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Design, Synthesis, and Cell Lines Studies of Oleanolic Acid—Hydrogen Sulfide Donor Hybrids
| Content Provider | MDPI |
|---|---|
| Author | Zhao, Fenqin Li, Jinyu Yue, Kexin Song, Beibei Sun, Erying Cheng, Xinru Ma, Jing Yan, Lin |
| Copyright Year | 2021 |
| Description | In order to develop new oleanolic acid (OA) derivatives endowed with improved antitumor activities, for the first time, a number of new hybrid compounds were reported by combining OA or 3-oxooleanolic acid with appropriate H2S-donor moiety, coupled via a suitable linker. The anti-tumor evaluation indicated that they exhibited excellent anti-cancer activities against the tested cancer cell lines. Moreover, 18d with 5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione moiety as H2S donor and β-alanine as the linker, showed more potent cytotoxicity against the tested cancer cell lines than OA and 3-oxooleanolic acid, especially for A549 cells. Furthermore, the preferred compound, 18d, preferentially accumulates in cancer cells (13.6 μM) over the matched normal cells LO2 (>100 μM) in vitro. The improved antitumor activity of this hybrid was probably due to its H2S-releasing capability. |
| Starting Page | 3364 |
| e-ISSN | 20763417 |
| DOI | 10.3390/app11083364 |
| Journal | Applied Sciences |
| Issue Number | 8 |
| Volume Number | 11 |
| Language | English |
| Publisher | MDPI |
| Publisher Date | 2021-04-08 |
| Access Restriction | Open |
| Subject Keyword | Applied Sciences Medicinal Chemistry Oleanolic Acid Derivative Hydrogen Sulfide Synthesis Anti-tumor Activity |
| Content Type | Text |
| Resource Type | Article |
