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  1. Article ; Online: Recent Developments in the Inhibition of Bacterial Adhesion as Promising Anti-Virulence Strategy

    Camilla Pecoraro / Daniela Carbone / Barbara Parrino / Stella Cascioferro / Patrizia Diana

    International Journal of Molecular Sciences, Vol 24, Iss 4872, p

    2023  Volume 4872

    Abstract: Infectious diseases caused by antimicrobial-resistant strains have become a serious threat to global health, with a high social and economic impact. Multi-resistant bacteria exhibit various mechanisms at both the cellular and microbial community levels. ... ...

    Abstract Infectious diseases caused by antimicrobial-resistant strains have become a serious threat to global health, with a high social and economic impact. Multi-resistant bacteria exhibit various mechanisms at both the cellular and microbial community levels. Among the different strategies proposed to fight antibiotic resistance, we reckon that the inhibition of bacterial adhesion to host surfaces represents one of the most valid approaches, since it hampers bacterial virulence without affecting cell viability. Many different structures and biomolecules involved in the adhesion of Gram-positive and Gram-negative pathogens can be considered valuable targets for the development of promising tools to enrich our arsenal against pathogens.
    Keywords antibiotic resistance ; anti-virulence agents ; bacterial adhesion ; biofilm formation ; Biology (General) ; QH301-705.5 ; Chemistry ; QD1-999
    Language English
    Publishing date 2023-03-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  2. Article ; Online: Nortopsentins as Leads from Marine Organisms for Anticancer and Anti-Inflammatory Agent Development

    Camilla Pecoraro / Francesca Terrana / Giovanna Panzeca / Barbara Parrino / Stella Cascioferro / Patrizia Diana / Elisa Giovannetti / Daniela Carbone

    Molecules, Vol 28, Iss 6450, p

    2023  Volume 6450

    Abstract: The marine environment is an excellent source of molecules that have a wide structural diversity and a variety of biological activities. Many marine natural products (MNPs) have been established as leads for anticancer drug discovery. Most of these ... ...

    Abstract The marine environment is an excellent source of molecules that have a wide structural diversity and a variety of biological activities. Many marine natural products (MNPs) have been established as leads for anticancer drug discovery. Most of these compounds are alkaloids, including several chemical subclasses. In this review, we focus on the bis-indolyl alkaloid Nortopsentins and their derivatives with antiproliferative properties. Nortopsentins A–C were found to exhibit in vitro cytotoxicity against the P388 murine leukaemia cell line. Their structural manipulation provided a wide range of derivatives with significant anti-tumour activity against human cell lines derived from different cancer types (bladder, colon, gastric, CNS, liver, lung, breast, melanoma, ovarian, pancreatic, prostate, pleural mesothelioma, renal, sarcoma, and uterus). In vivo assays on animal models also proved that Nortopsentins and related bis-indolyl compounds have potent anti-inflammatory activity. These remarks set the foundation for future investigations into the development of new Nortopsentin derivatives as new anticancer and anti-inflammatory agents.
    Keywords natural products ; marine alkaloids ; nortopsentin derivatives ; anticancer agents ; anti-inflammatory agents ; Organic chemistry ; QD241-441
    Subject code 540
    Language English
    Publishing date 2023-09-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  3. Article ; Online: Synthesis and Antioxidative Properties of 1,2,3,4-Tetrahydropyridine Derivatives with Different Substituents in 4-Position

    Daniele Aiello / Hendrik Jonas / Anna Carbone / Daniela Carbone / Camilla Pecoraro / Luisa Tesoriere / Jens Köhler / Bernhard Wünsch / Patrizia Diana

    Molecules, Vol 27, Iss 7423, p

    2022  Volume 7423

    Abstract: Natural products are an excellent source of inspiration for the development of new drugs. Among them, betalains have been extensively studied for their antioxidant properties and potential application as natural food dyes. Herein, we describe the seven- ... ...

    Abstract Natural products are an excellent source of inspiration for the development of new drugs. Among them, betalains have been extensively studied for their antioxidant properties and potential application as natural food dyes. Herein, we describe the seven-step synthesis of new betalamic acid analogs without carboxy groups in the 2- and 6-position with an overall yield of ~70%. The Folin–Ciocalteu assay was used to determine the antioxidant properties of protected intermediate 21 . Additionally, the five-step synthesis of betalamic acid analog 35 with three ester moieties was performed. Using NMR techniques, the stability of the obtained compounds towards oxygen was analyzed.
    Keywords indicaxanthins ; betalamic acid ; antioxidant ; dehydrobromination ; TEMPO oxidation ; (E)-(Z) configuration ; Organic chemistry ; QD241-441
    Language English
    Publishing date 2022-11-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  4. Article ; Online: A New Oxadiazole-Based Topsentin Derivative Modulates Cyclin-Dependent Kinase 1 Expression and Exerts Cytotoxic Effects on Pancreatic Cancer Cells

    Camilla Pecoraro / Barbara Parrino / Stella Cascioferro / Adrian Puerta / Amir Avan / Godefridus J. Peters / Patrizia Diana / Elisa Giovannetti / Daniela Carbone

    Molecules, Vol 27, Iss 19, p

    2022  Volume 19

    Abstract: Pancreatic ductal adenocarcinoma (PDAC) is a highly lethal form of cancer characterized by drug resistance, urging new therapeutic strategies. In recent years, protein kinases have emerged as promising pharmacological targets for the treatment of several ...

    Abstract Pancreatic ductal adenocarcinoma (PDAC) is a highly lethal form of cancer characterized by drug resistance, urging new therapeutic strategies. In recent years, protein kinases have emerged as promising pharmacological targets for the treatment of several solid and hematological tumors. Interestingly, cyclin-dependent kinase 1 (CDK1) is overexpressed in PDAC tissues and has been correlated to the aggressive nature of these tumors because of its key role in cell cycle progression and resistance to the induction of apoptosis. For these reasons, CDK1 is one of the main causes of chemoresistance, representing a promising pharmacological target. In this study, we report the synthesis of new 1,2,4-oxadiazole compounds and evaluate their ability to inhibit the cell growth of PATU-T, Hs766T, and HPAF-II cell lines and a primary PDAC cell culture (PDAC3). Compound 6b was the most active compound, with IC 50 values ranging from 5.7 to 10.7 µM. Molecular docking of 6b into the active site of CDK1 showed the ability of the compound to interact effectively with the adenosine triphosphate binding pocket. Therefore, we assessed its ability to induce apoptosis (which increased 1.5- and 2-fold in PATU-T and PDAC3 cells, respectively) and to inhibit CDK1 expression, which was reduced to 45% in Hs766T. Lastly, compound 6b passed the ADME prediction, showing good pharmacokinetic parameters. These data demonstrate that 6b displays cytotoxic activity, induces apoptosis, and targets CDK1, supporting further studies for the development of similar compounds against PDAC.
    Keywords 1,2,4-oxadiazole ; marine alkaloids ; topsentin ; CDK1 inhibitor ; pancreatic cancer ; PDAC ; Organic chemistry ; QD241-441
    Subject code 500
    Language English
    Publishing date 2022-12-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  5. Article ; Online: HIV-1-induced nuclear invaginations mediated by VAP-A, ORP3, and Rab7 complex explain infection of activated T cells

    Mark F. Santos / Germana Rappa / Jana Karbanová / Patrizia Diana / Girolamo Cirrincione / Daniela Carbone / David Manna / Feryal Aalam / David Wang / Cheryl Vanier / Denis Corbeil / Aurelio Lorico

    Nature Communications, Vol 14, Iss 1, Pp 1-

    2023  Volume 22

    Abstract: Abstract The mechanism of human immunodeficiency virus 1 (HIV-1) nuclear entry, required for productive infection, is not fully understood. Here, we report that in HeLa cells and activated CD4+ T cells infected with HIV-1 pseudotyped with VSV-G and ... ...

    Abstract Abstract The mechanism of human immunodeficiency virus 1 (HIV-1) nuclear entry, required for productive infection, is not fully understood. Here, we report that in HeLa cells and activated CD4+ T cells infected with HIV-1 pseudotyped with VSV-G and native Env protein, respectively, Rab7+ late endosomes containing endocytosed HIV-1 promote the formation of nuclear envelope invaginations (NEIs) by a molecular mechanism involving the VOR complex, composed of the outer nuclear membrane protein VAP-A, hyperphosphorylated ORP3 and Rab7. Silencing VAP-A or ORP3 and drug-mediated impairment of Rab7 binding to ORP3-VAP-A inhibited the nuclear transfer of the HIV-1 components and productive infection. In HIV-1-resistant quiescent CD4+ T cells, ORP3 was not hyperphosphorylated and neither VOR complex nor NEIs were formed. This new cellular pathway and its molecular players are potential therapeutic targets, perhaps shared by other viruses that require nuclear entry to complete their life cycle.
    Keywords Science ; Q
    Subject code 570
    Language English
    Publishing date 2023-08-01T00:00:00Z
    Publisher Nature Portfolio
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  6. Article ; Online: Thiazole Analogues of the Marine Alkaloid Nortopsentin as Inhibitors of Bacterial Biofilm Formation

    Anna Carbone / Stella Cascioferro / Barbara Parrino / Daniela Carbone / Camilla Pecoraro / Domenico Schillaci / Maria Grazia Cusimano / Girolamo Cirrincione / Patrizia Diana

    Molecules, Vol 26, Iss 81, p

    2021  Volume 81

    Abstract: 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 ...

    Abstract 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 and the Gram-negative strain Pseudomonas aeruginosa ATCC 15442. Most of the new compounds showed a marked selectivity against the Gram-positive strains. Remarkably, five compounds exhibited BIC 50 values against S. aureus ATCC 25923 ranging from 1.0 to 9.1 µM. The new compounds, affecting the biofilm formation without any interference on microbial growth, can be considered promising lead compounds for the development of a new class of anti-virulence agents.
    Keywords antibiofilm agents ; antibiotic resistance ; thiazole derivatives ; marine alkaloids analogues ; nortopsentin ; Organic chemistry ; QD241-441
    Subject code 540
    Language English
    Publishing date 2021-12-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  7. Article ; Online: New 1,2,4-Oxadiazole Nortopsentin Derivatives with Cytotoxic Activity

    Stella Cascioferro / Alessandro Attanzio / Veronica Di Sarno / Simona Musella / Luisa Tesoriere / Girolamo Cirrincione / Patrizia Diana / Barbara Parrino

    Marine Drugs, Vol 17, Iss 1, p

    2019  Volume 35

    Abstract: New analogs of nortopsentin, a natural 2,4-bis(3′-indolyl)imidazole alkaloid, in which the central imidazole ring of the natural lead was replaced by a 1,2,4-oxadiazole moiety, and in which a 7-azaindole portion substituted the original indole moiety, ... ...

    Abstract New analogs of nortopsentin, a natural 2,4-bis(3′-indolyl)imidazole alkaloid, in which the central imidazole ring of the natural lead was replaced by a 1,2,4-oxadiazole moiety, and in which a 7-azaindole portion substituted the original indole moiety, were efficiently synthesized. Among all derivatives, prescreened against the HCT-116 colon rectal carcinoma cell line, the two most active compounds were selected and further investigated in different human tumor cells showing IC50 values in the micromolar and submicromolar range. Flow cytometric analysis of propidium iodide-stained MCF-7 cells demonstrated that both the active derivatives caused cell cycle arrest in the G0–G1 phase. The cell death mechanism induced by the compounds was considered to be apoptotic by measuring the exposure of phosphatidylserine to the outer membrane and observed morphological evaluation using acridine orange/ethidium bromide double staining. Moreover, further tested on intestinal normal-like differentiated Caco-2 cell line, they exhibited preferential toxicity towards cancer cells.
    Keywords marine alkaloids ; nortopsentin analogs ; 1,2,4-oxadiazole derivatives ; anti-cancer agents ; antiproliferative activity ; Biology (General) ; QH301-705.5
    Subject code 540
    Language English
    Publishing date 2019-01-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  8. Article ; Online: 3-(6-Phenylimidazo [2,1- b ][1,3,4]thiadiazol-2-yl)-1 H -Indole Derivatives as New Anticancer Agents in the Treatment of Pancreatic Ductal Adenocarcinoma

    Stella Cascioferro / Giovanna Li Petri / Barbara Parrino / Btissame El Hassouni / Daniela Carbone / Vincenzo Arizza / Ugo Perricone / Alessandro Padova / Niccola Funel / Godefridus J. Peters / Girolamo Cirrincione / Elisa Giovannetti / Patrizia Diana

    Molecules, Vol 25, Iss 2, p

    2020  Volume 329

    Abstract: A new series of imidazo[2,1- b ][1,3,4]thiadiazole derivatives was efficiently synthesized and screened for their in vitro antiproliferative activity on a panel of pancreatic ductal adenocarcinoma (PDAC) cells, including SUIT-2, Capan-1 and Panc-1. ... ...

    Abstract A new series of imidazo[2,1- b ][1,3,4]thiadiazole derivatives was efficiently synthesized and screened for their in vitro antiproliferative activity on a panel of pancreatic ductal adenocarcinoma (PDAC) cells, including SUIT-2, Capan-1 and Panc-1. Compounds 9c and 9l, showed relevant in vitro antiproliferative activity on all three pre-clinical models with half maximal inhibitory concentration (IC 50 ) ranging from 5.11 to 10.8 µM, while the compounds 9e and 9n were active in at least one cell line. In addition, compound 9c significantly inhibited the migration rate of SUIT-2 and Capan-1 cells in the scratch wound-healing assay. In conclusion, our results will support further studies to increase the library of imidazo [2,1- b ][1,3,4] thiadiazole derivatives for deeper understanding of the relationship between biological activity of the compounds and their structures in the development of new antitumor compounds against pancreatic diseases.
    Keywords imidazo[2,1- b ][1,3,4]thiadiazole derivatives ; antiproliferative activity ; migration assay ; indole compounds ; pancreatic cancer ; resistance ; Organic chemistry ; QD241-441
    Subject code 540
    Language English
    Publishing date 2020-01-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  9. Article ; Online: New Tripentone Analogs with Antiproliferative Activity

    Barbara Parrino / Salviana Ullo / Alessandro Attanzio / Virginia Spanò / Stella Cascioferro / Alessandra Montalbano / Paola Barraja / Luisa Tesoriere / Girolamo Cirrincione / Patrizia Diana

    Molecules, Vol 22, Iss 11, p

    2017  Volume 2005

    Abstract: Tripentones represent an interesting class of compounds due to their significant cytotoxicity against different human tumor cells in the submicro-nanomolar range. New tripentone analogs, in which a pyridine moiety replaces the thiophene ring originating ... ...

    Abstract Tripentones represent an interesting class of compounds due to their significant cytotoxicity against different human tumor cells in the submicro-nanomolar range. New tripentone analogs, in which a pyridine moiety replaces the thiophene ring originating the fused azaindole system endowed with anticancer activity viz 8H-thieno[2,3-b]pyrrolizinones, were efficiently synthesized in four steps with fair overall yields (34–57%). All tripentone derivatives were tested in the range of 0.1–100 μM for cytotoxicity against two human tumor cell lines, HCT-116 (human colorectal carcinoma) and MCF-7 (human breast cancer). The most active derivative, with GI50 values of 4.25 µM and 20.73 µM for HCT-116 and MCF-7 cells, respectively, did not affect the viability of Caco-2 differentiated in normal intestinal-like cells, suggesting tumor cells as the main target of its cytotoxic action. The same compound was further investigated in order to study its mode of action. Results showed that it did not exert necrotic effects, while induced a clear shift of viable cells towards early apoptosis. Flow cytometric analysis demonstrated that this compound caused cell cycle alteration, inhibiting its progression in S and G2/M phases.
    Keywords tripentones ; aza-indoles ; 8H-thieno[2,3-b]pyrrolizinones ; antitumor activity ; proapoptotic agents ; Organic chemistry ; QD241-441
    Subject code 610
    Language English
    Publishing date 2017-11-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  10. Article ; Online: Synthesis of pyrazolo[4,3-c][1,2,6]benzothiadiazocine, a new ring system as potential COX inhibitor

    Onofrio Migliara / Virginia Spanò / Barbara Parrino / Cristina Ciancimino / Patrizia Diana

    ARKIVOC, Vol 2012, Iss 2, Pp 41-

    2012  Volume 49

    Keywords Organic chemistry ; QD241-441
    Language English
    Publishing date 2012-03-01T00:00:00Z
    Publisher Arkat USA, Inc.
    Document type Article ; Online
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