dc.contributor.author | Llona-Minguez, S | |
dc.contributor.author | H?glund, A | |
dc.contributor.author | Ghassemian, A | |
dc.contributor.author | Desroses, M | |
dc.contributor.author | Calder?n-Monta?o, JM | |
dc.contributor.author | Burgos Mor?n, E | |
dc.contributor.author | Valerie, NCK | |
dc.contributor.author | Wiita, E | |
dc.contributor.author | Alml?f, I | |
dc.contributor.author | Koolmeister, T | |
dc.contributor.author | Mateus, A | |
dc.contributor.author | Cazares-K?rner, C | |
dc.contributor.author | Sanjiv, K | |
dc.contributor.author | Homan, E | |
dc.contributor.author | Loseva, O | |
dc.contributor.author | Baranczewski, P | |
dc.contributor.author | Darabi, M | |
dc.contributor.author | Mehdizadeh, A | |
dc.contributor.author | Fayezi, S | |
dc.contributor.author | Jemth, AS | |
dc.contributor.author | Warpman Berglund, U | |
dc.contributor.author | Sigmundsson, K | |
dc.contributor.author | Lundb?ck, T | |
dc.contributor.author | Jenmalm Jensen, A | |
dc.contributor.author | Artursson, P | |
dc.contributor.author | Scobie, M | |
dc.contributor.author | Helleday, T | |
dc.date.accessioned | 2018-08-26T04:59:52Z | |
dc.date.available | 2018-08-26T04:59:52Z | |
dc.date.issued | 2017 | |
dc.identifier.uri | http://dspace.tbzmed.ac.ir:8080/xmlui/handle/123456789/38890 | |
dc.description.abstract | The dCTP pyrophosphatase 1 (dCTPase) is a nucleotide pool "housekeeping" enzyme responsible for the catabolism of canonical and noncanonical nucleoside triphosphates (dNTPs) and has been associated with cancer progression and cancer cell stemness. We have identified a series of piperazin-1-ylpyridazines as a new class of potent dCTPase inhibitors. Lead compounds increase dCTPase thermal and protease stability, display outstanding selectivity over related enzymes and synergize with a cytidine analogue against leukemic cells. This new class of dCTPase inhibitors lays the first stone toward the development of drug-like probes for the dCTPase enzyme. | |
dc.language.iso | English | |
dc.relation.ispartof | Journal of medicinal chemistry | |
dc.subject | Antineoplastic Agents | |
dc.subject | Cell Line, Tumor | |
dc.subject | Cell Survival | |
dc.subject | Enzyme Inhibitors | |
dc.subject | Humans | |
dc.subject | Leukemia | |
dc.subject | Molecular Docking Simulation | |
dc.subject | Piperazines | |
dc.subject | Pyridazines | |
dc.subject | Pyrophosphatases | |
dc.title | Piperazin-1-ylpyridazine Derivatives Are a Novel Class of Human dCTP Pyrophosphatase 1 Inhibitors. | |
dc.type | article | |
dc.citation.volume | 60 | |
dc.citation.issue | 10 | |
dc.citation.spage | 4279 | |
dc.citation.epage | 4292 | |
dc.citation.index | Pubmed | |
dc.identifier.DOI | https://doi.org/10.1021/acs.jmedchem.7b00182 | |