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Updated: Aug 3, 2025

Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
Published on: May 28, 2014
Development of a zinc(II) 2-pyridinecarboxaldehyde thiosemicarbazone complex with remarkable antitumor and
Ming Jiang1,2, Jinhui Pang1, Xiaoying Jia1
1State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources/Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources (Ministry of Education of China), School of Chemistry and Pharmaceutical Sciences, Collaborative Innovation Center for Guangxi Ethnic Medicine, Guangxi Normal University, 15 Yucai Road, Guilin, Guangxi, 541004, China. fyang@mailbox.gxnu.edu.cn.
Abstract:
To develop the next-generation metal agents for efficiently inhibiting tumor growth, we synthesized a series of new Zn(II) complexes (C1-C5) derived from 2-pyridinecarboxaldehyde thiosemicarbazone and investigated their structure-activity relationships. C5 bearing two methyl groups at the N-4 position of the ligand exerted the strongest inhibition effect among all the Zn(II) complexes. Importantly, C5 exerted an effective inhibitory effect on tumor growth and produced few side effects in vivo. We further confirmed the antitumor mechanisms of C5, including arresting the cell cycle at the S phase, inducing apoptosis, inducing lethal autophagy, and suppressing angiogenesis.
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