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

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 starti...

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Detalles Bibliográficos
Autores principales: Meng, Jiang-Ping, Li, Shi-Qiang, Tang, Yan, Xu, Zhi-Gang, Chen, Zhong-Zhu, Gao, Li-Xia
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9037805/
https://www.ncbi.nlm.nih.gov/pubmed/35480764
http://dx.doi.org/10.1039/d1ra03740d
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author Meng, Jiang-Ping
Li, Shi-Qiang
Tang, Yan
Xu, Zhi-Gang
Chen, Zhong-Zhu
Gao, Li-Xia
author_facet Meng, Jiang-Ping
Li, Shi-Qiang
Tang, Yan
Xu, Zhi-Gang
Chen, Zhong-Zhu
Gao, Li-Xia
author_sort Meng, Jiang-Ping
collection PubMed
description 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 (IC(50) = 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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spelling pubmed-90378052022-04-26 Facile synthesis and biological evaluation of tryptamine-piperazine-2,5-dione conjugates as anticancer agents Meng, Jiang-Ping Li, Shi-Qiang Tang, Yan Xu, Zhi-Gang Chen, Zhong-Zhu Gao, Li-Xia RSC Adv Chemistry 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 (IC(50) = 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. The Royal Society of Chemistry 2021-08-17 /pmc/articles/PMC9037805/ /pubmed/35480764 http://dx.doi.org/10.1039/d1ra03740d Text en This journal is © The Royal Society of Chemistry https://creativecommons.org/licenses/by-nc/3.0/
spellingShingle Chemistry
Meng, Jiang-Ping
Li, Shi-Qiang
Tang, Yan
Xu, Zhi-Gang
Chen, Zhong-Zhu
Gao, Li-Xia
Facile synthesis and biological evaluation of tryptamine-piperazine-2,5-dione conjugates as anticancer agents
title Facile synthesis and biological evaluation of tryptamine-piperazine-2,5-dione conjugates as anticancer agents
title_full Facile synthesis and biological evaluation of tryptamine-piperazine-2,5-dione conjugates as anticancer agents
title_fullStr Facile synthesis and biological evaluation of tryptamine-piperazine-2,5-dione conjugates as anticancer agents
title_full_unstemmed Facile synthesis and biological evaluation of tryptamine-piperazine-2,5-dione conjugates as anticancer agents
title_short Facile synthesis and biological evaluation of tryptamine-piperazine-2,5-dione conjugates as anticancer agents
title_sort facile synthesis and biological evaluation of tryptamine-piperazine-2,5-dione conjugates as anticancer agents
topic Chemistry
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9037805/
https://www.ncbi.nlm.nih.gov/pubmed/35480764
http://dx.doi.org/10.1039/d1ra03740d
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