Synthesis and Structure-Activity Relationships of Fenbufen Amide Analogs
The previous discoveries of butyl fenbufen amide analogs with antitumor effects were further examined. The amide analogs with 1, 3, 4 and 8 carbons chains were prepared in 70-80% yield. Fenbufen had no cytotoxic effects at concentrations ranging from 10 to 100 μM. Methyl fenbufen amide had significa...
Main Authors: | , , , , , |
---|---|
Format: | Article |
Language: | English |
Published: |
MDPI AG
2010-12-01
|
Series: | Molecules |
Subjects: | |
Online Access: | http://www.mdpi.com/1420-3049/15/12/8796/ |
id |
doaj-81126daf9e6749288bf49a915940380e |
---|---|
record_format |
Article |
spelling |
doaj-81126daf9e6749288bf49a915940380e2020-11-24T23:44:06ZengMDPI AGMolecules1420-30492010-12-0115128796880310.3390/molecules15128796Synthesis and Structure-Activity Relationships of Fenbufen Amide AnalogsChia-Wen HuangKun-I LinYu-Chun HuangJhen-Yi JianChao-Hsun YangChung-Shan YuThe previous discoveries of butyl fenbufen amide analogs with antitumor effects were further examined. The amide analogs with 1, 3, 4 and 8 carbons chains were prepared in 70-80% yield. Fenbufen had no cytotoxic effects at concentrations ranging from 10 to 100 μM. Methyl fenbufen amide had significant cytotoxic effects at a concentration of 100 μM. As the length of the alkyl amide side chain increased, the cytotoxic effects increased, and the octyl fenbufen amide had the greatest cytotoxic effect. After treatment with 30 μM octyl fenbufen amide, nearly seventy percent of the cells lost their viability. At the concentration of 10 μM, fenbufen amide analogs did not show cytotoxicity according to the MTT assay results. The NO scavenging activities of the fenbufen amide analogs were not significantly different from those of fenbufen. http://www.mdpi.com/1420-3049/15/12/8796/macrophage RAW 264.7nitric oxideanti-inflammatoryfenbufen amide analog |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Chia-Wen Huang Kun-I Lin Yu-Chun Huang Jhen-Yi Jian Chao-Hsun Yang Chung-Shan Yu |
spellingShingle |
Chia-Wen Huang Kun-I Lin Yu-Chun Huang Jhen-Yi Jian Chao-Hsun Yang Chung-Shan Yu Synthesis and Structure-Activity Relationships of Fenbufen Amide Analogs Molecules macrophage RAW 264.7 nitric oxide anti-inflammatory fenbufen amide analog |
author_facet |
Chia-Wen Huang Kun-I Lin Yu-Chun Huang Jhen-Yi Jian Chao-Hsun Yang Chung-Shan Yu |
author_sort |
Chia-Wen Huang |
title |
Synthesis and Structure-Activity Relationships of Fenbufen Amide Analogs |
title_short |
Synthesis and Structure-Activity Relationships of Fenbufen Amide Analogs |
title_full |
Synthesis and Structure-Activity Relationships of Fenbufen Amide Analogs |
title_fullStr |
Synthesis and Structure-Activity Relationships of Fenbufen Amide Analogs |
title_full_unstemmed |
Synthesis and Structure-Activity Relationships of Fenbufen Amide Analogs |
title_sort |
synthesis and structure-activity relationships of fenbufen amide analogs |
publisher |
MDPI AG |
series |
Molecules |
issn |
1420-3049 |
publishDate |
2010-12-01 |
description |
The previous discoveries of butyl fenbufen amide analogs with antitumor effects were further examined. The amide analogs with 1, 3, 4 and 8 carbons chains were prepared in 70-80% yield. Fenbufen had no cytotoxic effects at concentrations ranging from 10 to 100 μM. Methyl fenbufen amide had significant cytotoxic effects at a concentration of 100 μM. As the length of the alkyl amide side chain increased, the cytotoxic effects increased, and the octyl fenbufen amide had the greatest cytotoxic effect. After treatment with 30 μM octyl fenbufen amide, nearly seventy percent of the cells lost their viability. At the concentration of 10 μM, fenbufen amide analogs did not show cytotoxicity according to the MTT assay results. The NO scavenging activities of the fenbufen amide analogs were not significantly different from those of fenbufen. |
topic |
macrophage RAW 264.7 nitric oxide anti-inflammatory fenbufen amide analog |
url |
http://www.mdpi.com/1420-3049/15/12/8796/ |
work_keys_str_mv |
AT chiawenhuang synthesisandstructureactivityrelationshipsoffenbufenamideanalogs AT kunilin synthesisandstructureactivityrelationshipsoffenbufenamideanalogs AT yuchunhuang synthesisandstructureactivityrelationshipsoffenbufenamideanalogs AT jhenyijian synthesisandstructureactivityrelationshipsoffenbufenamideanalogs AT chaohsunyang synthesisandstructureactivityrelationshipsoffenbufenamideanalogs AT chungshanyu synthesisandstructureactivityrelationshipsoffenbufenamideanalogs |
_version_ |
1725500067546136576 |