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Updated: Sep 25, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Facile synthesis and biological evaluation of tryptamine-piperazine-2,5-dione conjugates as anticancer agents
Jiang-Ping Meng1, Shi-Qiang Li1, Yan Tang1
1National & Local Joint Engineering Research Center of Targeted and Innovative Therapeutics, IATTI, College of Pharmacy, Chongqing University of Arts and Sciences Chongqing 402160 China LixiaGao@cqwu.edu.cn.
Abstract:
A facile and efficient route to synthesize N-heterocyclic fused tryptamine-piperazine-2,5-dione conjugates was developed via a post-Ugi cascade reaction. The targeted compounds were prepared by means of a mild reaction and simple operation procedure, which could be applied to a broad scope of starting materials. Compound 6h was demonstrated to induce significant growth inhibition of AsPC-1 and SW1990 human pancreatic cancer cell lines (IC50 = 6 ± 0.85 μM). Our protocol allows for the construction of a structurally diverse compound library and paves a new avenue for the discovery of pancreatic cancer drug candidates.
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