[8-14] showed higher TS and PSE values, than [1-7] and [15-21] The most active compound [8-14] induced apoptosis in C9-22 OSCC cells at 4-times higher CC50 Quantitative structure-activity relationship analysis of [1-14] demonstrated that their tumor-specificity was correlated with chemical descriptors that explain the molecular shape and hydrophobicity. CONCLUSION:7-Isopropyl-3-methyl-N-propylazulene-1-carboxamide [8] can be a potential candidate of lead compound for manufacturing new anticancer drug. |
| 巻・号 | 39(7) |
| ページ | 3507-3518 |
| 公開日 | 2019-7-1 |
| DOI | 10.21873/anticanres.13497 |
| PII | 39/7/3507 |
| PMID | 31262875 |
| MeSH | Amides / chemistry Amides / pharmacology* Antineoplastic Agents / chemistry Antineoplastic Agents / pharmacology* Apoptosis / drug effects Azulenes / chemistry Azulenes / pharmacology* Carcinoma, Squamous Cell / drug therapy* Cell Line Cell Survival / drug effects Humans Mouth Neoplasms / drug therapy* Quantitative Structure-Activity Relationship |
| IF | 1.994 |
| 引用数 | 0 |
| リソース情報 | |
| ヒト・動物細胞 | Ca9-22(RCB1976) HSC-2(RCB1945) HSC-3(RCB1975) HSC-4(RCB1902) |