Elena Gabriele
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View article: A Substance-Based Medical Device for Managing Hemorrhoidal Disease: Output from a Cross-Sectional Survey
A Substance-Based Medical Device for Managing Hemorrhoidal Disease: Output from a Cross-Sectional Survey Open
Background: Hemorrhoidal disease (HD) is a common anorectal condition characterized by symptoms such as bleeding, pain, discomfort and itching. While often underdiagnosed due to patient reluctance to seek care, HD significantly impacts qua…
View article: Design, Synthesis and In Vitro Investigation of Novel Basic Celastrol Carboxamides as Bio-Inspired Leishmanicidal Agents Endowed with Inhibitory Activity against Leishmania Hsp90
Design, Synthesis and In Vitro Investigation of Novel Basic Celastrol Carboxamides as Bio-Inspired Leishmanicidal Agents Endowed with Inhibitory Activity against Leishmania Hsp90 Open
The natural triterpene celastrol (CE) is here used as lead compound for the design and synthesis of a panel of eleven CE carboxamides that were tested in vitro for their growth inhibitory activity against Leishmania infantum and L.tropica …
View article: Benzimidazole derivatives endowed with potent antileishmanial activity
Benzimidazole derivatives endowed with potent antileishmanial activity Open
Two sets of benzimidazole derivatives were synthesised and tested in vitro for activity against promastigotes of Leishmania tropica and L. infantum. Most of the tested compounds resulted active against both Leishmania species, with IC…
View article: SYNTHESIS OF NEW SULFURATED DERIVATIVES OF NATURAL AND SYNTHETIC SYSTEMS AS MULTITARGET ANTICANCER AGENTS AND DEVELOPMENT OF NEW DRUG DISCOVERY METHODOLOGIES
SYNTHESIS OF NEW SULFURATED DERIVATIVES OF NATURAL AND SYNTHETIC SYSTEMS AS MULTITARGET ANTICANCER AGENTS AND DEVELOPMENT OF NEW DRUG DISCOVERY METHODOLOGIES Open
This PhD thesis is divided in two parts. The former, entitled "Design and synthesis of new derivatives of natural and synthetic systems endowed with anticancer activity, through a multitarget mechanism", has been carried out at the Univers…
View article: CCDC 1495448: Experimental Crystal Structure Determination
CCDC 1495448: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: New sulfurated derivatives of cinnamic acids and rosmaricine as inhibitors of STAT3 and NF-κB transcription factors
New sulfurated derivatives of cinnamic acids and rosmaricine as inhibitors of STAT3 and NF-κB transcription factors Open
A set of new sulfurated drug hybrids, mainly derived from caffeic and ferulic acids and rosmaricine, has been synthesized and their ability to inhibit both STAT3 and NF-κB transcription factors have been evaluated. Results showed that most…
View article: Methanethiosulfonate derivatives as ligands of the STAT3-SH2 domain
Methanethiosulfonate derivatives as ligands of the STAT3-SH2 domain Open
With the aim to discover new STAT3 direct inhibitors, potentially useful as anticancer agents, a set of methanethiosulfonate drug hybrids were synthesized. The in vitro tests showed that all the thiosulfonic compounds were able to strongly…
View article: Synthesis of new dithiolethione and methanethiosulfonate systems endowed with pharmaceutical interest
Synthesis of new dithiolethione and methanethiosulfonate systems endowed with pharmaceutical interest Open
Here we report synthetic methodology affording in the most efficient way the rapid preparation of new dithiolethiones (DTTs) and methanethiosulfonates (MTSs). These were evaluated as STAT3 inhibitors since these electrophilic systems could…