Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia MB Pappalardi, K Keenan, M Cockerill, WA Kellner, A Stowell, C Sherk, ... Nature cancer 2 (10), 1002-1017, 2021 | 163 | 2021 |
In vitro and in vivo induction of fetal hemoglobin with a reversible and selective DNMT1 inhibitor AG Gilmartin, A Groy, ER Gore, C Atkins, ER Long, MN Montoute, Z Wu, ... Haematologica 106 (7), 1979, 2021 | 48 | 2021 |
Cyclopropyl carboxamides, a chemically novel class of antimalarial agents identified in a phenotypic screen LM Sanz, MB Jiménez-Díaz, B Crespo, C De-Cozar, MJ Almela, ... Antimicrobial agents and chemotherapy 55 (12), 5740-5745, 2011 | 39 | 2011 |
Cyclopropyl carboxamides: a new oral antimalarial series derived from the Tres Cantos anti-malarial set (TCAMS) L Rueda, I Castellote, J Castro-Pichel, MJ Chaparro, JC de la Rosa, ... ACS Medicinal Chemistry Letters 2 (11), 840-844, 2011 | 38 | 2011 |
Development of Chemical Entities Endowed with Potent Fast-Killing Properties against Plasmodium falciparum Malaria Parasites AN Matralis, A Malik, M Penzo, I Moreno, MJ Almela, I Camino, B Crespo, ... Journal of medicinal chemistry 62 (20), 9217-9235, 2019 | 34 | 2019 |
Structural characterization of dicyanopyridine containing DNMT1-selective, non-nucleoside inhibitors JR Horton, S Pathuri, K Wong, R Ren, L Rueda, DT Fosbenner, ... Structure 30 (6), 793-802. e5, 2022 | 19 | 2022 |
Case study of small molecules as antimalarials: 2-amino-1-phenylethanol (APE) derivatives MJ Chaparro, J Vidal, I Angulo-Barturen, JM Bueno, J Burrows, ... ACS Medicinal Chemistry Letters 5 (6), 657-661, 2014 | 13 | 2014 |
The discovery of novel antimalarial aminoxadiazoles as a promising nonendoperoxide scaffold E Sandoval, MJ Lafuente-Monasterio, MJ Almela, P Castaneda, ... Journal of medicinal chemistry 60 (16), 6880-6896, 2017 | 12 | 2017 |
Discovery of selective, noncovalent small molecule inhibitors of DNMT1 as an alternative to traditional DNA hypomethylating agents MB Pappalardi, M Cockerill, JL Handler, A Stowell, K Keenan, CS Sherk, ... Cancer Research 78 (13_Supplement), 2994-2994, 2018 | 9 | 2018 |
A decade of malaria phenotypic screenings: Key lessons on the discovery and development of new antimalarial drugs E Fernández, MI Castellote, MJ Chaparro, B Díaz, J Fernández, M Gordo, ... Annual reports in medicinal chemistry 53, 1-23, 2019 | 5 | 2019 |
Substituted pyridines as inhibitors of DNMT1 ND Adams, AB Benowitz, MLR BENEDE, KA Evans, DT Fosbenner, ... US Patent 10,975,056, 2021 | 1 | 2021 |
Substituted pyridines as inhibitors of DNMT1 ND ADAMS, AB Benowitz, MLR BENEDE, KA Evans, DT Fosbenner, ... | 1 | 2017 |
Design and synthesis of aminopyridine containing biaryls reducing c-MYC protein levels in cells CN Di Marco, L Terrell, R Sanchez, L Rueda, L Shuster, EN Nartey, ... Bioorganic & Medicinal Chemistry Letters 92, 129385, 2023 | | 2023 |
Compuestos quimicos ND Adams, AB Benowitz, MLR Benede, KA Evans, DT Fosbenner, ... | | 2019 |
Substituted pyridines as inhibitors of dnmt1 ND ADAMS, AB Benowitz, MLR BENEDE, KA Evans, DT Fosbenner, ... | | 2019 |
Discovery of a selective, non-nucleoside small molecule inhibitor of DNA methyltransferase 1 (DNMT1) B King, A Benowitz, J Briand, C Burt, C Carpenter, M Cockerill, K Evans, ... ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY 256, 2018 | | 2018 |
SUBSTITUTED PYRIDINES AS INHIBITORS OF DNMT1 ML RUEDA BENEDE, ND (US). ADAMS, AB (US). BENOWITZ, ... | | 2017 |
SUBSTITUTED PYRIDINES AS INHIBITORS OF DNMT1 ML RUEDA BENEDE, ND (US). ADAMS, AB (US). BENOWITZ, ... US Patent WO/2017/216,726, 2017 | | 2017 |
NEW EFFORTS AIMED AT REPLACING ACTS: THE IDENTIFICATION OF NOVEL, DRUG-LIKE, AND FAST-ACTING ANTIMALARIAL COMPOUNDS FROM A PHENOTYPIC SCREENING L Rueda AMERICAN JOURNAL OF TROPICAL MEDICINE AND HYGIENE 93 (4), 295-295, 2015 | | 2015 |
Scaffold based analytics enabling hit to lead decisions by visualizing chemical series linked across large datasets ACS Conference, 2015 | | 2015 |