Design, Synthesis and Biological Activity Evaluation of β-Carboline Derivatives Containing Nitrogen Heterocycles
Guiyun Wu,
Wenhang Wang,
Fulian Li,
Chenlu Xu,
Yue Zhou,
Zhurui Li,
Bingqian Liu,
Lihui Shao,
Danping Chen,
Song Bai,
Zhenchao Wang
Affiliations
Guiyun Wu
Guizhou Engineering Laboratory for Synthetic Drugs, College of Pharmacy, Guizhou University, Guiyang 550025, China
Wenhang Wang
Guizhou Engineering Laboratory for Synthetic Drugs, College of Pharmacy, Guizhou University, Guiyang 550025, China
Fulian Li
Guizhou Engineering Laboratory for Synthetic Drugs, College of Pharmacy, Guizhou University, Guiyang 550025, China
Chenlu Xu
Guizhou Engineering Laboratory for Synthetic Drugs, College of Pharmacy, Guizhou University, Guiyang 550025, China
Yue Zhou
Guizhou Engineering Laboratory for Synthetic Drugs, College of Pharmacy, Guizhou University, Guiyang 550025, China
Zhurui Li
Guizhou Engineering Laboratory for Synthetic Drugs, College of Pharmacy, Guizhou University, Guiyang 550025, China
Bingqian Liu
Guizhou Engineering Laboratory for Synthetic Drugs, College of Pharmacy, Guizhou University, Guiyang 550025, China
Lihui Shao
State Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals, Guizhou University, Guiyang 550025, China
Danping Chen
Guizhou Engineering Laboratory for Synthetic Drugs, College of Pharmacy, Guizhou University, Guiyang 550025, China
Song Bai
Research Center for Green Chemistry and Ecological Environment Technology, Guizhou Industry Polytechnic College, Guiyang 550008, China
Zhenchao Wang
Guizhou Engineering Laboratory for Synthetic Drugs, College of Pharmacy, Guizhou University, Guiyang 550025, China
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 N-(4-(morpholinomethyl)phenyl)-2-((5-(1-(3,4,5-trimethoxyphenyl)-9H-pyrido[3,4-b]indol-3-yl)-1,3,4-oxadiazol-2-yl)thio)acetamide (8q) exhibited significant inhibitory activity against PC-3 cells with an IC50 value of 9.86 µM. Importantly, compound 8q effectively suppressed both the proliferation and migration of PC-3 cells. Mechanistic studies revealed that compound 8q 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.
