Search results for "Nortopsentin Analogue"

showing 8 items of 18 documents

Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin

2013

2,5-bis(3′-Indolyl)pyrroles, analogues of the marine alkaloid nortopsentin, were conveniently prepared through a three step procedure in good overall yields. Derivatives 1a and 1b exhibited concentration-dependent antitumor activity towards a panel of 42 human tumor cell lines with mean IC50 values of 1.54 μM and 0.67 μM, respectively. Investigating human tumor xenografts in an ex-vivo clonogenic assay revealed selective antitumor activity, whereas sensitive tumor models were scattered among various tumor histotypes.

ex-vivo xenograftsIndolesStereochemistryPharmaceutical ScienceMice NudeAntineoplastic AgentsArticleInhibitory Concentration 50MiceCell Line TumorNeoplasmsDrug Discoverybis-indolyl-pyrroles; nortopsentin analogues; marine alkaloids; antitumor; <i>ex-vivo </i>xenograftsIc50 valuesAnimalsHumansnortopsentin analoguePyrrolesClonogenic assayPharmacology Toxicology and Pharmaceutics (miscellaneous)lcsh:QH301-705.5Tumor Stem Cell AssayMice nudeantitumorAntitumor activityDose-Response Relationship DrugChemistryAlkaloidbis-indolyl-pyrroles; nortopsentin analogues; marine alkaloids; antitumor; ex-vivo xenograftsImidazolesTumor Stem Cell AssaySettore CHIM/08 - Chimica FarmaceuticaXenograft Model Antitumor Assaysbis-indolyl-pyrrolemarine alkaloidHuman tumornortopsentin analogueslcsh:Biology (General)Cell culturebis-indolyl-pyrrolesmarine alkaloidsMarine Drugs
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NOVEL NORTOPSENTIN ANALOGUES: PYRROLO[2,3-b]PYRIDINE,bis(PYRROLO[2,3-b]PYRIDINE AND 7 -CHLORO-PYRROLO[2,3-c]PYRIDINE ANALOGUES

2014

nortopsentin analogues
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SYNTHESIS OF PYRROLO[2,3-b]PYRIDINE, BIS(PYRROLO[2,3-b]PYRIDINE) and 7-CHLORO-PYRROLO[2,3-c]PYRIDINE, ANALOGUES OF MARINE BIS(INDOLE)ALKALOID NORTOPS…

2014

nortopsentin analogues
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Synthesis and biological activity of a new series of nortopsentin analogues

2015

nortopsentin analogues
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Synthesis of Nortopsentin analogues

2014

nortopsentin analogues
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Synthesis and antitumor activity of new 7-azaindole derivative nortopsentin analogues

2016

nortopsentin analoguesSettore CHIM/08 - Chimica Farmaceutica
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Structural Manipulations of Marine Natural Products Inspire a New Library of 3-Amino-1,2,4-Triazine PDK Inhibitors Endowed with Antitumor Activity in…

2023

Pancreatic ductal adenocarcinoma (PDAC) is one of the main aggressive types of cancer, characterized by late prognosis and drug resistance. Among the main factors sustaining PDAC progression, the alteration of cell metabolism has emerged to have a key role in PDAC cell proliferation, invasion, and resistance to standard chemotherapeutic agents. Taking into account all these factors and the urgency in evaluating novel options to treat PDAC, in the present work we reported the synthesis of a new series of indolyl-7-azaindolyl triazine compounds inspired by marine bis-indolyl alkaloids. We first assessed the ability of the new triazine compounds to inhibit the enzymatic activity of pyruvate de…

nortopsentin analoguespancreatic ductal adenocarcinoma (PDAC); nortopsentin analogues; antitumor activity; pyruvate dehydrogenase kinases (PDKs); cytotoxic activity; metabolic alterations; ligand-based homology modeling; KRASDrug Discoveryligand-based homology modelingKRASPharmaceutical Scienceantitumor activitymetabolic alterationspancreatic ductal adenocarcinoma (PDAC)Pharmacology Toxicology and Pharmaceutics (miscellaneous)cytotoxic activitypyruvate dehydrogenase kinases (PDKs)
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Synthesis and anticancer activity of new thiazole nortopsentin analogues

2015

thiazole nortopsentin analoguesSettore CHIM/08 - Chimica Farmaceutica
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