ArticleMarine drugs2015
3-[4-(1H-indol-3-yl)-1,3-thiazol-2-yl]-1H-pyrrolo[2,3-b]pyridines, nortopsentin analogues with antiproliferative activity.
Article in Marine drugs, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed.
- Anti colorectal cancer activity and in silico studies of novel pyridine nortopsentin analog as cyclin dependent kinase 6 inhibitor.Scientific reports · 2024Article
- Marine-Derived Bisindoles for Potent Selective Cancer Drug Discovery and Development.Molecules (Basel, Switzerland) · 2024Review
- 4-(Indol-3-yl)thiazole-2-amines and 4-ιndol-3-yl)thiazole Acylamines as Νovel Antimicrobial Agents: Synthesis, In Silico and In Vitro Evaluation.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Retracted Article: The synthesis and biological activity of marine alkaloid derivatives and analogues.RSC advances · 2020Article
- 3-(6-Phenylimidazo [2,1-Molecules (Basel, Switzerland) · 2020Article
- New 1,2,4-Oxadiazole Nortopsentin Derivatives with Cytotoxic Activity.Marine drugs · 2019Article
- New Thiazole Nortopsentin Analogues Inhibit Bacterial Biofilm Formation.Marine drugs · 2018Article
- New Tripentone Analogs with Antiproliferative Activity.Molecules (Basel, Switzerland) · 2017Article
- Cytotoxic Indole Alkaloid 3α-Acetonyltabersonine Induces Glioblastoma Apoptosis via Inhibition of DNA Damage Repair.Toxins · 2017Article
- Synthesis and Antitumor Activity of New Thiazole Nortopsentin Analogs.Marine drugs · 2016Article
- New 3-Cyano-2-Substituted Pyridines Induce Apoptosis in MCF 7 Breast Cancer Cells.Molecules (Basel, Switzerland) · 2016Article
- Crystal structure of 2-[2-phenyl-1-(phenyl-sulfon-yl)eth-yl]-1-phenyl-sulfonyl-1H-indole.Acta crystallographica. Section E, Crystallographic communications · 2015Article
- Antitumor Effects and Related Mechanisms of Penicitrinine A, a Novel Alkaloid with a Unique Spiro Skeleton from the Marine Fungus Penicillium citrinum.Marine drugs · 2015Article
- Crystal structure of methyl (2Z)-3-(4-chloro-phen-yl)-2-[(3-methyl-1H-indol-1-yl)meth-yl]prop-2-enoate.Acta crystallographica. Section E, Crystallographic communications · 2015Article
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Authors and funding
12 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A new series of nortopsentin analogues, in which the imidazole ring of the natural product was replaced by thiazole and the indole unit bound to position 2 of the thiazole ring was substituted by a 7-azaindole moiety, was efficiently synthesized. Two of the new nortopsentin analogues showed good antiproliferative effect against the totality of the NCI full panel of human tumor cell lines (~60) having GI50 values ranging from low micromolar to nanomolar level. The mechanism of the antiproliferative effect of these derivatives, investigated on human hepatoma HepG2 cells, was pro-apoptotic, being associated with externalization of plasma membrane phosphatidylserine and mitochondrial dysfunction. Moreover, the compounds induced a concentration-dependent accumulation of cells in the subG0/G1phase, while confined viable cells in G2/M phase.
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