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Facile synthesis and biological evaluation of tryptamine-piperazine-2,5-dione conjugates as anticancer agents.

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.

SUBMITTER: Meng JP

PROVIDER: S-EPMC9037805 | biostudies-literature | 2021 Aug

REPOSITORIES: biostudies-literature

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Facile synthesis and biological evaluation of tryptamine-piperazine-2,5-dione conjugates as anticancer agents.

Meng Jiang-Ping JP Li Shi-Qiang SQ Tang Yan Y Xu Zhi-Gang ZG Chen Zhong-Zhu ZZ Gao Li-Xia LX

RSC advances 20210817 45

A facile and efficient route to synthesize N-heterocyclic fused tryptamine-piperazine-2,5-dione conjugates was developed <i>via</i> 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 (IC<sub>50</sub> = 6 ± 0.85 μM). Our protocol allows f ...[more]

PMID: 35480764

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