Novel piperazinediones as antitumor agents

Chun Li Wang; On Lee; George Hsiao; Jang Feng Lian; Yu Wen Cheng

Novel piperazinediones as antitumor agents

Chun Li Wang, On Lee, George Hsiao, Jang Feng Lian, Yu Wen Cheng

Research output: Contribution to journal › Article › peer-review

Abstract

Chemical modification of dipeptide mimetic azatyrosine led to a series of piperazinediones. Thirteen piperazinediones were synthesized and tested for their anticancer activity. This series of piperazinedione compounds exhibited potent anticancer activities against human disease-oriented cancer cell lines in NCI60 cancer screening (National Cancer Institute, USA). Among them, four leads (compound 10, 18, 21, and 22) exhibited in vitro tumor growth suppression, reducing tumor cell growth to 45.7%-56.3%, and exhibited broad-spectrum activities. Compound 18, with 50% cancer cell growth inhibition (GI₅₀)

Original language	English
Pages (from-to)	4013-4020
Number of pages	8
Journal	Anticancer Research
Volume	34
Issue number	8
Publication status	Published - Aug 1 2014

Keywords

Azatyrosinamide
COMPARE algorithm
DTP
In vivo antitumor activity
Mechanism of action prediction
NCI-60 anticancer screening
NCI/NIH
Piperazinediones
Tubulin polymerization inhibitor

ASJC Scopus subject areas

Oncology
Cancer Research

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

Cite this

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title = "Novel piperazinediones as antitumor agents",

abstract = "Chemical modification of dipeptide mimetic azatyrosine led to a series of piperazinediones. Thirteen piperazinediones were synthesized and tested for their anticancer activity. This series of piperazinedione compounds exhibited potent anticancer activities against human disease-oriented cancer cell lines in NCI60 cancer screening (National Cancer Institute, USA). Among them, four leads (compound 10, 18, 21, and 22) exhibited in vitro tumor growth suppression, reducing tumor cell growth to 45.7%-56.3%, and exhibited broad-spectrum activities. Compound 18, with 50% cancer cell growth inhibition (GI50) ",

keywords = "Azatyrosinamide, COMPARE algorithm, DTP, In vivo antitumor activity, Mechanism of action prediction, NCI-60 anticancer screening, NCI/NIH, Piperazinediones, Tubulin polymerization inhibitor",

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year = "2014",

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language = "English",

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journal = "Anticancer Research",

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TY - JOUR

T1 - Novel piperazinediones as antitumor agents

AU - Wang, Chun Li

AU - Lee, On

AU - Hsiao, George

AU - Lian, Jang Feng

AU - Cheng, Yu Wen

PY - 2014/8/1

Y1 - 2014/8/1

N2 - Chemical modification of dipeptide mimetic azatyrosine led to a series of piperazinediones. Thirteen piperazinediones were synthesized and tested for their anticancer activity. This series of piperazinedione compounds exhibited potent anticancer activities against human disease-oriented cancer cell lines in NCI60 cancer screening (National Cancer Institute, USA). Among them, four leads (compound 10, 18, 21, and 22) exhibited in vitro tumor growth suppression, reducing tumor cell growth to 45.7%-56.3%, and exhibited broad-spectrum activities. Compound 18, with 50% cancer cell growth inhibition (GI50)

AB - Chemical modification of dipeptide mimetic azatyrosine led to a series of piperazinediones. Thirteen piperazinediones were synthesized and tested for their anticancer activity. This series of piperazinedione compounds exhibited potent anticancer activities against human disease-oriented cancer cell lines in NCI60 cancer screening (National Cancer Institute, USA). Among them, four leads (compound 10, 18, 21, and 22) exhibited in vitro tumor growth suppression, reducing tumor cell growth to 45.7%-56.3%, and exhibited broad-spectrum activities. Compound 18, with 50% cancer cell growth inhibition (GI50)

KW - Azatyrosinamide

KW - COMPARE algorithm

KW - DTP

KW - In vivo antitumor activity

KW - Mechanism of action prediction

KW - NCI-60 anticancer screening

KW - NCI/NIH

KW - Piperazinediones

KW - Tubulin polymerization inhibitor

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M3 - Article

C2 - 25075024

AN - SCOPUS:84908667301

SN - 0250-7005

VL - 34

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JO - Anticancer Research

JF - Anticancer Research

IS - 8

ER -

Novel piperazinediones as antitumor agents

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

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