Pubblicazioni

First-in-Class Selenium-Containing Potent Serotonin Receptor 5-HT6 Agents with a Beneficial Neuroprotective Profile against Alzheimer's Disease

2024 - JOURNAL OF MEDICINAL CHEMISTRY
Pyka, Patryk; Haberek, Wawrzyniec; Więcek, Małgorzata; Szymanska, Ewa; Ali, Wesam; Cios, Agnieszka; Jastrzębska-Więsek, Magdalena; Satała, Grzegorz; Podlewska, Sabina; Di Giacomo, Silvia; Di Sotto, Antonella; Garbo, Sabrina; Karcz, Tadeusz; Lambona, Chiara; Marocco, Francesco; Latacz, Gniewomir; Sudoł-Tałaj, Sylwia; Mordyl, Barbara; Głuch-Lutwin, Monika; Siwek, Agata; Czarnota-Łydka, Kinga; Gogola, Dawid; Olejarz-Maciej, Agnieszka; Wilczyńska-Zawal, Natalia; Honkisz-Orzechowska, Ewelina; Starek, Małgorzata; Dąbrowska, Monika; Kucwaj-Brysz, Katarzyna; Fioravanti, Rossella; Nasim, Muhammad Jawad; Hittinger, Marius; Partyka, Anna; Wesołowska, Anna; Battistelli, Cecilia; Zwergel, Clemens; Handzlik, Jadwiga

SIRT3 Activation a Promise in Drug Development? New Insights into SIRT3 Biology and Its Implications on the Drug Discovery Process

2024 - JOURNAL OF MEDICINAL CHEMISTRY
Lambona, Chiara; Zwergel, Clemens; Valente, Sergio; Mai, Antonello

Fragment merging, growing, and linking identify new trypanothione reductase inhibitors for Leishmaniasis

2024 - JOURNAL OF MEDICINAL CHEMISTRY
Exertier, Cécile; Salerno, Alessandra; Antonelli, Lorenzo; Fiorillo, Annarita; Ocello, Riccardo; Seghetti, Francesca; Caciolla, Jessica; Uliassi, Elisa; Masetti, Matteo; Fiorentino, Eleonora; Orsini, Stefania; Di Muccio, Trentina; Ilari, Andrea; Bolognesi, Maria Laura

Specific Inhibitors of Mitochondrial Deacylase Sirtuin 4 Endowed with Cellular Activity

2024 - JOURNAL OF MEDICINAL CHEMISTRY
Pannek, M.; Alhalabi, Z.; Tomaselli, D.; Menna, M.; Fiorentino, F.; Robaa, D.; Weyand, M.; Puhlmann, M.; Tomassi, S.; Barreca, F.; Tafani, M.; Zaganjor, E.; Haigis, M. C.; Sippl, W.; Rotili, D.; Mai, A.; Steegborn, C.

Computational Design of Pore-Forming Peptides with Potent Antimicrobial and Anticancer Activities

2024 - JOURNAL OF MEDICINAL CHEMISTRY
Deb, Rahul; Torres, Marcelo D T; Boudný, Miroslav; Koběrská, Markéta; Cappiello, Floriana; Popper, Miroslav; Dvořáková Bendová, Kateřina; Drabinová, Martina; Hanáčková, Adelheid; Jeannot, Katy; Petřík, Miloš; Mangoni, Maria Luisa; Balíková Novotná, Gabriela; Mráz, Marek; de la Fuente-Nunez, Cesar; Vácha, Robert

SAR Analysis of Novel Coxsackie virus A9 Capsid Binders

2024 - JOURNAL OF MEDICINAL CHEMISTRY
Tammaro, Chiara; Plavec, Zlatka; Myllymäki, Laura; Mitchell, Cristopher; Consalvi, Sara; Biava, Mariangela; Ciogli, Alessia; Domanska, Aušra; Leppilampi, Valtteri; Buckner, Cienna; Manetto, Simone; Sciò, Pietro; Coluccia, Antonio; Laajala, Mira; Dondio, Giulio M; Bigogno, Chiara; Marjomäki, Varpu; Butcher, Sarah J; Poce, Giovanna

Development of N-(4-(1 H-Imidazol-1-yl)phenyl)-4-chlorobenzenesulfonamide, a Novel Potent Inhibitor of β-Catenin with Enhanced Antitumor Activity and Metabolic Stability

2024 - JOURNAL OF MEDICINAL CHEMISTRY
Puxeddu, Michela; Ling, Lele; Ripa, Silvia; D'Ambrosio, Michele; Nalli, Marianna; Parisi, Anastasia; Scio', Pietro; Coluccia, Antonio; Granese, Arianna; Santelli, Martina; Masci, Domiziana; Cuřínová, Petra; Naro, Chiara; Sette, Claudio; Pastore, Arianna; Stornaiuolo, Mariano; Bigogno, Chiara; Dondio, Giulio; DI MAGNO, Laura; Canettieri, Gianluca; Liu, Te; Silvestri, Romano; LA REGINA, Giuseppe

Novel Far-Red Fluorescent 1,4-Dihydropyridines for L-Type Calcium Channel Imaging

2024 - JOURNAL OF MEDICINAL CHEMISTRY
Borgarelli, Carlotta; Klingl, Yvonne E; Escamilla-Ayala, Abril; Scarponi, Carlotta; La Rovere, Rita M L; Stoklund Dittlau, Katarina; Bultynck, Geert; Sampaolesi, Maurilio; Schoenberger, Matthias; Munck, Sebastian; Van Den Bosch, Ludo; De Borggraeve, Wim M; Ismalaj, Ermal

Systematic Design of Adenosine Analogs as Inhibitors of a Clostridioides difficile-Specific DNA Adenine Methyltransferase Required for Normal Sporulation and Persistence

2023 - JOURNAL OF MEDICINAL CHEMISTRY
Zhou, Jujun; Horton, John R.; Menna, Martina; Fiorentino, Francesco; Ren, Ren; Yu, Dan; Hajian, Taraneh; Vedadi, Masoud; Mazzoccanti, Giulia; Ciogli, Alessia; Weinhold, Elmar; Hüben, Michael; Blumenthal, Robert M.; Zhang, Xing; Mai, Antonello; Rotili, Dante; Cheng, Xiaodong

Novel Insights on CAI–CORM Hybrids: Evaluation of the CO Releasing Properties and Pain-Relieving Activity of Differently Substituted Coumarins for the Treatment of Rheumatoid Arthritis

2023 - JOURNAL OF MEDICINAL CHEMISTRY
Berrino, Emanuela; Micheli, Laura; Carradori, Simone; di Cesare Mannelli, Lorenzo; Guglielmi, Paolo; De Luca, Alessandro; Carta, Fabrizio; Ghelardini, Carla; Secci, Daniela; Supuran, Claudiu T.

METTL3 from Target Validation to the First Small-Molecule Inhibitors: A Medicinal Chemistry Journey

2023 - JOURNAL OF MEDICINAL CHEMISTRY
Fiorentino, Francesco; Menna, Martina; Rotili, Dante; Valente, Sergio; Mai, Antonello

First-in-Class Selective Inhibitors of the Lysine Acetyltransferase KAT8

2023 - JOURNAL OF MEDICINAL CHEMISTRY
Fiorentino, Francesco; Sementilli, Sara; Menna, Martina; Turrisi, Federica; Tomassi, Stefano; Pellegrini, FRANCESCA ROMANA; Iuzzolino, Angela; D'Acunzo, Francesca; Feoli, Alessandra; Wapenaar, Hannah; Taraglio, Sophie; Fraschetti, Caterina; Del Bufalo, Donatella; Sbardella, Gianluca; Dekker, Frank J.; Paiardini, Alessandro; Trisciuoglio, Daniela; Mai, Antonello; Rotili, Dante

Novel 1,4-Dihydropyridines as Specific Binders and Activators of SIRT3 Impair Cell Viability and Clonogenicity and Downregulate Hypoxia-Induced Targets in Cancer Cells

2023 - JOURNAL OF MEDICINAL CHEMISTRY
Zwergel, Clemens; Aventaggiato, Michele; Garbo, Sabrina; DI BELLO, Elisabetta; Fassari, Bruno; Noce, Beatrice; Castiello, Carola; Lambona, Chiara; Barreca, Federica; Rotili, Dante; Fioravanti, Rossella; Schmalz, Thomas; Weyand, Michael; Niedermeier, Amelie; Tripodi, Marco; Colotti, Gianni; Steegborn, Clemens; Battistelli, Cecilia; Tafani, Marco; Valente, Sergio; Mai, Antonello

Amino Acids as Chelating Ligands for Platinum: Enhanced Stability in an Aqueous Environment Promoted by Biocompatible Molecules

2023 - JOURNAL OF MEDICINAL CHEMISTRY
Cucchiaro, Andrea; Scherfler, Amelie; Corinti, Davide; Berden, Giel; Oomens, Jos; Wurst, Klaus; Gust, Ronald; Crestoni, Maria Elisa; Kircher, Brigitte; Cziferszky, Monika

Miconazole-like Scaffold is a Promising Lead for Naegleria fowleri-Specific CYP51 Inhibitors

2023 - JOURNAL OF MEDICINAL CHEMISTRY
Sharma, Vandna; Madia, VALENTINA NOEMI; Tudino, Valeria; V Nguyen, Jennifer; Debnath, Anjan; Messore, Antonella; Ialongo, Davide; Patacchini, Elisa; Palenca, Irene; BASILI FRANZIN, Silvia; Seguella, Luisa; Esposito, Giuseppe; Petrucci, Rita; DI MATTEO, Paola; Bortolami, Martina; Saccoliti, Francesco; DI SANTO, Roberto; Scipione, Luigi; Costi, Roberta; M Podust, Larissa

4-(3-Phenyl-4-(3,4,5-trimethoxybenzoyl)-1H-pyrrol-1-yl)benzenesulfonamide, a Novel Carbonic Anhydrase and Wnt/β-Catenin Signaling Pathway Dual-Targeting Inhibitor with Potent Activity against Multidrug Resistant Cancer Cells

2023 - JOURNAL OF MEDICINAL CHEMISTRY
Masci, Domiziana; Puxeddu, Michela; Di Magno, Laura; D'Ambrosio, Michele; Parisi, Anastasia; Nalli, Marianna; Bai, Ruoli; Coluccia, Antonio; Sciò, Pietro; Orlando, Viviana; D'Angelo, Sara; Biagioni, Stefano; Urbani, Andrea; Hamel, Ernest; Nocentini, Alessio; Filiberti, Serena; Turati, Marta; Ronca, Roberto; Kopecka, Joanna; Riganti, Chiara; Fionda, Cinzia; Bordone, Rosa; Della Rocca, Giorgia; Canettieri, Gianluca; Supuran, Claudiu T; Silvestri, Romano; La Regina, Giuseppe

Therapeutic Potential and Activity Modulation of the Protein Lysine Deacylase Sirtuin 5

2022 - JOURNAL OF MEDICINAL CHEMISTRY
Fiorentino, F.; Castiello, C.; Mai, A.; Rotili, D.

Potent and Specific Activators for Mitochondrial Sirtuins Sirt3 and Sirt5

2022 - JOURNAL OF MEDICINAL CHEMISTRY
Suenkel, Benjamin; Valente, Sergio; Zwergel, Clemens; Weiss, Sandra; DI BELLO, Elisabetta; Fioravanti, Rossella; Aventaggiato, Michele; Amorim, João A.; Garg, Neha; Kumar, Surinder; Lombard, David B.; Hu, Tuo; Singh, Pankaj K.; Tafani, Marco; Palmeira, Carlos M.; Sinclair, David; Mai, Antonello; Steegborn, Clemens

Induction of Ferroptosis in Glioblastoma and Ovarian Cancers by a New Pyrrole Tubulin Assembly Inhibitor

2022 - JOURNAL OF MEDICINAL CHEMISTRY
Puxeddu, Michela; Wu, Jianchao; Bai, Ruoli; D'Ambrosio, Michele; Nalli, Marianna; Coluccia, Antonio; Manetto, Simone; Ciogli, Alessia; Masci, Domiziana; Urbani, Andrea; Fionda, Cinzia; Coni, Sonia; Bordone, Rosa; Canettieri, Gianluca; Bigogno, Chiara; Dondio, Giulio; Hamel, Ernest; Liu, Te; Silvestri, Romano; LA REGINA, Giuseppe

Quinolinonyl non-diketo acid derivatives as Inhibitors of HIV-1 ribonuclease H and polymerase functions of reverse transcriptase

2021 - JOURNAL OF MEDICINAL CHEMISTRY
Messore, Antonella; Corona, Angela; Madia, Valentina Noemi; Saccoliti, Francesco; Tudino, Valeria; De Leo, Alessandro; Ialongo, Davide; Scipione, Luigi; De Vita, Daniela; Amendola, Giorgio; Novellino, Ettore; Cosconati, Sandro; Métifiot, Mathieu; Andreola, Marie-Line; Esposito, Francesca; Grandi, Nicole; Tramontano, Enzo; Costi, Roberta; Di Santo, Roberto

Structure-Guided Development of Small-Molecule PRC2 Inhibitors Targeting EZH2–EED Interaction

2021 - JOURNAL OF MEDICINAL CHEMISTRY
Du, Daohai; Xu, Dandan; Zhu, Licheng; Stazi, Giulia; Zwergel, Clemens; Liu, Yanli; Luo, Zhongyuan; Li, Yuanqing; Zhang, Yuanyuan; Zhu, Kongkai; Ding, Yiluan; Liu, Jingqiu; Fan, Shijie; Zhao, Kaiyan; Zhang, Naixia; Kong, Xiangqian; Jiang, Hualiang; Chen, Kaixian; Zhao, Kehao; Valente, Sergio; Min, Jinrong; Duan, Wenhu; Luo, Cheng

First-in-Class Inhibitors of the Ribosomal Oxygenase MINA53

2021 - JOURNAL OF MEDICINAL CHEMISTRY
Nowak, R. P.; Tumber, A.; Hendrix, E.; Ansari, M. S. Z.; Sabatino, M.; Antonini, L.; Andrijes, R.; Salah, E.; Mautone, N.; Pellegrini, F. R.; Simelis, K.; Kawamura, A.; Johansson, C.; Passeri, D.; Pellicciari, R.; Ciogli, A.; Del Bufalo, D.; Ragno, R.; Coleman, M. L.; Trisciuoglio, D.; Mai, A.; Oppermann, U.; Schofield, C. J.; Rotili, D.

Polycomb repressive complex 2 modulation through the development of EZH2–EED interaction inhibitors and EED binders

2021 - JOURNAL OF MEDICINAL CHEMISTRY
Tomassi, Stefano; Romanelli, Annalisa; Zwergel, Clemens; Valente, Sergio; Mai, Antonello

First-in-class cyclic Temporin L analogue: design, synthesis, and antimicrobial assessment

2021 - JOURNAL OF MEDICINAL CHEMISTRY
Bellavita, R.; Casciaro, B.; Di Maro, S.; Brancaccio, D.; Carotenuto, A.; Falanga, A.; Cappiello, F.; Buommino, E.; Galdiero, S.; Novellino, E.; Grossmann, T. N.; Mangoni, M. L.; Merlino, F.; Grieco, P.

Emerging Therapeutic Potential of SIRT6 Modulators

2021 - JOURNAL OF MEDICINAL CHEMISTRY
Fiorentino, F.; Mai, A.; Rotili, D.

© Università degli Studi di Roma "La Sapienza" - Piazzale Aldo Moro 5, 00185 Roma