2020年9月
Antitumor Effects and Tumor-specificity of Guaiazulene-3-Carboxylate Derivatives against Oral Squamous Cell Carcinoma in Vitro
Anticancer Research
- 巻
- 40
- 号
- 9
- 開始ページ
- 4885
- 終了ページ
- 4894
- 記述言語
- 英語
- 掲載種別
- 研究論文(学術雑誌)
- DOI
- 10.21873/anticanres.14491
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 (CC ) 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 CC value 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 subG and G /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-3carboxylates [6, 7] can be potential candidates of lead compound for developing novel anticancer drugs. 50 50 1 2
- リンク情報
-
- DOI
- https://doi.org/10.21873/anticanres.14491
- PubMed
- https://www.ncbi.nlm.nih.gov/pubmed/32878776
- Scopus
- https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85090261251&origin=inward 本文へのリンクあり
- Scopus Citedby
- https://www.scopus.com/inward/citedby.uri?partnerID=HzOxMe3b&scp=85090261251&origin=inward
- ID情報
-
- DOI : 10.21873/anticanres.14491
- ISSN : 0250-7005
- eISSN : 1791-7530
- PubMed ID : 32878776
- SCOPUS ID : 85090261251