Search results for "bis-indole"

showing 3 items of 3 documents

A Facile Synthesis of Deaza-Analogues of the Bisindole Marine Alkaloid Topsentin

2013

A series of substituted ethyl 1-[(tert-butoxycarbonyl)amino]-2-methyl-5- (1-methyl-1H-indol-3-yl)-4-[(1-methyl-1H-indol-3-yl)carbonyl]-1H-pyrrole-3-carboxylates were prepared in excellent yields (82-98%) by one-pot reactions between β-dicarbonyl compounds 12a-e and 1,2-diaza-1,3-diene (DD) 13. Derivatives 10a,c-e, deazaanalogues of the bis-indole alkaloid topsentin, screened by the National Cancer Institute (Bethesda, MD, USA) in the in vitro one dose primary anticancer assay against a panel of about 60 human tumor cell lines, showed no significant activity, with the exception of compound 9e, which showed moderate activity against the HOP-92 cell line of the non small cell lung cancer sub-p…

IndolesStereochemistryPharmaceutical ScienceAntineoplastic AgentsModerate activityArticleAnalytical Chemistrylcsh:QD241-441Alkaloidslcsh:Organic chemistrytopsentin; bis-indole alkaloids; antitumor activity; ethyl 1-[(<i>tert</i>-butoxycarbonyl)amino]-2-methyl-5-(1-methyl-1<i>H</i>-indol-3-yl)-4-[(1-methyl-1<i>H</i>-indol-3-yl)-carbonyl]-1<i>H</i>-pyrrole-3-carboxylatesCell Line Tumortopsentin; bis-indole alkaloids; antitumor activity; ethyl 1-[(tertbutoxycarbonyl) amino]-2-methyl-5-(1-methyl-1H-indol-3-yl)-4-[(1-methyl-1H-indol-3-yl)- carbonyl]-1H-pyrrole-3-carboxylatesDrug DiscoverymedicineHumansantitumor activityethyl 1-[(tert-butoxycarbonyl)amino]-2-methyl-5-(1-methyl-1H-indol-3-yl)-4-[(1-methyl-1H-indol-3-yl)-carbonyl]-1H-pyrrole-3-carboxylatesPhysical and Theoretical ChemistryAntitumor activityethyl 1-[(tertbutoxycarbonyl) amino]-2-methyl-5-(1-methyl-1H-indol-3-yl)-4-[(1-methyl-1H-indol-3-yl)- carbonyl]-1H-pyrrole-3-carboxylatesChemistryAlkaloidOrganic ChemistryImidazolesCancermedicine.diseaseSettore CHIM/08 - Chimica FarmaceuticaIn vitroHuman tumorbis-indole alkaloidsChemistry (miscellaneous)Cell culturebis-indole alkaloidMolecular MedicineNon small cellDrug Screening Assays AntitumortopsentinMolecules; Volume 18; Issue 3; Pages: 2518-2527
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Discovery of the 3-Amino-1,2,4-triazine-Based Library as Selective PDK1 Inhibitors with Therapeutic Potential in Highly Aggressive Pancreatic Ductal …

2023

Pyruvate dehydrogenase kinases (PDKs) are serine/threonine kinases, that are directly involved in altered cancer cell metabolism, resulting in cancer aggressiveness and resistance. Dichloroacetic acid (DCA) is the first PDK inhibitor that has entered phase II clinical; however, several side effects associated with weak anticancer activity and excessive drug dose (100 mg/kg) have led to its limitation in clinical application. Building upon a molecular hybridization approach, a small library of 3-amino-1,2,4-triazine derivatives has been designed, synthesized, and characterized for their PDK inhibitory activity using in silico, in vitro, and in vivo assays. Biochemical screenings showed that …

PDK inhibitorsOrganic ChemistryKras-mutated pancreatic ductal adenocarcinomaGeneral Medicine3-amino-124-triazine derivativesantitumor agentsCatalysisbis-indole derivativesComputer Science ApplicationsInorganic Chemistryligand-based homology modelingPhysical and Theoretical ChemistryMolecular BiologySpectroscopyInternational Journal of Molecular Sciences
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New indole and 7-azaindole derivatives as protein kinase inhibitors

2023

protein kinase inhibitorantiproliferativebis-indoleindole derivative7-azaindole derivativeanticancerSettore CHIM/08 - Chimica Farmaceutica
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