1,720,982 research outputs found
A new entry to the substituted Pyrrolo[3,2-c]quinoline derivatives of biological interest by intramolecular heteroannulation of internal imines
No full textTargeted synthesis of pyrrolo tricycles for selective biomolecules overexpressed in cancer cells
No full text1,2-Dihydropyrazole[1,2-a]benzo[1,2,4]triazine-3-one: deaza analogue tricyclic scaffold with valuable antiproliferative activity
No full text
The role of side chains in Substituted Pyrrole derivatives towards antiproliferative activity
No full textIn the last years, the introduction of side chains in different molecular compounds takes increasing importance. As recently reported in literature, heterocyclic scaffolds with poor biological activity , if properly decorated with selected side chains, can improve their anticancer activity against a large spectrum of human tumor cell lines. For example, the annelated Pyrrolo[3,4-e]Pyrimidines and Pyrrolo[3,2-e]Pyrimidines, opportunely functionalized with a large number of side chains, showed a good increase in the antitumor activity with respect to the starting core structure. New compound thus obtained showed antiproliferative activity against all the human tumor cells, generally in the low micromolar concentration range (1).
Furthermore, this increase in activity is confirmed in the new linear derivatives Thieno[3,2-d][1,2,3]Triazolo [1,5- α]Pyrimidines (2) and their angular isomer Thieno[2,3-e][1,2,3]Triazolo[1,5- α]Pyrimidines (3).
Another confirmation is provided by the Indolo [3,2-e][1,2,3]Triazolo [1,5- α]Pyrimidines, that resulted inactive as antitumor agent, but when a functionalization with side chains takes place, the anticancer activity
has interestingly appeared (4). Here, with the aim to explore the importance of the addition of side chains on smaller molecular scaffolds, of
easier synthetic access and decoration, we focused our attention on a new series of substituted “chained” pyrrole derivatives in order to evaluate their anticancer potential
In vitro and in silico studies of polycondensed diazine systems as anti-infective agents
No full textInfective diseases caused by protozoarian agents are still relevant today
more than ever. In fact, they represent the first cause of death all over the world
with seventeen millions victims every year. The development of drug resistance
and the broad diffusion of these pathologies make actual the research of new
molecules able to act as selective and effective anti-infective chemotherapics.[1]
Recently several polycondensed
diazine derivatives, by means 1,3-dipolar
cycloaddition, reactions [2, 3] were
synthesized.
A broad selection of these
compounds chosen with a wide pattern of
substitutions were submitted to biological
in vitro screening against Plasmodium
falciparum, Leishmania Infantum,
Trypanosoma brucei e Trypanosoma
cruzi, and they resulted active at
micromolar level. In order to identify
molecular targets able to explain the
mechanism of action of these compounds,
we performed Induced Fit Docking/MM-GBSA modeling studies. The obtained
results give interesting indications about the probable mechanism of action of the
most active compounds.
[1] M. Gonzaalez, H. Cerecetto, Expert Opinion on Therapeutic Patents, 21,
2011, 699-715.
[2] A. Lauria, A. Guarcello, G. Dattolo, A.M. Almerico, Tetrahedron Lett., 49,
2008, 1847-1850.
[3] A. Lauria, A. Guarcello, G. Macaluso, G. Dattolo, A.M. Almerico,
Tetrahedron Lett., 50, 2009, 7333-7336
Going Beyond Counting First Authors in Author Co-citation Analysis
Full text linkThe present study examines one of the fundamental aspects of author co-citation analysis (ACA) - the way co-citation
counts are defined. Co-citation counting provides the data on which all subsequent statistical analyses and mappings
are based, and we compare ACA results based on two different types of co-citation counting - the traditional type that
only counts the first one among a cited work's authors on the one hand and a non-traditional type that takes into
account the first 5 authors of a cited work on the other hand. Results indicate that the picture produced through this non-traditional author co-citation counting contains more coherent author groups and is therefore considerably clearer. However, this picture represents fewer specialties in the research field being studied than that produced through the traditional first-author co-citation counting when the same number of top-ranked authors is selected and analyzed. Reasons for these effects are discussed
Variations on the Author
Full text link“Variations on the Author” discusses two of Eduardo Coutinho’s recent films (Um Dia na Vida, from 2010, and Últimas Conversas, posthumously released in 2015) and their contribution to the general question of documentary authorship. The director’s filmography is characterized by a consistent yet self-effacing form of authorial self-inscription: Coutinho often features as an interviewer that rather than express opinions propels discourses; an interviewer that is good at listening. This mode of self-inscription characterizes him as an author who is not expressive but who is nonetheless markedly present on the screen. In Um Dia na Vida, however, Coutinho is completely absent form the image, while Últimas Conversas, on the contrary, includes a confessional prologue that moves the director from the margins to the center of his films. This article examines the ways in which these works stand out in the filmography of a director who offers new insights into the notion of cinematic authorship
Appropriate Similarity Measures for Author Cocitation Analysis
Full text linkWe provide a number of new insights into the methodological discussion about author cocitation analysis. We first argue that the use of the Pearson correlation for measuring the similarity between authors’ cocitation profiles is not very satisfactory. We then discuss what kind of similarity measures may be used as an alternative to the Pearson correlation. We consider three similarity measures in particular. One is the well-known cosine. The other two similarity measures have not been used before in the bibliometric literature. Finally, we show by means of an example that our findings have a high practical relevance.information science;Pearson correlation;cosine;similarity measure;author cocitation analysis
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