Over the years, carbazoles have been largely studied for their numerous biological properties, in... more Over the years, carbazoles have been largely studied for their numerous biological properties, including antibacterial, antimalarial, antioxidant, antidiabetic, neuroprotective, anticancer, and many more. Some of them have gained great interest for their anticancer activity in breast cancer due to their capability in inhibiting essential DNA-dependent enzymes, namely topoisomerases I and II. With this in mind, we studied the anticancer activity of a series of carbazole derivatives against two breast cancer cell lines, namely the triple negative MDA-MB-231 and MCF-7 cells. Compounds 3 and 4 were found to be the most active towards the MDA-MB-231 cell line without interfering with the normal counterpart. Using docking simulations, we assessed the ability of these carbazole derivatives to bind human topoisomerases I and II and actin. In vitro specific assays confirmed that the lead compounds selectively inhibited the human topoisomerase I and interfered with the normal organization of ...
The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) was the seventh known human coro... more The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) was the seventh known human coronavirus, and it was identified in Wuhan, Hubei province, China, in 2020. It caused the highly contagious disease called coronavirus disease 2019 (COVID-19), declared a global pandemic by the World Health Organization (WHO) on 11 March 2020. A great number of studies in the search of new therapies and vaccines have been carried out in these three long years, producing a series of successes; however, the need for more effective vaccines, therapies and other solutions is still being pursued. This review represents a tracking shot of the current pharmacological therapies used for the treatment of COVID-19.
Metal complexes play a crucial role in pharmaceutical sciences owing to their wide and significan... more Metal complexes play a crucial role in pharmaceutical sciences owing to their wide and significant activities. Schiff bases (SBs) are multifaceted pharmacophores capable of forming chelating complexes with various metals in different oxidation states. Complexes with SBs are extensively studied for their numerous advantages, including low cost and simple synthetic strategies. They have been reported to possess a variety of biological activities, including antimicrobial, anticancer, antioxidant, antimalarial, analgesic, antiviral, antipyretic, and antidiabetic ones. This review summarizes the most recent studies on the antimicrobial and antiproliferative activities of SBs-metal complexes. Moreover, recent studies regarding mononuclear and binuclear complexes with SBs are described, including antioxidant, antidiabetic, antimalarial, antileishmanial, anti-Alzheimer, and catecholase activities.
Cancer is going to be the first cause of mortality worldwide in the 21th century. It is considere... more Cancer is going to be the first cause of mortality worldwide in the 21th century. It is considered a multifactorial disease that results from the combined influence of many genetic aberrations, leading to abnormal cell proliferation. As microtubules are strongly implicated in cellular growth, they represent an important target for cancer treatment. The well‐known microtubule‐targeting agents (MTAs) including paclitaxel, colchicine and vinca alkaloids are commonly used in the treatment of various cancers. However, adverse effects and drug resistance are major limitations in their clinical use.To find new candidates able to induce microtubule alteration with reduced toxic effects or drug resistance, we studied a small new series of derivatives that present imidazolinic, guanidinic, thioureidic and hydrazinic groups (1–9). All the compounds were tested for their antitumor activity against a panel of six tumoral cell models. In particular, compound 8 (nonane‐1,9‐diyl‐bis‐S‐amidinothiour...
La Chimica inorganica applicata alla Biomedicina, nota oggi come la medicina elementare, è un imp... more La Chimica inorganica applicata alla Biomedicina, nota oggi come la medicina elementare, è un importante campo della Chimica, poco esplorato. Essa offre il potenziale per la progettazione di nuovi agenti terapeutici e diagnostici utili al trattamento e alla comprensione delle patologie oncologiche, che sono ora intrattabili [1-3]. Gli Elementi inorganici hanno un ruolo cruciale nei processi biologici e biomedici; infatti, è evidente che molti composti organici utilizzati in medicina non hanno una modalità di azione chiara; alcuni di essi sono attivati o biotrasformati da ioni metallici, tra cui i metallo-enzimi [4], altri hanno un effetto diretto o indiretto sul metabolismo degli ioni metallici. La Biomedicina della chimica inorganica offre reali possibilità per le industrie farmaceutiche, che tradizionalmente sono dominate dalla chimica organica, per la scoperta di farmaci innovativi con nuovi meccanismi d’azione. Questo campo è stato stimolato dal successo del cisplatino, il farmaco antitumorale più venduto al mondo, e dai complessi del platino con ridotta tossicità, mentre l’attività contro i tumori chemio-resistenti è attualmente in sperimentazione clinica. Altri complessi organo-metallici, come il titanocene dicloruro, sono stati somministrati ai pazienti mostrando una promettente attività antimetastatica. Recenti progressi nella comprensione della chimica di coordinazione e biochimica dei metallo-farmaci, come gli antiartritici e farmaci antiulcera, aprono all’individuazione di nuovi composti farmacologicamente attivi. La crescente conoscenza della chimica organo-metallica fornirà gli elementi per la progettazione di nuovi composti nella terapia del cancro
1 Department of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, 84084, Fisciano (SA),... more 1 Department of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, 84084, Fisciano (SA), Italy. 2 IRCCS (National Cancer Institute,IRCCS,”G.Pascale” Foundation), Via Mariano Semmola, 52-108, 80131, Naples. 3 Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Arcavacata’s Campus, via Pietro Bucci, 87036 Arcavacata di Rende (CS), Italy. Department of Chemistry and Biology, University of Salerno, Via Giovanni Paolo II 132, 84084, Fisciano (SA), Italy
Over the years, carbazoles have been largely studied for their numerous biological properties, in... more Over the years, carbazoles have been largely studied for their numerous biological properties, including antibacterial, antimalarial, antioxidant, antidiabetic, neuroprotective, anticancer, and many more. Some of them have gained great interest for their anticancer activity in breast cancer due to their capability in inhibiting essential DNA-dependent enzymes, namely topoisomerases I and II. With this in mind, we studied the anticancer activity of a series of carbazole derivatives against two breast cancer cell lines, namely the triple negative MDA-MB-231 and MCF-7 cells. Compounds 3 and 4 were found to be the most active towards the MDA-MB-231 cell line without interfering with the normal counterpart. Using docking simulations, we assessed the ability of these carbazole derivatives to bind human topoisomerases I and II and actin. In vitro specific assays confirmed that the lead compounds selectively inhibited the human topoisomerase I and interfered with the normal organization of ...
The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) was the seventh known human coro... more The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) was the seventh known human coronavirus, and it was identified in Wuhan, Hubei province, China, in 2020. It caused the highly contagious disease called coronavirus disease 2019 (COVID-19), declared a global pandemic by the World Health Organization (WHO) on 11 March 2020. A great number of studies in the search of new therapies and vaccines have been carried out in these three long years, producing a series of successes; however, the need for more effective vaccines, therapies and other solutions is still being pursued. This review represents a tracking shot of the current pharmacological therapies used for the treatment of COVID-19.
Metal complexes play a crucial role in pharmaceutical sciences owing to their wide and significan... more Metal complexes play a crucial role in pharmaceutical sciences owing to their wide and significant activities. Schiff bases (SBs) are multifaceted pharmacophores capable of forming chelating complexes with various metals in different oxidation states. Complexes with SBs are extensively studied for their numerous advantages, including low cost and simple synthetic strategies. They have been reported to possess a variety of biological activities, including antimicrobial, anticancer, antioxidant, antimalarial, analgesic, antiviral, antipyretic, and antidiabetic ones. This review summarizes the most recent studies on the antimicrobial and antiproliferative activities of SBs-metal complexes. Moreover, recent studies regarding mononuclear and binuclear complexes with SBs are described, including antioxidant, antidiabetic, antimalarial, antileishmanial, anti-Alzheimer, and catecholase activities.
Cancer is going to be the first cause of mortality worldwide in the 21th century. It is considere... more Cancer is going to be the first cause of mortality worldwide in the 21th century. It is considered a multifactorial disease that results from the combined influence of many genetic aberrations, leading to abnormal cell proliferation. As microtubules are strongly implicated in cellular growth, they represent an important target for cancer treatment. The well‐known microtubule‐targeting agents (MTAs) including paclitaxel, colchicine and vinca alkaloids are commonly used in the treatment of various cancers. However, adverse effects and drug resistance are major limitations in their clinical use.To find new candidates able to induce microtubule alteration with reduced toxic effects or drug resistance, we studied a small new series of derivatives that present imidazolinic, guanidinic, thioureidic and hydrazinic groups (1–9). All the compounds were tested for their antitumor activity against a panel of six tumoral cell models. In particular, compound 8 (nonane‐1,9‐diyl‐bis‐S‐amidinothiour...
La Chimica inorganica applicata alla Biomedicina, nota oggi come la medicina elementare, è un imp... more La Chimica inorganica applicata alla Biomedicina, nota oggi come la medicina elementare, è un importante campo della Chimica, poco esplorato. Essa offre il potenziale per la progettazione di nuovi agenti terapeutici e diagnostici utili al trattamento e alla comprensione delle patologie oncologiche, che sono ora intrattabili [1-3]. Gli Elementi inorganici hanno un ruolo cruciale nei processi biologici e biomedici; infatti, è evidente che molti composti organici utilizzati in medicina non hanno una modalità di azione chiara; alcuni di essi sono attivati o biotrasformati da ioni metallici, tra cui i metallo-enzimi [4], altri hanno un effetto diretto o indiretto sul metabolismo degli ioni metallici. La Biomedicina della chimica inorganica offre reali possibilità per le industrie farmaceutiche, che tradizionalmente sono dominate dalla chimica organica, per la scoperta di farmaci innovativi con nuovi meccanismi d’azione. Questo campo è stato stimolato dal successo del cisplatino, il farmaco antitumorale più venduto al mondo, e dai complessi del platino con ridotta tossicità, mentre l’attività contro i tumori chemio-resistenti è attualmente in sperimentazione clinica. Altri complessi organo-metallici, come il titanocene dicloruro, sono stati somministrati ai pazienti mostrando una promettente attività antimetastatica. Recenti progressi nella comprensione della chimica di coordinazione e biochimica dei metallo-farmaci, come gli antiartritici e farmaci antiulcera, aprono all’individuazione di nuovi composti farmacologicamente attivi. La crescente conoscenza della chimica organo-metallica fornirà gli elementi per la progettazione di nuovi composti nella terapia del cancro
1 Department of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, 84084, Fisciano (SA),... more 1 Department of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, 84084, Fisciano (SA), Italy. 2 IRCCS (National Cancer Institute,IRCCS,”G.Pascale” Foundation), Via Mariano Semmola, 52-108, 80131, Naples. 3 Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Arcavacata’s Campus, via Pietro Bucci, 87036 Arcavacata di Rende (CS), Italy. Department of Chemistry and Biology, University of Salerno, Via Giovanni Paolo II 132, 84084, Fisciano (SA), Italy
Uploads
Papers by Pasquale Longo