ARTICLE | doi:10.20944/preprints201807.0515.v1
Subject: Chemistry, Organic Chemistry Keywords: EMICORON; organic synthesis; synthesis improvements; G-quadruplex structures; anticancer activity
Online: 26 July 2018 (14:25:19 CEST)
In this paper, the modification of two synthetic steps to obtain EMICORON, with respect to the usual protocol, is reported. EMICORON is a benzo[ghi]perylen-diimmide which was synthesized the first time in our laboratory in 2012 and showed to have in-vivo antitumor activities interfering with tumor growth and development by a multi-target mechanism of action. The provided modifications regarded the reaction times and the reaction conditions as well as the work-up procedures and allowed to increase the global yield of the process from 28% to about 40%. Thus, this new procedure may be more suitable in order to get larger amounts of EMICORON for further preclinical studies.
REVIEW | doi:10.20944/preprints202209.0305.v1
Subject: Chemistry, Organic Chemistry Keywords: Leucosceptoside A; Leucosceptoside B; occurrence in plants; biological activities
Online: 20 September 2022 (10:34:18 CEST)
In this review paper, the occurrence in the plant kingdom and the biological activities associated to two specific phenyl-ethanoid glycosides i.e., leucosceptoside A and leucosceptoside B, were shown and discussed. This is the first work ever done on such subject. Analysis of the literature data clearly indicates that leucosceptoside A is much more common in plants and exerts many more biological activities than leucosceptoside B even if this also presents some important elements. All of this was widely discussed in this paper.
ARTICLE | doi:10.20944/preprints201805.0189.v1
Subject: Chemistry, Medicinal Chemistry Keywords: G-quadruplex DNA; interactions; berberine and palmatine analogues; chemotherapy; NMR; FRET and MST assays
Online: 14 May 2018 (11:44:10 CEST)
In this article/review, the selective interactions of several berberine and palmatine derivatives with various DNA G-quadruplex structures are reported. These derivatives were constructed starting from two natural compounds, berberine and palamatine, through specific synthetic passages following two different schemes for each of them and using several substituents. The details of these synthesis are also described. Indeed, the study of the interactions of these derivative compounds with various G-quadruplex forming sequences was carried out by means of various structural and biochemical techniques. The results show that the presence of suitable side chains are very useful to improve the interaction of the ligands with G-quadruplex structures. Thus, since G-quadruplex formation is promoted by these compounds, which have never been reported before, these may be tested as potential anticancer drugs.
REVIEW | doi:10.20944/preprints201911.0367.v1
Online: 29 November 2019 (03:27:12 CET)
In this review article, the occurrence of nor-lignans and their biological activities are explored and described. Nor-lignans have proven to be present in several different families also belonging to chemosystematically distant orders as well as to have many different beneficial pharmacological activities. This review article represents the first one on this argument and is thought to give a first overview on these compounds with the hope that their study may continue if not raise after this.
REVIEW | doi:10.20944/preprints201906.0304.v1
Subject: Chemistry, Other Keywords: Pedicularis L. genus; Orobanchaceae family; Phytochemistry; Chemotaxonomy; Ethnopharmacology
Online: 29 June 2019 (10:34:48 CEST)
In this review, the relevance of plants belonging to the Pedicularis L. genus was explored from different points of view. Particular emphasys was given especially to the phytochemistry and the ethnopharmacology of the genus since several classes of natural compounds have been evidenced within it and several Pedicularis species are well known to be employed in the traditional medicine of many Asian countries. Nevertheless, some important conclusions on the chemotaxonomic and chemosystematic aspects of the genus were also provided for the first time. This work represents the first total comprehensive review on the genus Pedicularis.