| Autor: |
Wu G; Guizhou Engineering Laboratory for Synthetic Drugs, College of Pharmacy, Guizhou University, Guiyang 550025, China., Wang W; Guizhou Engineering Laboratory for Synthetic Drugs, College of Pharmacy, Guizhou University, Guiyang 550025, China., Li F; Guizhou Engineering Laboratory for Synthetic Drugs, College of Pharmacy, Guizhou University, Guiyang 550025, China., Xu C; Guizhou Engineering Laboratory for Synthetic Drugs, College of Pharmacy, Guizhou University, Guiyang 550025, China., Zhou Y; Guizhou Engineering Laboratory for Synthetic Drugs, College of Pharmacy, Guizhou University, Guiyang 550025, China., Li Z; Guizhou Engineering Laboratory for Synthetic Drugs, College of Pharmacy, Guizhou University, Guiyang 550025, China., Liu B; Guizhou Engineering Laboratory for Synthetic Drugs, College of Pharmacy, Guizhou University, Guiyang 550025, China., Shao L; 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., Chen D; Guizhou Engineering Laboratory for Synthetic Drugs, College of Pharmacy, Guizhou University, Guiyang 550025, China., Bai S; Research Center for Green Chemistry and Ecological Environment Technology, Guizhou Industry Polytechnic College, Guiyang 550008, China., Wang Z; Guizhou Engineering Laboratory for Synthetic Drugs, College of Pharmacy, Guizhou University, Guiyang 550025, China.; 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. |
| Abstrakt: |
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)-9 H -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 IC 50 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. |
