Synthesis and cytotoxicity of 2,5-dihydroxychalcones and related compounds

Nguyen Hai Nam; Dong Ho Hong; Young Jae You; Yong Kim; Seong Cheol Bang; Hwan Mook Kim; Byung Zun Ahn

doi:10.1007/BF02980153

Synthesis and cytotoxicity of 2,5-dihydroxychalcones and related compounds

Nguyen Hai Nam
, Dong Ho Hong
, Young Jae You
, Yong Kim
, Seong Cheol Bang
, Hwan Mook Kim
, Byung Zun Ahn

Pharmaceutical Sciences

Chungnam National University
Korea Research Institute of Bioscience and Biotechnology

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

17 Scopus citations

Abstract

A series of 2, 5-dihydroxychalcones and related compounds were synthesized, and their cytotoxicities against tumor cell lines and human umbilical venous endothelial cells (HUVEC) evaluated. It was found that chalcones, with electron-withdrawing substituents on an A ring, exhibited significant cytotoxicities. Among the synthesized compounds, 2′-chloro-2, 5-dihydroxychalcone (9) was most potent, with an IC₅₀ value as low as 0.31 μg/mL. This compound also exhibited a significant cytotoxic selectivity toward HUVEC.

Original language	English
Pages (from-to)	581-588
Number of pages	8
Journal	Archives of Pharmacal Research
Volume	27
Issue number	6
DOIs	https://doi.org/10.1007/BF02980153
State	Published - Jun 30 2004

Keywords

Chalcone
Cytotoxicity
Structure-activity relationship

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10.1007/BF02980153

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title = "Synthesis and cytotoxicity of 2,5-dihydroxychalcones and related compounds",

abstract = "A series of 2, 5-dihydroxychalcones and related compounds were synthesized, and their cytotoxicities against tumor cell lines and human umbilical venous endothelial cells (HUVEC) evaluated. It was found that chalcones, with electron-withdrawing substituents on an A ring, exhibited significant cytotoxicities. Among the synthesized compounds, 2′-chloro-2, 5-dihydroxychalcone (9) was most potent, with an IC50 value as low as 0.31 μg/mL. This compound also exhibited a significant cytotoxic selectivity toward HUVEC.",

keywords = "Chalcone, Cytotoxicity, Structure-activity relationship",

author = "Nam, \{Nguyen Hai\} and Hong, \{Dong Ho\} and You, \{Young Jae\} and Yong Kim and Bang, \{Seong Cheol\} and Kim, \{Hwan Mook\} and Ahn, \{Byung Zun\}",

year = "2004",

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doi = "10.1007/BF02980153",

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T1 - Synthesis and cytotoxicity of 2,5-dihydroxychalcones and related compounds

AU - Nam, Nguyen Hai

AU - Hong, Dong Ho

AU - You, Young Jae

AU - Kim, Yong

AU - Bang, Seong Cheol

AU - Kim, Hwan Mook

AU - Ahn, Byung Zun

PY - 2004/6/30

Y1 - 2004/6/30

N2 - A series of 2, 5-dihydroxychalcones and related compounds were synthesized, and their cytotoxicities against tumor cell lines and human umbilical venous endothelial cells (HUVEC) evaluated. It was found that chalcones, with electron-withdrawing substituents on an A ring, exhibited significant cytotoxicities. Among the synthesized compounds, 2′-chloro-2, 5-dihydroxychalcone (9) was most potent, with an IC50 value as low as 0.31 μg/mL. This compound also exhibited a significant cytotoxic selectivity toward HUVEC.

AB - A series of 2, 5-dihydroxychalcones and related compounds were synthesized, and their cytotoxicities against tumor cell lines and human umbilical venous endothelial cells (HUVEC) evaluated. It was found that chalcones, with electron-withdrawing substituents on an A ring, exhibited significant cytotoxicities. Among the synthesized compounds, 2′-chloro-2, 5-dihydroxychalcone (9) was most potent, with an IC50 value as low as 0.31 μg/mL. This compound also exhibited a significant cytotoxic selectivity toward HUVEC.

KW - Chalcone

KW - Cytotoxicity

KW - Structure-activity relationship

UR - https://www.scopus.com/pages/publications/21644442255

U2 - 10.1007/BF02980153

DO - 10.1007/BF02980153

M3 - Article

C2 - 15283456

AN - SCOPUS:21644442255

SN - 0253-6269

VL - 27

SP - 581

EP - 588

JO - Archives of Pharmacal Research

JF - Archives of Pharmacal Research

IS - 6

ER -

Synthesis and cytotoxicity of 2,5-dihydroxychalcones and related compounds

Abstract

Keywords

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