Design and Synthesis of Novel Tetrapeptide Analogues as New Cytotoxic Agents

New series of compounds based on a tetrapeptide scaffold containing methyl sulfonyl group at the para position of a phenyl ring were synthesized and their cytotoxic activities were examined against several human cancer cell lines including MCF-7 (breast cancer Cell Line), HepG2 (human liver cancer C...

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Main Authors: Mohammad Ali Ahmaditaba, Mohammad Hassan Houshdar Tehrani, Afshin Zarghi, Sorayya Shahosseini, Sara Hariri
Format: Article
Language:English
Published: Shahid Beheshti University of Medical Sciences 2017-09-01
Series:Trends in Peptide and Protein Sciences
Subjects:
Online Access:https://journals.sbmu.ac.ir/protein/article/view/17476
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author Mohammad Ali Ahmaditaba
Mohammad Hassan Houshdar Tehrani
Afshin Zarghi
Sorayya Shahosseini
Sara Hariri
author_facet Mohammad Ali Ahmaditaba
Mohammad Hassan Houshdar Tehrani
Afshin Zarghi
Sorayya Shahosseini
Sara Hariri
author_sort Mohammad Ali Ahmaditaba
collection DOAJ
description New series of compounds based on a tetrapeptide scaffold containing methyl sulfonyl group at the para position of a phenyl ring were synthesized and their cytotoxic activities were examined against several human cancer cell lines including MCF-7 (breast cancer Cell Line), HepG2 (human liver cancer Cell Line), HT-29 (Human Colorectal Adenocarcinoma Cell Line) and A549 (adenocarcinomic human alveolar basal epithelial cells) using MTT assay. Based on the results, among the synthesized peptides, 5e, 5f, 1g, and 3g were the most potent cytotoxic compounds that were more toxic than the reference compound, Celecoxib, against the tested cell lines. These compounds could be candidate for finding cytotoxic agents with new peptide scaffolds which show COX-2 inhibitory activity as well.   HIGHLIGHTS •A group of tetrapeptides was reported as COX-2 inhibitors with antiproliferative activity. •New tetrapeptides containing methyl sulfonyl group at the para position of a phenyl ring were synthesized. •Some of novel compounds exhibited more potent cytotoxic effect than Celecoxib as the reference.
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spelling doaj.art-4df29774617a4e268a04ba981607bc8a2022-12-21T19:29:53ZengShahid Beheshti University of Medical SciencesTrends in Peptide and Protein Sciences2538-24462017-09-011416717610.22037/tpps.v1i4.1747617476Design and Synthesis of Novel Tetrapeptide Analogues as New Cytotoxic AgentsMohammad Ali AhmaditabaMohammad Hassan Houshdar TehraniAfshin ZarghiSorayya ShahosseiniSara HaririNew series of compounds based on a tetrapeptide scaffold containing methyl sulfonyl group at the para position of a phenyl ring were synthesized and their cytotoxic activities were examined against several human cancer cell lines including MCF-7 (breast cancer Cell Line), HepG2 (human liver cancer Cell Line), HT-29 (Human Colorectal Adenocarcinoma Cell Line) and A549 (adenocarcinomic human alveolar basal epithelial cells) using MTT assay. Based on the results, among the synthesized peptides, 5e, 5f, 1g, and 3g were the most potent cytotoxic compounds that were more toxic than the reference compound, Celecoxib, against the tested cell lines. These compounds could be candidate for finding cytotoxic agents with new peptide scaffolds which show COX-2 inhibitory activity as well.   HIGHLIGHTS •A group of tetrapeptides was reported as COX-2 inhibitors with antiproliferative activity. •New tetrapeptides containing methyl sulfonyl group at the para position of a phenyl ring were synthesized. •Some of novel compounds exhibited more potent cytotoxic effect than Celecoxib as the reference.https://journals.sbmu.ac.ir/protein/article/view/17476cytotoxic activitymethyl sulfonyl groupmttsynthesistetrapeptide scaffold
spellingShingle Mohammad Ali Ahmaditaba
Mohammad Hassan Houshdar Tehrani
Afshin Zarghi
Sorayya Shahosseini
Sara Hariri
Design and Synthesis of Novel Tetrapeptide Analogues as New Cytotoxic Agents
Trends in Peptide and Protein Sciences
cytotoxic activity
methyl sulfonyl group
mtt
synthesis
tetrapeptide scaffold
title Design and Synthesis of Novel Tetrapeptide Analogues as New Cytotoxic Agents
title_full Design and Synthesis of Novel Tetrapeptide Analogues as New Cytotoxic Agents
title_fullStr Design and Synthesis of Novel Tetrapeptide Analogues as New Cytotoxic Agents
title_full_unstemmed Design and Synthesis of Novel Tetrapeptide Analogues as New Cytotoxic Agents
title_short Design and Synthesis of Novel Tetrapeptide Analogues as New Cytotoxic Agents
title_sort design and synthesis of novel tetrapeptide analogues as new cytotoxic agents
topic cytotoxic activity
methyl sulfonyl group
mtt
synthesis
tetrapeptide scaffold
url https://journals.sbmu.ac.ir/protein/article/view/17476
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AT afshinzarghi designandsynthesisofnoveltetrapeptideanaloguesasnewcytotoxicagents
AT sorayyashahosseini designandsynthesisofnoveltetrapeptideanaloguesasnewcytotoxicagents
AT sarahariri designandsynthesisofnoveltetrapeptideanaloguesasnewcytotoxicagents