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View article: Effect of Indole-Containing Pyrazino[2,1-b]quinazoline-3,6-diones in the Virulence of Resistant Bacteria
Effect of Indole-Containing Pyrazino[2,1-b]quinazoline-3,6-diones in the Virulence of Resistant Bacteria Open
Drug resistance is rising to alarming levels, constituting one of the major threats to global health. The overexpression of efflux pumps and the formation of biofilms constitute two of the most common resistance mechanisms, favoring the vi…
View article: Fiscalin Derivatives as Potential Neuroprotective Agents
Fiscalin Derivatives as Potential Neuroprotective Agents Open
Neurodegenerative diseases (ND) share common molecular/cellular mechanisms that contribute to their progression and pathogenesis. In this sense, we are here proposing new neuroprotection strategies by using marine-derived compounds as fisc…
View article: Indole-Containing Pyrazino[2,1-<i>b</i>]quinazoline-3,6-diones Active against <i>Plasmodium</i> and Trypanosomatids
Indole-Containing Pyrazino[2,1-<i>b</i>]quinazoline-3,6-diones Active against <i>Plasmodium</i> and Trypanosomatids Open
Malaria, leishmaniasis, and sleeping sickness are potentially fatal diseases that represent a real health risk for more than 3,5 billion people. New antiparasitic compounds are urgent leading to a constant search for novel scaffolds. Herei…
View article: Determination of the Absolute Configuration of Bioactive Indole-Containing Pyrazino[2,1-b]quinazoline-3,6-diones and Study of Their In Vitro Metabolic Profile
Determination of the Absolute Configuration of Bioactive Indole-Containing Pyrazino[2,1-b]quinazoline-3,6-diones and Study of Their In Vitro Metabolic Profile Open
In recent decades, fungi-derived naturally occurring quinazolines have emerged as potential drug candidates. Nevertheless, most studies are conducted for bioactivity assays, and little is known about their absorption, distribution, metabol…
View article: Semi-Synthesis of Small Molecules of Aminocarbazoles: Tumor Growth Inhibition and Potential Impact on p53
Semi-Synthesis of Small Molecules of Aminocarbazoles: Tumor Growth Inhibition and Potential Impact on p53 Open
The tumor suppressor p53 is inactivated by mutation in approximately 50% of human cancers. Small molecules that bind and stabilize those mutants may represent effective anticancer drugs. Herein, we report the tumor cell growth inhibitory a…
View article: New marine-derived indolymethyl pyrazinoquinazoline alkaloids with promising antimicrobial profiles
New marine-derived indolymethyl pyrazinoquinazoline alkaloids with promising antimicrobial profiles Open
Indolomethyl pyrazino [1,2-b]quinazoline-3,6-diones were prepared using a one-pot multicomponent polycondensation of amino acids and were evaluated for their antimicrobial activity against a panel of nine bacterial strains and five fungal …
View article: Synthetic strategies towards bioactive nature-inspired indole-containing alkaloids
Synthetic strategies towards bioactive nature-inspired indole-containing alkaloids Open
Currently drug resistance is rising to dangerously high levels worldwide and threatening our ability to treat even common infectious diseases. Secondary metabolites, especially alkaloids containing an indole group and structurally related …
View article: Histological and toxicological evaluation, in rat, of a P-glycoprotein inducer and activator: 1-(propan-2-ylamino)-4-propoxy-9h-thioxanthen-9-one (TX5)
Histological and toxicological evaluation, in rat, of a P-glycoprotein inducer and activator: 1-(propan-2-ylamino)-4-propoxy-9h-thioxanthen-9-one (TX5) Open
P-glycoprotein (P-gp) is an ATP-binding cassette transporter involved in the efflux of numerous compounds that influences the pharmacokinetics of xenobiotics. It reduces intestinal absorption and exposure of target cells to toxicity. Thiox…
View article: Synthesis of New Proteomimetic Quinazolinone Alkaloids and Evaluation of Their Neuroprotective and Antitumor Effects
Synthesis of New Proteomimetic Quinazolinone Alkaloids and Evaluation of Their Neuroprotective and Antitumor Effects Open
New quinazolinone derivatives of the marine-derived alkaloids fiscalin B (3) and fumiquinazoline G (1), with neuroprotective and antitumor effects, were synthesized. Eleven quinazolinone-containing indole alkaloids were synthesized, procee…
View article: Small molecules from the sea: models for innovative antimicrobial agents
Small molecules from the sea: models for innovative antimicrobial agents Open
Antimicrobial resistance is one of the most pressing health issues of our days. The marine environment has proven to be a very rich source of diverse natural products with broad-spectra of biologically activities being a very helpful resou…
View article: Antitumor Activity of Quinazolinone Alkaloids Inspired by Marine Natural Products
Antitumor Activity of Quinazolinone Alkaloids Inspired by Marine Natural Products Open
Many fungal quinazolinone metabolites, which contain the methyl-indole pyrazino [1,2-b]quinazoline-3,6-dione core, have been found to possess promising antitumor activity. The purpose of this work was to synthesize the enantiomeric pairs o…
View article: Synthesis and tumor cell growth inhibitory effects of the marine product analogues of fiscalin B
Synthesis and tumor cell growth inhibitory effects of the marine product analogues of fiscalin B Open
Aim: The aim of this work was to synthesize fiscalin B, to pursuit the development of a library of derivatives and to investigate the derivatives for their potential antitumor activity. Introduction: Marine organisms provided numerous nove…
View article: Marine Natural Products as Models to Circumvent Multidrug Resistance
Marine Natural Products as Models to Circumvent Multidrug Resistance Open
Multidrug resistance (MDR) to anticancer drugs is a serious health problem that in many cases leads to cancer treatment failure. The ATP binding cassette (ABC) transporter P-glycoprotein (P-gp), which leads to premature efflux of drugs fro…