Matches in SemOpenAlex for { <https://semopenalex.org/work/W2724796663> ?p ?o ?g. }
- W2724796663 endingPage "6527" @default.
- W2724796663 startingPage "6516" @default.
- W2724796663 abstract "Aberrant signaling of the FGF/FGFR pathway occurs frequently in cancers and is an oncogenic driver in many solid tumors. Clinical validation of FGFR as a therapeutic target has been demonstrated in bladder, liver, lung, breast, and gastric cancers. Our goal was to develop an irreversible covalent inhibitor of FGFR1-4 for use in oncology indications. An irreversible covalent binding mechanism imparts many desirable pharmacological benefits including high potency, selectivity, and prolonged target inhibition. Herein we report the structure-based design, medicinal chemistry optimization, and unique ADME assays of our irreversible covalent drug discovery program which culminated in the discovery of compound 34 (PRN1371), a highly selective and potent FGFR1-4 inhibitor." @default.
- W2724796663 created "2017-07-14" @default.
- W2724796663 creator A5003039440 @default.
- W2724796663 creator A5007039813 @default.
- W2724796663 creator A5028513468 @default.
- W2724796663 creator A5030442443 @default.
- W2724796663 creator A5032842967 @default.
- W2724796663 creator A5033606709 @default.
- W2724796663 creator A5034351013 @default.
- W2724796663 creator A5039359774 @default.
- W2724796663 creator A5041633622 @default.
- W2724796663 creator A5056730171 @default.
- W2724796663 creator A5064779408 @default.
- W2724796663 creator A5071916490 @default.
- W2724796663 creator A5071966738 @default.
- W2724796663 creator A5072175892 @default.
- W2724796663 creator A5077081162 @default.
- W2724796663 creator A5080764781 @default.
- W2724796663 date "2017-07-25" @default.
- W2724796663 modified "2023-10-14" @default.
- W2724796663 title "Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-<i>d</i>]pyrimidin-7(8<i>H</i>)-one (PRN1371) for the Treatment of Solid Tumors" @default.
- W2724796663 cites W1526377515 @default.
- W2724796663 cites W1826437673 @default.
- W2724796663 cites W1960850967 @default.
- W2724796663 cites W1963721433 @default.
- W2724796663 cites W1963826141 @default.
- W2724796663 cites W1968177654 @default.
- W2724796663 cites W1971340381 @default.
- W2724796663 cites W1974519242 @default.
- W2724796663 cites W1987343069 @default.
- W2724796663 cites W1988476050 @default.
- W2724796663 cites W2010993054 @default.
- W2724796663 cites W2015786768 @default.
- W2724796663 cites W2019050932 @default.
- W2724796663 cites W2019711215 @default.
- W2724796663 cites W2021220203 @default.
- W2724796663 cites W2026415908 @default.
- W2724796663 cites W2027239974 @default.
- W2724796663 cites W2047494200 @default.
- W2724796663 cites W2051766214 @default.
- W2724796663 cites W2057079741 @default.
- W2724796663 cites W2058570288 @default.
- W2724796663 cites W2058800522 @default.
- W2724796663 cites W2068473321 @default.
- W2724796663 cites W2071648775 @default.
- W2724796663 cites W2093090488 @default.
- W2724796663 cites W2096950509 @default.
- W2724796663 cites W2097036454 @default.
- W2724796663 cites W2104858248 @default.
- W2724796663 cites W2124560610 @default.
- W2724796663 cites W2134917212 @default.
- W2724796663 cites W2138297714 @default.
- W2724796663 cites W2152905269 @default.
- W2724796663 cites W2161608625 @default.
- W2724796663 cites W2161730969 @default.
- W2724796663 cites W2169752008 @default.
- W2724796663 cites W2170454377 @default.
- W2724796663 cites W2232826249 @default.
- W2724796663 cites W2322586343 @default.
- W2724796663 cites W2465965969 @default.
- W2724796663 cites W2486669929 @default.
- W2724796663 cites W2568666199 @default.
- W2724796663 cites W4251068168 @default.
- W2724796663 doi "https://doi.org/10.1021/acs.jmedchem.7b00360" @default.
- W2724796663 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/28665128" @default.
- W2724796663 hasPublicationYear "2017" @default.
- W2724796663 type Work @default.
- W2724796663 sameAs 2724796663 @default.
- W2724796663 citedByCount "75" @default.
- W2724796663 countsByYear W27247966632017 @default.
- W2724796663 countsByYear W27247966632018 @default.
- W2724796663 countsByYear W27247966632019 @default.
- W2724796663 countsByYear W27247966632020 @default.
- W2724796663 countsByYear W27247966632021 @default.
- W2724796663 countsByYear W27247966632022 @default.
- W2724796663 countsByYear W27247966632023 @default.
- W2724796663 crossrefType "journal-article" @default.
- W2724796663 hasAuthorship W2724796663A5003039440 @default.
- W2724796663 hasAuthorship W2724796663A5007039813 @default.
- W2724796663 hasAuthorship W2724796663A5028513468 @default.
- W2724796663 hasAuthorship W2724796663A5030442443 @default.
- W2724796663 hasAuthorship W2724796663A5032842967 @default.
- W2724796663 hasAuthorship W2724796663A5033606709 @default.
- W2724796663 hasAuthorship W2724796663A5034351013 @default.
- W2724796663 hasAuthorship W2724796663A5039359774 @default.
- W2724796663 hasAuthorship W2724796663A5041633622 @default.
- W2724796663 hasAuthorship W2724796663A5056730171 @default.
- W2724796663 hasAuthorship W2724796663A5064779408 @default.
- W2724796663 hasAuthorship W2724796663A5071916490 @default.
- W2724796663 hasAuthorship W2724796663A5071966738 @default.
- W2724796663 hasAuthorship W2724796663A5072175892 @default.
- W2724796663 hasAuthorship W2724796663A5077081162 @default.
- W2724796663 hasAuthorship W2724796663A5080764781 @default.
- W2724796663 hasBestOaLocation W27247966631 @default.
- W2724796663 hasConcept C178790620 @default.
- W2724796663 hasConcept C180577832 @default.
- W2724796663 hasConcept C185592680 @default.
- W2724796663 hasConcept C202751555 @default.