Synthesis and pharmacological evaluation of polyamine-diarylidenyl piperidone derivatives as potent antitumor agents

Two polyamine-diarylidenyl piperidone (DAP) derivatives, dimer polyamine-H-4073 and tetrameric polyamine-H-4073, were designed and synthesized as antitumor agents by coupling the bifluoro-substituted DAP STAT3 inhibitor H-4073 to two different polyamines through the binary fatty acid chains, respect...

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Bibliographic Details
Published in:Monatshefte für Chemie 2024-07, Vol.155 (7), p.747-753
Main Authors: Mao, Zhi-Chen, Liu, Shuang-Qiang, Chen, Xiao-Man, Wei, Jian-Hua, Huang, Ri-Zhen, Zhang, Ye
Format: Article
Language:English
Subjects:
Analytical Chemistry
Chemistry
Chemistry and Materials Science
Chemistry/Food Science
Dimers
Doxorubicin
Inhibitors
Inorganic Chemistry
Low resistance
Organic Chemistry
Original Paper
Physical Chemistry
Polyamines
Theoretical and Computational Chemistry
Xenotransplantation
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Summary:Two polyamine-diarylidenyl piperidone (DAP) derivatives, dimer polyamine-H-4073 and tetrameric polyamine-H-4073, were designed and synthesized as antitumor agents by coupling the bifluoro-substituted DAP STAT3 inhibitor H-4073 to two different polyamines through the binary fatty acid chains, respectively. MTT assay and a SW480 xenograft model identified dimer polyamine-H-4073 as good candidate antitumor agent with good efficacy, limited toxicity, and low resistance, in comparison with H-4073, cisplatin, and doxorubicin. Western blot analysis results indicated that dimer polyamine-H-4073 exhibited effectively inhibition on signal transducer and activator of transcription 3 (STAT3), indicating that it may be a STAT3 inhibitor. Graphical abstract
ISSN:0026-9247
1434-4475
DOI:10.1007/s00706-024-03220-5