Design, Synthesis and Biological Activity Evaluation of β-Carboline Derivatives Containing Nitrogen Heterocycles
A series of β-carboline derivatives containing nitrogen heterocycles were designed and synthesized. All compounds were screened for their antitumor activity against four human tumor cell lines (A549, K562, PC-3, T47D). Notably, compound <i>N</i>-(4-(morpholinomethyl)phenyl)-2-((5-(1-(3,4,5-trimethoxyphenyl)-9<i>H</i>-pyrido[3,4-b]indol-3-yl)-1,3,4-oxadiazol-2-yl)thio)acetamide (<b>8q</b>) exhibited significant inhibitory activity against PC-3 cells with an IC<sub>50</sub> value of 9.86 µM. Importantly, compound <b>8q</b> effectively suppressed both the proliferation and migration of PC-3 cells. Mechanistic studies revealed that compound <b>8q</b> induced cell apoptosis and caused the accumulation of reactive oxygen species (ROS), leading to cell cycle arrest in the G0/G1 phase in PC-3 cells.
Authors
- Zhurui Li (ORCID: https://orcid.org/0009-0003-6683-8842)
- Bingqian Liu (ORCID: https://orcid.org/0000-0001-5710-7210)
- Guiyun Wu
- Chenlu Xu
- Fulian Li
- Yue Zhou (ORCID: https://orcid.org/0009-0005-3498-5025)
- Lihui Shao
- Danping Chen (ORCID: https://orcid.org/0009-0001-9851-037X)
- Song Bai (ORCID: https://orcid.org/0000-0002-1972-2834)
- Zhenchao Wang (ORCID: https://orcid.org/0000-0002-9560-7627)
- Wenhang Wang
Institutions
- Guizhou University (CN)
- Zhejiang Industry Polytechnic College (CN)
Publication Details
- Journal
- Molecules
- Published
- 2024-10-31
- DOI
- https://doi.org/10.3390/molecules29215155
- Citations
- 5
- Primary Topic
- Synthesis and bioactivity of alkaloids
- Type
- article
- Field-Weighted Citation Impact
- 1.17
Funders
- National Natural Science Foundation of China
- Natural Science Foundation of Guizhou Province
- National Key Research and Development Program of China