| Affiliation: | 1. Department of Biological Sciences, Konkuk University, Seoul 05029, Republic of Korea;2. Division of Bioscience and Biotechnology, BBRC, Konkuk University, Seoul 05029, Republic of Korea;3. Department of Applied Chemistry, Dongduk Women’s University, Seoul 02748, Republic of Korea;1. Research Center for New Energy Technology, Shanghai Institute of Microsystem and Information Technology, 235 Chengbei Road, Jiading, 201800 Shanghai, PR China;2. University of Chinese Academy of Sciences, 100039 Beijing, PR China;1. Xinjiang Fishery Research Institute, 614 West Xihong Road, Urumqi 830000, China;2. Institute of Evolution & Marine Biodiversity, Ocean University of China, 5 Yushan Road, Qingdao 266003, China;3. Fisheries College of Huazhong Agricultural University, 1 Shizishan Street, Wuhan 430070, China;1. School of Physics and Materials Science, Anhui University, Hefei, 230601, China;2. Anhui Key Laboratory of Information Materials and Devices, Hefei 230601, China |
| Abstract: | A moderate elevation in reactive oxygen species (ROS) levels can generally be controlled in normal cells, but may lead to death of cancer cells as the ROS level in cancer cells is already elevated. Therefore, a ROS-generating compound can act as a selective chemotherapeutic agent for cancer cells that does not affect normal cells. In our previous study, a compound containing a Michael acceptor was selectively cytotoxic to cancer cells without affecting normal cells; therefore, we designed and synthesized 26 compounds containing a Michael acceptor. Their cytotoxicities against HCT116 human colon cancer cell lines were measured by using a clonogenic long-term survival assay. To derive the structural conditions required to obtain stronger cytotoxicity against cancer cells, the relationships between the half-maximal cell growth inhibitory concentration values of the synthesized compounds and their physicochemical properties were evaluated by Comparative Molecular Field Analysis and Comparative Molecular Similarity Indices Analysis. It was confirmed that the compound with the best half-maximal cell growth inhibitory concentration triggered apoptosis through ROS generation, which then led to stimulation of the caspase pathway. |
