Indole: A privileged scaffold for the design of anti-cancer agents.
Identifieur interne : 003086 ( Ncbi/Curation ); précédent : 003085; suivant : 003087Indole: 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 :
- European journal of medicinal chemistry [ 1768-3254 ] ; 2019.
Descripteurs français
- KwdFr :
- Antinéoplasiques (), Antinéoplasiques (pharmacologie), Antinéoplasiques (synthèse chimique), Conception de médicament, Humains, Indoles (), Indoles (pharmacologie), Indoles (synthèse chimique), Protéine Mcl-1 (antagonistes et inhibiteurs), Protéine Mcl-1 (métabolisme), Protéines proto-oncogènes c-pim-1 (antagonistes et inhibiteurs), Protéines proto-oncogènes c-pim-1 (métabolisme), Tests de criblage d'agents antitumoraux, Tubuline (métabolisme), Tumeurs (métabolisme), Tumeurs (traitement médicamenteux).
- MESH :
- antagonistes et inhibiteurs : Protéine Mcl-1, Protéines proto-oncogènes c-pim-1.
- métabolisme : Protéine Mcl-1, Protéines proto-oncogènes c-pim-1, Tubuline, Tumeurs.
- pharmacologie : Antinéoplasiques, Indoles.
- synthèse chimique : Antinéoplasiques, Indoles.
- traitement médicamenteux : Tumeurs.
- Antinéoplasiques, Conception de médicament, Humains, Indoles, Tests de criblage d'agents antitumoraux.
English descriptors
- KwdEn :
- Antineoplastic Agents (chemical synthesis), Antineoplastic Agents (chemistry), Antineoplastic Agents (pharmacology), Drug Design, Drug Screening Assays, Antitumor, Humans, Indoles (chemical synthesis), Indoles (chemistry), Indoles (pharmacology), Myeloid Cell Leukemia Sequence 1 Protein (antagonists & inhibitors), Myeloid Cell Leukemia Sequence 1 Protein (metabolism), Neoplasms (drug therapy), Neoplasms (metabolism), Proto-Oncogene Proteins c-pim-1 (antagonists & inhibitors), Proto-Oncogene Proteins c-pim-1 (metabolism), Tubulin (metabolism).
- MESH :
- chemical , antagonists & inhibitors : Myeloid Cell Leukemia Sequence 1 Protein, Proto-Oncogene Proteins c-pim-1.
- chemical , chemical synthesis : Antineoplastic Agents, Indoles.
- chemical , chemistry : Antineoplastic Agents, Indoles.
- chemical , metabolism : Myeloid Cell Leukemia Sequence 1 Protein, Proto-Oncogene Proteins c-pim-1, Tubulin.
- chemical , pharmacology : Antineoplastic Agents, Indoles.
- drug therapy : Neoplasms.
- metabolism : Neoplasms.
- Drug Design, Drug Screening Assays, Antitumor, Humans.
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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<profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Antineoplastic Agents (chemical synthesis)</term>
<term>Antineoplastic Agents (chemistry)</term>
<term>Antineoplastic Agents (pharmacology)</term>
<term>Drug Design</term>
<term>Drug Screening Assays, Antitumor</term>
<term>Humans</term>
<term>Indoles (chemical synthesis)</term>
<term>Indoles (chemistry)</term>
<term>Indoles (pharmacology)</term>
<term>Myeloid Cell Leukemia Sequence 1 Protein (antagonists & inhibitors)</term>
<term>Myeloid Cell Leukemia Sequence 1 Protein (metabolism)</term>
<term>Neoplasms (drug therapy)</term>
<term>Neoplasms (metabolism)</term>
<term>Proto-Oncogene Proteins c-pim-1 (antagonists & inhibitors)</term>
<term>Proto-Oncogene Proteins c-pim-1 (metabolism)</term>
<term>Tubulin (metabolism)</term>
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<keywords scheme="KwdFr" xml:lang="fr"><term>Antinéoplasiques ()</term>
<term>Antinéoplasiques (pharmacologie)</term>
<term>Antinéoplasiques (synthèse chimique)</term>
<term>Conception de médicament</term>
<term>Humains</term>
<term>Indoles ()</term>
<term>Indoles (pharmacologie)</term>
<term>Indoles (synthèse chimique)</term>
<term>Protéine Mcl-1 (antagonistes et inhibiteurs)</term>
<term>Protéine Mcl-1 (métabolisme)</term>
<term>Protéines proto-oncogènes c-pim-1 (antagonistes et inhibiteurs)</term>
<term>Protéines proto-oncogènes c-pim-1 (métabolisme)</term>
<term>Tests de criblage d'agents antitumoraux</term>
<term>Tubuline (métabolisme)</term>
<term>Tumeurs (métabolisme)</term>
<term>Tumeurs (traitement médicamenteux)</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="antagonists & inhibitors" xml:lang="en"><term>Myeloid Cell Leukemia Sequence 1 Protein</term>
<term>Proto-Oncogene Proteins c-pim-1</term>
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<term>Indoles</term>
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<term>Indoles</term>
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<keywords scheme="MESH" type="chemical" qualifier="metabolism" xml:lang="en"><term>Myeloid Cell Leukemia Sequence 1 Protein</term>
<term>Proto-Oncogene Proteins c-pim-1</term>
<term>Tubulin</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Antineoplastic Agents</term>
<term>Indoles</term>
</keywords>
<keywords scheme="MESH" qualifier="antagonistes et inhibiteurs" xml:lang="fr"><term>Protéine Mcl-1</term>
<term>Protéines proto-oncogènes c-pim-1</term>
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<term>Protéines proto-oncogènes c-pim-1</term>
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<term>Tumeurs</term>
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<term>Indoles</term>
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<front><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>
</front>
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