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Indole: A privileged scaffold for the design of anti-cancer agents.

Identifieur interne : 000885 ( PubMed/Checkpoint ); précédent : 000884; suivant : 000886

Indole: A privileged scaffold for the design of anti-cancer agents.

Auteurs : Yichao Wan [République populaire de Chine] ; Yuanhua Li [République populaire de Chine] ; Chunxing Yan [République populaire de Chine] ; Mi Yan [République populaire de Chine] ; Zilong Tang [République populaire de Chine]

Source :

RBID : pubmed:31536895

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English descriptors

Abstract

In general, heterocyclic compounds are a significant source of pharmacologically active compounds. Among them, the indole scaffold widely distributes in natural products and bioactive molecules including anti-cancer agents. In view of its unique physic-chemical and biological properties, it has been used as a privileged scaffold in the anti-cancer agents design. So far, many natural and synthetic indole derivatives have been discovered as promising anti-cancer agents used in clinic or clinical evaluations, suggesting its prominent place in anti-cancer drugs development. This review aimed to provide a clear knowledge on the recent development of indoles as anti-cancer agents, such as myeloid cell leukemia-1 (Mcl-1) inhibitors, proviral insertion site in moloney murine leukemia virus (Pim) inhibitors, histone deacetylase (HDAC) inhibitors, silent mating type information regulation 2 homolog (SIRT) inhibitors and tubulin inhibitors, and made an insight into the corresponding structure-activity relationships (SARs). We hope the review could give a guide to develop new anti-cancer agents with greater potency against drug-sensitive and drug-resistant cancers in the future.

DOI: 10.1016/j.ejmech.2019.111691
PubMed: 31536895


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pubmed:31536895

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<div type="abstract" xml:lang="en">In general, heterocyclic compounds are a significant source of pharmacologically active compounds. Among them, the indole scaffold widely distributes in natural products and bioactive molecules including anti-cancer agents. In view of its unique physic-chemical and biological properties, it has been used as a privileged scaffold in the anti-cancer agents design. So far, many natural and synthetic indole derivatives have been discovered as promising anti-cancer agents used in clinic or clinical evaluations, suggesting its prominent place in anti-cancer drugs development. This review aimed to provide a clear knowledge on the recent development of indoles as anti-cancer agents, such as myeloid cell leukemia-1 (Mcl-1) inhibitors, proviral insertion site in moloney murine leukemia virus (Pim) inhibitors, histone deacetylase (HDAC) inhibitors, silent mating type information regulation 2 homolog (SIRT) inhibitors and tubulin inhibitors, and made an insight into the corresponding structure-activity relationships (SARs). We hope the review could give a guide to develop new anti-cancer agents with greater potency against drug-sensitive and drug-resistant cancers in the future.</div>
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<Chemical>
<RegistryNumber>8724FJW4M5</RegistryNumber>
<NameOfSubstance UI="C030374">indole</NameOfSubstance>
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<Chemical>
<RegistryNumber>EC 2.7.11.1</RegistryNumber>
<NameOfSubstance UI="D051573">Proto-Oncogene Proteins c-pim-1</NameOfSubstance>
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<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>
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<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>
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<DescriptorName UI="D064549" MajorTopicYN="N">Myeloid Cell Leukemia Sequence 1 Protein</DescriptorName>
<QualifierName UI="Q000037" MajorTopicYN="N">antagonists & inhibitors</QualifierName>
<QualifierName UI="Q000378" MajorTopicYN="N">metabolism</QualifierName>
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<DescriptorName UI="D009369" MajorTopicYN="N">Neoplasms</DescriptorName>
<QualifierName UI="Q000188" MajorTopicYN="Y">drug therapy</QualifierName>
<QualifierName UI="Q000378" MajorTopicYN="N">metabolism</QualifierName>
</MeshHeading>
<MeshHeading>
<DescriptorName UI="D051573" MajorTopicYN="N">Proto-Oncogene Proteins c-pim-1</DescriptorName>
<QualifierName UI="Q000037" MajorTopicYN="N">antagonists & inhibitors</QualifierName>
<QualifierName UI="Q000378" MajorTopicYN="N">metabolism</QualifierName>
</MeshHeading>
<MeshHeading>
<DescriptorName UI="D014404" MajorTopicYN="N">Tubulin</DescriptorName>
<QualifierName UI="Q000378" MajorTopicYN="N">metabolism</QualifierName>
</MeshHeading>
</MeshHeadingList>
<KeywordList Owner="NOTNLM">
<Keyword MajorTopicYN="N">Anti-Cancer</Keyword>
<Keyword MajorTopicYN="N">Drug design</Keyword>
<Keyword MajorTopicYN="N">Indole</Keyword>
<Keyword MajorTopicYN="N">Structure-activity relationships</Keyword>
</KeywordList>
</MedlineCitation>
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<Year>2019</Year>
<Month>07</Month>
<Day>16</Day>
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<PubMedPubDate PubStatus="revised">
<Year>2019</Year>
<Month>09</Month>
<Day>05</Day>
</PubMedPubDate>
<PubMedPubDate PubStatus="accepted">
<Year>2019</Year>
<Month>09</Month>
<Day>07</Day>
</PubMedPubDate>
<PubMedPubDate PubStatus="pubmed">
<Year>2019</Year>
<Month>9</Month>
<Day>20</Day>
<Hour>6</Hour>
<Minute>0</Minute>
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<PubMedPubDate PubStatus="medline">
<Year>2019</Year>
<Month>12</Month>
<Day>18</Day>
<Hour>6</Hour>
<Minute>0</Minute>
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<PubMedPubDate PubStatus="entrez">
<Year>2019</Year>
<Month>9</Month>
<Day>20</Day>
<Hour>6</Hour>
<Minute>0</Minute>
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</History>
<PublicationStatus>ppublish</PublicationStatus>
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<ArticleId IdType="pubmed">31536895</ArticleId>
<ArticleId IdType="pii">S0223-5234(19)30841-4</ArticleId>
<ArticleId IdType="doi">10.1016/j.ejmech.2019.111691</ArticleId>
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<list>
<country>
<li>République populaire de Chine</li>
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<noRegion>
<name sortKey="Wan, Yichao" sort="Wan, Yichao" uniqKey="Wan Y" first="Yichao" last="Wan">Yichao Wan</name>
</noRegion>
<name sortKey="Li, Yuanhua" sort="Li, Yuanhua" uniqKey="Li Y" first="Yuanhua" last="Li">Yuanhua Li</name>
<name sortKey="Tang, Zilong" sort="Tang, Zilong" uniqKey="Tang Z" first="Zilong" last="Tang">Zilong Tang</name>
<name sortKey="Yan, Chunxing" sort="Yan, Chunxing" uniqKey="Yan C" first="Chunxing" last="Yan">Chunxing Yan</name>
<name sortKey="Yan, Mi" sort="Yan, Mi" uniqKey="Yan M" first="Mi" last="Yan">Mi Yan</name>
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