Dual Anti-cancer and Anti-Itch Activity of PD176252 Analogues: Design, Synthesis and Biological Evaluation.
Identifieur interne : 000056 ( PubMed/Corpus ); précédent : 000055; suivant : 000057Dual Anti-cancer and Anti-Itch Activity of PD176252 Analogues: Design, Synthesis and Biological Evaluation.
Auteurs : Ming-Jun Yu ; Sen Yao ; Ting-Ting Li ; Rui Yang ; Ri-Sheng YaoSource :
- Anti-cancer agents in medicinal chemistry [ 1875-5992 ] ; 2019.
English descriptors
- KwdEn :
- Animals, Antineoplastic Agents (chemical synthesis), Antineoplastic Agents (chemistry), Antineoplastic Agents (pharmacology), Antipruritics (chemical synthesis), Antipruritics (chemistry), Antipruritics (pharmacology), Cell Proliferation (drug effects), Dose-Response Relationship, Drug, Drug Design, Drug Screening Assays, Antitumor, Female, Humans, Indoles (chemical synthesis), Indoles (chemistry), Indoles (pharmacology), Male, Mice, Mice, Inbred Strains, Molecular Structure, Pruritus (drug therapy), Structure-Activity Relationship, Tumor Cells, Cultured.
- MESH :
- chemical , chemical synthesis : Antineoplastic Agents, Antipruritics, Indoles.
- chemical , chemistry : Antineoplastic Agents, Antipruritics, Indoles.
- chemical , pharmacology : Antineoplastic Agents, Antipruritics, Indoles.
- drug effects : Cell Proliferation.
- drug therapy : Pruritus.
- Animals, Dose-Response Relationship, Drug, Drug Design, Drug Screening Assays, Antitumor, Female, Humans, Male, Mice, Mice, Inbred Strains, Molecular Structure, Structure-Activity Relationship, Tumor Cells, Cultured.
Abstract
Cancer patients treated with targeted anti-cancer drug suffer from itch or pruritus. Itch or pruritus is an unpleasant sensation that brings about a negative impact on quality of life, and serious itch may lead to dose reduction and even discontinuation. Gastrin releasing peptide receptor (GRPR) plays a critical role in itch, inflammation and cancer, and GRPR antagonist has obvious effect on cancer, inflammation and itch. The aim of this paper is to develop a new agent with anti-cancer and anti-itch activity.
DOI: 10.2174/1871520619666190408133141
PubMed: 30961511
Links to Exploration step
pubmed:30961511Le document en format XML
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China.</nlm:affiliation></affiliation></author><author><name sortKey="Yang, Rui" sort="Yang, Rui" uniqKey="Yang R" first="Rui" last="Yang">Rui Yang</name><affiliation><nlm:affiliation>School of Food and Biological Engineering, Hefei University of Technology, Hefei 230009, China.</nlm:affiliation></affiliation></author><author><name sortKey="Yao, Ri Sheng" sort="Yao, Ri Sheng" uniqKey="Yao R" first="Ri-Sheng" last="Yao">Ri-Sheng Yao</name><affiliation><nlm:affiliation>School of Food and Biological Engineering, Hefei University of Technology, Hefei 230009, China.</nlm:affiliation></affiliation></author></titleStmt><publicationStmt><idno type="wicri:source">PubMed</idno><date when="2019">2019</date><idno type="RBID">pubmed:30961511</idno><idno type="pmid">30961511</idno><idno type="doi">10.2174/1871520619666190408133141</idno><idno type="wicri:Area/PubMed/Corpus">000056</idno><idno type="wicri:explorRef" wicri:stream="PubMed" wicri:step="Corpus" wicri:corpus="PubMed">000056</idno></publicationStmt><sourceDesc><biblStruct><analytic><title xml:lang="en">Dual Anti-cancer and Anti-Itch Activity of PD176252 Analogues: Design, Synthesis and Biological Evaluation.</title><author><name sortKey="Yu, Ming Jun" sort="Yu, Ming Jun" uniqKey="Yu M" first="Ming-Jun" last="Yu">Ming-Jun Yu</name><affiliation><nlm:affiliation>School of Food and Biological Engineering, Hefei University of Technology, Hefei 230009, China.</nlm:affiliation></affiliation></author><author><name sortKey="Yao, Sen" sort="Yao, Sen" uniqKey="Yao S" first="Sen" last="Yao">Sen Yao</name><affiliation><nlm:affiliation>School of Food and Biological Engineering, Hefei University of Technology, Hefei 230009, China.</nlm:affiliation></affiliation></author><author><name sortKey="Li, Ting Ting" sort="Li, Ting Ting" uniqKey="Li T" first="Ting-Ting" last="Li">Ting-Ting Li</name><affiliation><nlm:affiliation>School of Food and Biological Engineering, Hefei University of Technology, Hefei 230009, China.</nlm:affiliation></affiliation></author><author><name sortKey="Yang, Rui" sort="Yang, Rui" uniqKey="Yang R" first="Rui" last="Yang">Rui Yang</name><affiliation><nlm:affiliation>School of Food and Biological Engineering, Hefei University of Technology, Hefei 230009, China.</nlm:affiliation></affiliation></author><author><name sortKey="Yao, Ri Sheng" sort="Yao, Ri Sheng" uniqKey="Yao R" first="Ri-Sheng" last="Yao">Ri-Sheng Yao</name><affiliation><nlm:affiliation>School of Food and Biological Engineering, Hefei University of Technology, Hefei 230009, China.</nlm:affiliation></affiliation></author></analytic><series><title level="j">Anti-cancer agents in medicinal chemistry</title><idno type="eISSN">1875-5992</idno><imprint><date when="2019" type="published">2019</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animals</term><term>Antineoplastic Agents (chemical synthesis)</term><term>Antineoplastic Agents (chemistry)</term><term>Antineoplastic Agents (pharmacology)</term><term>Antipruritics (chemical synthesis)</term><term>Antipruritics (chemistry)</term><term>Antipruritics (pharmacology)</term><term>Cell Proliferation (drug effects)</term><term>Dose-Response Relationship, Drug</term><term>Drug Design</term><term>Drug Screening Assays, Antitumor</term><term>Female</term><term>Humans</term><term>Indoles (chemical synthesis)</term><term>Indoles (chemistry)</term><term>Indoles (pharmacology)</term><term>Male</term><term>Mice</term><term>Mice, Inbred Strains</term><term>Molecular Structure</term><term>Pruritus (drug therapy)</term><term>Structure-Activity Relationship</term><term>Tumor Cells, Cultured</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemical synthesis" xml:lang="en"><term>Antineoplastic Agents</term><term>Antipruritics</term><term>Indoles</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Antineoplastic Agents</term><term>Antipruritics</term><term>Indoles</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Antineoplastic Agents</term><term>Antipruritics</term><term>Indoles</term></keywords><keywords scheme="MESH" qualifier="drug effects" xml:lang="en"><term>Cell Proliferation</term></keywords><keywords scheme="MESH" qualifier="drug therapy" xml:lang="en"><term>Pruritus</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Animals</term><term>Dose-Response Relationship, Drug</term><term>Drug Design</term><term>Drug Screening Assays, Antitumor</term><term>Female</term><term>Humans</term><term>Male</term><term>Mice</term><term>Mice, Inbred Strains</term><term>Molecular Structure</term><term>Structure-Activity Relationship</term><term>Tumor Cells, Cultured</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Cancer patients treated with targeted anti-cancer drug suffer from itch or pruritus. Itch or pruritus is an unpleasant sensation that brings about a negative impact on quality of life, and serious itch may lead to dose reduction and even discontinuation. Gastrin releasing peptide receptor (GRPR) plays a critical role in itch, inflammation and cancer, and GRPR antagonist has obvious effect on cancer, inflammation and itch. The aim of this paper is to develop a new agent with anti-cancer and anti-itch activity.</div></front></TEI><pubmed><MedlineCitation Status="MEDLINE" Owner="NLM"><PMID Version="1">30961511</PMID><DateCompleted><Year>2020</Year><Month>03</Month><Day>24</Day></DateCompleted><DateRevised><Year>2020</Year><Month>03</Month><Day>24</Day></DateRevised><Article PubModel="Print"><Journal><ISSN IssnType="Electronic">1875-5992</ISSN><JournalIssue CitedMedium="Internet"><Volume>19</Volume><Issue>8</Issue><PubDate><Year>2019</Year></PubDate></JournalIssue><Title>Anti-cancer agents in medicinal chemistry</Title><ISOAbbreviation>Anticancer Agents Med Chem</ISOAbbreviation></Journal><ArticleTitle>Dual Anti-cancer and Anti-Itch Activity of PD176252 Analogues: Design, Synthesis and Biological Evaluation.</ArticleTitle><Pagination><MedlinePgn>992-1001</MedlinePgn></Pagination><ELocationID EIdType="doi" ValidYN="Y">10.2174/1871520619666190408133141</ELocationID><Abstract><AbstractText Label="BACKGROUND">Cancer patients treated with targeted anti-cancer drug suffer from itch or pruritus. Itch or pruritus is an unpleasant sensation that brings about a negative impact on quality of life, and serious itch may lead to dose reduction and even discontinuation. Gastrin releasing peptide receptor (GRPR) plays a critical role in itch, inflammation and cancer, and GRPR antagonist has obvious effect on cancer, inflammation and itch. The aim of this paper is to develop a new agent with anti-cancer and anti-itch activity.</AbstractText><AbstractText Label="METHODS">A series of GRPR antagonist PD176252 analogues (3a-3l) were designed and synthesized. Both anticancer and anti-itch activities were evaluated. Anti-cancer activity was evaluated in three human cancer cell lines in vitro, the anti-itch activity in evaluated with Kunming mice by intrathecal injection of chloroquine phosphate as a modeling medium. And the cytotoxicity on normal cells was evaluated.</AbstractText><AbstractText Label="RESULTS">Of the tested compounds, compound 3i showed potently anti-cancer activity to all cancer cell lines tested with IC50 values of 10.5µM (lung), 11.6µM (breast) and 12.8µM (liver) respectively and it also showed significant inhibition of the scratching behavior. Comparing with PD17625, compound 3i and 3g gave better inhibition activities against all cancer cell lines, compound 3b, 3c and 3i showed better anti-itch activity. The compound 3i is safe for normal breast and liver normal cells, but it has high cytotoxicity on normal lung cell.</AbstractText><AbstractText Label="CONCLUSION">The synthesized compounds have dual anti-cancer and anti-itch activity, so the development of drug with dual anti-tumor and anti-itch property is possible.</AbstractText><CopyrightInformation>Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.</CopyrightInformation></Abstract><AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Yu</LastName><ForeName>Ming-Jun</ForeName><Initials>MJ</Initials><AffiliationInfo><Affiliation>School of Food and Biological Engineering, Hefei University of Technology, Hefei 230009, China.</Affiliation></AffiliationInfo><AffiliationInfo><Affiliation>Traditional Chinese Medicine College, Bozhou University, Bozhou 236800, China.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Yao</LastName><ForeName>Sen</ForeName><Initials>S</Initials><AffiliationInfo><Affiliation>School of Food and Biological Engineering, Hefei University of Technology, Hefei 230009, China.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Li</LastName><ForeName>Ting-Ting</ForeName><Initials>TT</Initials><AffiliationInfo><Affiliation>School of Food and Biological Engineering, Hefei University of Technology, Hefei 230009, China.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Yang</LastName><ForeName>Rui</ForeName><Initials>R</Initials><AffiliationInfo><Affiliation>School of Food and Biological Engineering, Hefei University of Technology, Hefei 230009, China.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Yao</LastName><ForeName>Ri-Sheng</ForeName><Initials>RS</Initials><AffiliationInfo><Affiliation>School of Food and Biological Engineering, Hefei University of Technology, Hefei 230009, China.</Affiliation></AffiliationInfo><AffiliationInfo><Affiliation>Engineering Research Center of Bioprocess, Ministry of Education, PRC, Hefei University of Technology, Hefei 230009, China.</Affiliation></AffiliationInfo></Author></AuthorList><Language>eng</Language><PublicationTypeList><PublicationType UI="D016428">Journal Article</PublicationType><PublicationType UI="D013485">Research Support, Non-U.S. Gov't</PublicationType></PublicationTypeList></Article><MedlineJournalInfo><Country>Netherlands</Country><MedlineTA>Anticancer Agents Med Chem</MedlineTA><NlmUniqueID>101265649</NlmUniqueID><ISSNLinking>1871-5206</ISSNLinking></MedlineJournalInfo><ChemicalList><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="D000970">Antineoplastic Agents</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="D000982">Antipruritics</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="D007211">Indoles</NameOfSubstance></Chemical><Chemical><RegistryNumber>JT21Y57650</RegistryNumber><NameOfSubstance UI="C116774">PD 176252</NameOfSubstance></Chemical></ChemicalList><CitationSubset>IM</CitationSubset><MeshHeadingList><MeshHeading><DescriptorName UI="D000818" MajorTopicYN="N">Animals</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D000970" MajorTopicYN="N">Antineoplastic Agents</DescriptorName><QualifierName UI="Q000138" MajorTopicYN="N">chemical synthesis</QualifierName><QualifierName UI="Q000737" MajorTopicYN="N">chemistry</QualifierName><QualifierName UI="Q000494" MajorTopicYN="Y">pharmacology</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D000982" MajorTopicYN="N">Antipruritics</DescriptorName><QualifierName UI="Q000138" MajorTopicYN="N">chemical synthesis</QualifierName><QualifierName UI="Q000737" MajorTopicYN="N">chemistry</QualifierName><QualifierName UI="Q000494" MajorTopicYN="Y">pharmacology</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D049109" MajorTopicYN="N">Cell Proliferation</DescriptorName><QualifierName UI="Q000187" MajorTopicYN="N">drug effects</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D004305" MajorTopicYN="N">Dose-Response Relationship, Drug</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D015195" MajorTopicYN="Y">Drug Design</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D004354" MajorTopicYN="N">Drug Screening Assays, Antitumor</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D005260" MajorTopicYN="N">Female</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D006801" MajorTopicYN="N">Humans</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D007211" MajorTopicYN="N">Indoles</DescriptorName><QualifierName UI="Q000138" MajorTopicYN="N">chemical synthesis</QualifierName><QualifierName UI="Q000737" MajorTopicYN="N">chemistry</QualifierName><QualifierName UI="Q000494" MajorTopicYN="Y">pharmacology</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D008297" MajorTopicYN="N">Male</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D051379" MajorTopicYN="N">Mice</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D008815" MajorTopicYN="N">Mice, Inbred Strains</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D015394" MajorTopicYN="N">Molecular Structure</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D011537" MajorTopicYN="N">Pruritus</DescriptorName><QualifierName UI="Q000188" MajorTopicYN="Y">drug therapy</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D013329" MajorTopicYN="N">Structure-Activity Relationship</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D014407" MajorTopicYN="N">Tumor Cells, Cultured</DescriptorName></MeshHeading></MeshHeadingList><KeywordList Owner="NOTNLM"><Keyword MajorTopicYN="Y">Analogues</Keyword><Keyword MajorTopicYN="Y">GRPR</Keyword><Keyword MajorTopicYN="Y">MHCC97H cells</Keyword><Keyword MajorTopicYN="Y">NCI-H1299 cells</Keyword><Keyword MajorTopicYN="Y">PD176252</Keyword><Keyword MajorTopicYN="Y">anti-cancer</Keyword><Keyword MajorTopicYN="Y">anti-itch.</Keyword></KeywordList></MedlineCitation><PubmedData><History><PubMedPubDate PubStatus="received"><Year>2018</Year><Month>09</Month><Day>25</Day></PubMedPubDate><PubMedPubDate PubStatus="revised"><Year>2018</Year><Month>10</Month><Day>27</Day></PubMedPubDate><PubMedPubDate PubStatus="accepted"><Year>2019</Year><Month>03</Month><Day>25</Day></PubMedPubDate><PubMedPubDate PubStatus="pubmed"><Year>2019</Year><Month>4</Month><Day>10</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="medline"><Year>2020</Year><Month>3</Month><Day>25</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="entrez"><Year>2019</Year><Month>4</Month><Day>10</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate></History><PublicationStatus>ppublish</PublicationStatus><ArticleIdList><ArticleId IdType="pubmed">30961511</ArticleId><ArticleId IdType="pii">ACAMC-EPUB-97904</ArticleId><ArticleId IdType="doi">10.2174/1871520619666190408133141</ArticleId></ArticleIdList></PubmedData></pubmed></record>Pour manipuler ce document sous Unix (Dilib)
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