The Monti Lab Innovation in Chemical Genomics & Drug Optimisation

Research

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2023

Structure-Activity Relationships, Tolerability and Efficacy of Microtubule-Active 1,2,4-Triazolo 1,5-a pyrimidines as Potential Candidates to Treat Human African Trypanosomiasis.
Structure-Activity Relationships, Tolerability and Efficacy of Microtubule-Active 1,2,4-Triazolo[1,5-a]pyrimidines as Potential Candidates to Treat Human African Trypanosomiasis.
Ludovica Monti, Lawrence J Liu, Carmine Varricchio, Bobby Lucero, Thibault Alle, …, Michael Gilson, Kurt R Brunden, Andrea Brancale, Conor R Caffrey, Carlo Ballatore
ChemMedChem  ·  24 Jul 2023  ·  pmid:37429821
G-Quadruplexes as Key Transcriptional Regulators in Neglected Trypanosomatid Parasites.
G-Quadruplexes as Key Transcriptional Regulators in Neglected Trypanosomatid Parasites.
Ludovica Monti, Marco Di Antonio
Chembiochem : a European journal of chemical biology  ·  23 May 2023  ·  pmid:37146230
Structure-activity relationship of dibenzylideneacetone analogs against the neglected disease pathogen, Trypanosoma brucei
Structure-activity relationship of dibenzylideneacetone analogs against the neglected disease pathogen, Trypanosoma brucei
Karol R. Francisco, Ludovica Monti, Wenqian Yang, Hayoung Park, Lawrence J. Liu, …, Luis O. Regasini, Antônio Eduardo Miller Crotti, Romano Silvestri, Lizandra Guidi Magalhães, Conor R. Caffrey
Bioorganic & Medicinal Chemistry Letters  ·  01 Feb 2023  ·  doi:10.1016/j.bmcl.2023.129123

2022

From rational design to serendipity: Discovery of novel thiosemicarbazones as potent trypanocidal compounds
From rational design to serendipity: Discovery of novel thiosemicarbazones as potent trypanocidal compounds
Saulo Fehelberg Pinto Braga, Viviane Corrêa Santos, Rafael Pinto Vieira, Elany Barbosa da Silva, Ludovica Monti, …, Luiz Carlos Dias, Conor R. Caffrey, Jair L. Siqueira-Neto, Renata Barbosa de Oliveira, Rafaela Salgado Ferreira
European Journal of Medicinal Chemistry  ·  01 Dec 2022  ·  doi:10.1016/j.ejmech.2022.114876
G-quadruplexes Mark Sites of Methylation Instability Associated with Ageing and Cancer.
G-quadruplexes Mark Sites of Methylation Instability Associated with Ageing and Cancer.
Jonas Rauchhaus, Jenna Robinson, Ludovica Monti, Marco Di Antonio
Genes  ·  17 Sep 2022  ·  pmid:36140833
Tubulin and Microtubules as Drug Targets for Potential Cancer Chemotherapy and CNS-Directed Therapies
Tubulin and Microtubules as Drug Targets for Potential Cancer Chemotherapy and CNS-Directed Therapies
Ludovica Monti
Sapienza Università Editrice  ·  01 Jan 2022  ·  doi:10.13133/9788893772426
Long-range DNA interactions: inter-molecular G-quadruplexes and their potential biological relevance
Long-range DNA interactions: inter-molecular G-quadruplexes and their potential biological relevance
Denise Liano, Ludovica Monti, Souroprobho Chowdhury, Federica Raguseo, Marco Di Antonio
Chemical Communications  ·  01 Jan 2022  ·  doi:10.1039/d2cc04872h

2021

Structure-Based Optimization of Quinazolines as Cruzain and
Structure-Based Optimization of Quinazolines as Cruzain and
Elany Barbosa da Silva, Débora A Rocha, Isadora S Fortes, Wenqian Yang, Ludovica Monti, Jair L Siqueira-Neto, Conor R Caffrey, James McKerrow, Saulo F Andrade, Rafaela S Ferreira
Journal of medicinal chemistry  ·  30 Aug 2021  ·  pmid:34461718
Drug Discovery and Development for Kinetoplastid Diseases
Drug Discovery and Development for Kinetoplastid Diseases
Conor R. Caffrey, Dietmar Steverding, Rafaela S. Ferreira, Renata B. de Oliveira, Anthony J. O’Donoghue, …, Alex M. Clark, Melina Mottin, Carolina H. Andrade, Jair L. de Siqueira‐Neto, Sean Ekins
Burger's Medicinal Chemistry and Drug Discovery  ·  26 Apr 2021  ·  doi:10.1002/0471266949.bmc235.pub2
Evaluation of the Structure-Activity Relationship of Microtubule-Targeting 1,2,4-Triazolo 1,5-
Evaluation of the Structure-Activity Relationship of Microtubule-Targeting 1,2,4-Triazolo[1,5-
Killian Oukoloff, Goodwell Nzou, Carmine Varricchio, Bobby Lucero, Thibault Alle, …, Virginia M-Y Lee, Amos B Smith, Andrea Brancale, Kurt R Brunden, Carlo Ballatore
Journal of medicinal chemistry  ·  07 Jan 2021  ·  pmid:33411523

2020

Congeners Derived from Microtubule-Active Phenylpyrimidines Produce a Potent and Long-Lasting Paralysis of
Congeners Derived from Microtubule-Active Phenylpyrimidines Produce a Potent and Long-Lasting Paralysis of
Ludovica Monti, Anne-Sophie Cornec, Killian Oukoloff, Jane Kovalevich, Kristen Prijs, …, Lawrence J Liu, Ali Syed, Danielle E Skinner, Carlo Ballatore, Conor R Caffrey
ACS infectious diseases  ·  31 Oct 2020  ·  pmid:33135408
Identification of anisomycin, prodigiosin and obatoclax as compounds with broad-spectrum anti-parasitic activity.
Identification of anisomycin, prodigiosin and obatoclax as compounds with broad-spectrum anti-parasitic activity.
Gretchen Ehrenkaufer, Pengyang Li, Erin E Stebbins, Monica M Kangussu-Marcolino, Anjan Debnath, …, Ludovica Monti, Conor R Caffrey, Christopher D Huston, Bo Wang, Upinder Singh
PLoS neglected tropical diseases  ·  20 Mar 2020  ·  pmid:32196500

2018

Brain-Penetrant Triazolopyrimidine and Phenylpyrimidine Microtubule Stabilizers as Potential Leads to Treat Human African Trypanosomiasis.
Brain-Penetrant Triazolopyrimidine and Phenylpyrimidine Microtubule Stabilizers as Potential Leads to Treat Human African Trypanosomiasis.
Ludovica Monti, Steven C Wang, Killian Oukoloff, Amos B Smith, Kurt R Brunden, Conor R Caffrey, Carlo Ballatore
ChemMedChem  ·  07 Aug 2018  ·  pmid:29969537

2017

Evaluation of Oxetan-3-ol, Thietan-3-ol, and Derivatives Thereof as Bioisosteres of the Carboxylic Acid Functional Group.
Evaluation of Oxetan-3-ol, Thietan-3-ol, and Derivatives Thereof as Bioisosteres of the Carboxylic Acid Functional Group.
Pierrik Lassalas, Killian Oukoloff, Vishruti Makani, Michael James, Van Tran, …, Virginia M-Y Lee, Marisa C Kozlowski, Amos B Smith, Kurt R Brunden, Carlo Ballatore
ACS medicinal chemistry letters  ·  05 Jul 2017  ·  pmid:28835803
Multitargeted Imidazoles: Potential Therapeutic Leads for Alzheimer s and Other Neurodegenerative Diseases.
Multitargeted Imidazoles: Potential Therapeutic Leads for Alzheimer's and Other Neurodegenerative Diseases.
Anne-Sophie Cornec, Ludovica Monti, Jane Kovalevich, Vishruti Makani, Michael J James, …, Virginia M-Y Lee, John Q Trojanowski, Amos B Smith, Kurt R Brunden, Carlo Ballatore
Journal of medicinal chemistry  ·  08 Jun 2017  ·  pmid:28530811

2016

Evaluation of the analgesic effect of 4-anilidopiperidine scaffold containing ureas and carbamates.
Evaluation of the analgesic effect of 4-anilidopiperidine scaffold containing ureas and carbamates.
Ludovica Monti, Azzurra Stefanucci, Stefano Pieretti, Francesca Marzoli, Lorenzo Fidanza, …, Anna I Erdei, Reza Samavati, Szabolcs Dvorácskó, Csaba Tömböly, Ettore Novellino
Journal of enzyme inhibition and medicinal chemistry  ·  11 Apr 2016  ·  pmid:27063555
Arylboronic acids as dual-action FAAH and TRPV1 ligands.
Arylboronic acids as dual-action FAAH and TRPV1 ligands.
Enrico Morera, Vincenzo Di Marzo, Ludovica Monti, Marco Allarà, Aniello Schiano Moriello, Marianna Nalli, Giorgio Ortar, Luciano De Petrocellis
Bioorganic & medicinal chemistry letters  ·  25 Jan 2016  ·  pmid:26850005

2015

Discovery of 1,1 -Biphenyl-4-sulfonamides as a New Class of Potent and Selective Carbonic Anhydrase XIV Inhibitors.
Discovery of 1,1'-Biphenyl-4-sulfonamides as a New Class of Potent and Selective Carbonic Anhydrase XIV Inhibitors.
Giuseppe La Regina, Antonio Coluccia, Valeria Famiglini, Sveva Pelliccia, Ludovica Monti, …, Peiwen Pan, Seppo Parkkila, Claudiu T Supuran, Armando Rossello, Romano Silvestri
Journal of medicinal chemistry  ·  04 Nov 2015  ·  pmid:26497049
New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer.
New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer.
Giuseppe La Regina, Ruoli Bai, Antonio Coluccia, Valeria Famiglini, Sveva Pelliccia, …, Chiara Bigogno, Giulio Dondio, Ernest Hamel, Patrizia Lavia, Romano Silvestri
Journal of medicinal chemistry  ·  20 Jul 2015  ·  pmid:26132075