Search results for "topsentin"
showing 10 items of 41 documents
New Topsentin analogs as inhibitors of biofilm formation
Synthesis and antiproliferative activity of thiazolyl-bis-pyrrolo[2,3- b]pyridines, indolyl-thiazolyl-pyrrolo[2,3-b]pyridines and indolylthiazolyl- p…
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.
NOVEL NORTOPSENTIN ANALOGUES: PYRROLO[2,3-b]PYRIDINE,bis(PYRROLO[2,3-b]PYRIDINE AND 7 -CHLORO-PYRROLO[2,3-c]PYRIDINE ANALOGUES
2014
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
Synthesis and biological activity of a new series of nortopsentin analogues
2015
Synthesis of Nortopsentin analogues
2014
Synthesis and antitumor activity of new 7-azaindole derivative nortopsentin analogues
2016
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…
Thiazole Analogues of the Marine Alkaloid Nortopsentin as Inhibitors of Bacterial Biofilm Formation
2020
Anti-virulence strategy is currently considered a promising approach to overcome the global threat of the antibiotic resistance. Among different bacterial virulence factors, the biofilm formation is recognized as one of the most relevant. Considering the high and growing percentage of multi-drug resistant infections that are biofilm-mediated, new therapeutic agents capable of counteracting the formation of biofilms are urgently required. In this scenario, a new series of 18 thiazole derivatives was efficiently synthesized and evaluated for its ability to inhibit biofilm formation against the Gram-positive bacterial reference strains Staphylococcus aureus ATCC 25923 and S. aureus ATCC 6538 a…