Synthesis of Chalcones with Anticancer Activities

Several chalcones were synthesized and their<em> in vitro </em>cytotoxicity against various human cell lines, including human breast adenocarcinoma cell line MCF-7, human lung adenocarcinoma cell line A549, human prostate cancer cell line PC3, human adenocarcinoma cell li...

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Main Authors: Syam Mohan, Siddig Ibrahim Abdelwahab, Suvitha Syam, Mohammed Ali Al-Mamary
Format: Article
Language:English
Published: MDPI AG 2012-05-01
Series:Molecules
Subjects:
Online Access:http://www.mdpi.com/1420-3049/17/6/6179
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author Syam Mohan
Siddig Ibrahim Abdelwahab
Suvitha Syam
Mohammed Ali Al-Mamary
author_facet Syam Mohan
Siddig Ibrahim Abdelwahab
Suvitha Syam
Mohammed Ali Al-Mamary
author_sort Syam Mohan
collection DOAJ
description Several chalcones were synthesized and their<em> in vitro </em>cytotoxicity against various human cell lines, including human breast adenocarcinoma cell line MCF-7, human lung adenocarcinoma cell line A549, human prostate cancer cell line PC3, human adenocarcinoma cell line HT-29 (colorectal cancer) and human<strong> </strong>normal liver cell line WRL-68 was evaluated. Most of the compounds being active cytotoxic agents, four of them with minimal IC<sub>50</sub> values were chosen and studied in detail with MCF-7 cells. The compounds <strong>1</strong>, <strong>5</strong>, <strong>23</strong>, and <strong>25</strong> were capable in eliciting apoptosis in MCF-7 cells as shown by multiparameter cytotoxicity assay and caspase-3/7, -8, and -9 activities (<em>p</em> < 0.05). The ROS level showed 1.3-fold increase (<em>p</em> < 0.05) at the low concentrations used and thus it was concluded that the compounds increased the ROS level eventually leading to apoptosis in MCF-7 cells through intrinsic as well as extrinsic pathways.
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spelling doaj.art-3091bc706ee54123881722a02172d4802022-12-21T17:48:17ZengMDPI AGMolecules1420-30492012-05-011766179619510.3390/molecules17066179Synthesis of Chalcones with Anticancer ActivitiesSyam MohanSiddig Ibrahim AbdelwahabSuvitha SyamMohammed Ali Al-MamarySeveral chalcones were synthesized and their<em> in vitro </em>cytotoxicity against various human cell lines, including human breast adenocarcinoma cell line MCF-7, human lung adenocarcinoma cell line A549, human prostate cancer cell line PC3, human adenocarcinoma cell line HT-29 (colorectal cancer) and human<strong> </strong>normal liver cell line WRL-68 was evaluated. Most of the compounds being active cytotoxic agents, four of them with minimal IC<sub>50</sub> values were chosen and studied in detail with MCF-7 cells. The compounds <strong>1</strong>, <strong>5</strong>, <strong>23</strong>, and <strong>25</strong> were capable in eliciting apoptosis in MCF-7 cells as shown by multiparameter cytotoxicity assay and caspase-3/7, -8, and -9 activities (<em>p</em> < 0.05). The ROS level showed 1.3-fold increase (<em>p</em> < 0.05) at the low concentrations used and thus it was concluded that the compounds increased the ROS level eventually leading to apoptosis in MCF-7 cells through intrinsic as well as extrinsic pathways.http://www.mdpi.com/1420-3049/17/6/6179chalconesyntheticcytotoxicityMCF-7 cellsapoptosishigh content screeningcaspaseROS
spellingShingle Syam Mohan
Siddig Ibrahim Abdelwahab
Suvitha Syam
Mohammed Ali Al-Mamary
Synthesis of Chalcones with Anticancer Activities
Molecules
chalcone
synthetic
cytotoxicity
MCF-7 cells
apoptosis
high content screening
caspase
ROS
title Synthesis of Chalcones with Anticancer Activities
title_full Synthesis of Chalcones with Anticancer Activities
title_fullStr Synthesis of Chalcones with Anticancer Activities
title_full_unstemmed Synthesis of Chalcones with Anticancer Activities
title_short Synthesis of Chalcones with Anticancer Activities
title_sort synthesis of chalcones with anticancer activities
topic chalcone
synthetic
cytotoxicity
MCF-7 cells
apoptosis
high content screening
caspase
ROS
url http://www.mdpi.com/1420-3049/17/6/6179
work_keys_str_mv AT syammohan synthesisofchalconeswithanticanceractivities
AT siddigibrahimabdelwahab synthesisofchalconeswithanticanceractivities
AT suvithasyam synthesisofchalconeswithanticanceractivities
AT mohammedalialmamary synthesisofchalconeswithanticanceractivities