Huaxia Xie: College of Basic Medicine and Forensic Medicine, Henan University of Science and Technology, Luoyang, China.
Longfei Mao: College of Basic Medicine and Forensic Medicine, Henan University of Science and Technology, Luoyang, China.
Gaolu Fan: Department of Pharmacy, Luoyang Third People's Hospital, Luoyang, China.
Ziyuan Wu: College of Basic Medicine and Forensic Medicine, Henan University of Science and Technology, Luoyang, China.
Yimian Wang: College of Basic Medicine and Forensic Medicine, Henan University of Science and Technology, Luoyang, China.
Xixi Hou: Department of Pharmacy, The First Affiliated Hospital, College of Clinical Medicine of Henan University of Science and Technology, Luoyang, China.
Jiangang Wang: College of Basic Medicine and Forensic Medicine, Henan University of Science and Technology, Luoyang, China.
Huili Wang: University of North Carolina Hospitals, Chapel Hill, NC, United States.
Ling Liu: College of Basic Medicine and Forensic Medicine, Henan University of Science and Technology, Luoyang, China.
Sanqiang Li: College of Basic Medicine and Forensic Medicine, Henan University of Science and Technology, Luoyang, China.
Based on the structure of the anti-HIV drug cabotegravir, we introduced 1,2,3-triazole groups with different substituents to obtain 19 cabotegravir derivatives and tested their activity against HepG2 cells. The proliferation of HepG2 cells was examined following treatment with derivatives. Most of the compounds demonstrated significant inhibitory effects, particularly compounds KJ-5 and KJ-12 with IC values of 4.29 �� 0.10 and 4.07 �� 0.09 ��M, respectively. Furthermore, both compounds 5 and 12 significantly caused cell apoptosis, G2/M arrest, and DNA damage, and suppressed invasion and migration in a concentration-dependent manner. In addition, KJ-5 and KJ-12 could trigger apoptosis via the mitochondrial pathway by increasing the ratio of Bax/Bcl-2 and activating cleaved caspase-9, cleaved caspase-3, and cleaved PARP.
