Synthesis, mechanisms of action, and toxicity of novel aminophosphonates derivatives conjugated irinotecan in vitro and in vivo as potent antitumor agents
Twenty novel aminophosphonates derivatives (5a-5j and 6a-6j) conjugated irinotecan were synthesized through esterification reaction, and evaluated their anticancer activities using MTT assay. In vitro evaluation revealed that they displayed similar or superior cytotoxicity compared to the positive drug irinotecan against A549, MCF-7, SK-OV-3, MG-63, U2OS and multidrug-resistant (MDR) SK-OV-3/CDDP cancer cell lines. Among them, 9b displayed the most potent activity, with IC
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National Natural Science Foundation of China Grant 21977021National Natural Science Foundation of China Grant 81760626Ministry of Education Grant IRT_16R15Ministry of Education Grant 2016GXNSFGA380005Natural Science Foundation of Guangxi Province Grant AB17292075Key University Science Research Project of Jiangsu Province Grant 18KJA360001National Science Foundation of the Jiangsu Higher Education Institutions of China Grant 19KJA150008Jiangsu Key Laboratory of Regional Resource Exploitation and Medicinal Research Grant LPRK201805Jiangsu Key Laboratory of Regional Resource Exploitation and Medicinal Research Grant LPRK201902natural science research in Colleges and universities of Jiangsu Province Grant 18KJA530002