Matches in SemOpenAlex for { <https://semopenalex.org/work/W2020163306> ?p ?o ?g. }
- W2020163306 endingPage "1468" @default.
- W2020163306 startingPage "1464" @default.
- W2020163306 abstract "Aldo-keto reductase 1C3 (AKR1C3) also known as type 5 17β-hydroxysteroid dehydrogenase has been implicated as one of the key enzymes driving the elevated intratumoral androgen levels observed in castrate resistant prostate cancer (CRPC). AKR1C3 inhibition therefore presents a rational approach to managing CRPC. Inhibitors should be selective for AKR1C3 over other AKR1C enzymes involved in androgen metabolism. We have synthesized 2-, 3-, and 4-(phenylamino)benzoic acids and identified 3-(phenylamino)benzoic acids that have nanomolar affinity and exhibit over 200-fold selectivity for AKR1C3 versus other AKR1C isoforms. The AKR1C3 inhibitory potency of the 4'-substituted 3-(phenylamino)benzoic acids shows a linear correlation with both electronic effects of substituents and the pK(a) of the carboxylic acid and secondary amine groups, which are interdependent. These compounds may be useful in treatment and/or prevention of CRPC as well as understanding the role of AKR1C3 in endocrinology." @default.
- W2020163306 created "2016-06-24" @default.
- W2020163306 creator A5003915964 @default.
- W2020163306 creator A5019174025 @default.
- W2020163306 creator A5058273955 @default.
- W2020163306 creator A5059737908 @default.
- W2020163306 creator A5061938264 @default.
- W2020163306 creator A5066957020 @default.
- W2020163306 date "2011-03-01" @default.
- W2020163306 modified "2023-09-27" @default.
- W2020163306 title "Discovery of substituted 3-(phenylamino)benzoic acids as potent and selective inhibitors of type 5 17β-hydroxysteroid dehydrogenase (AKR1C3)" @default.
- W2020163306 cites W1789755874 @default.
- W2020163306 cites W1966939483 @default.
- W2020163306 cites W1969888593 @default.
- W2020163306 cites W1986420914 @default.
- W2020163306 cites W1995093170 @default.
- W2020163306 cites W2000207142 @default.
- W2020163306 cites W2005674716 @default.
- W2020163306 cites W2006746802 @default.
- W2020163306 cites W2010311152 @default.
- W2020163306 cites W2011462808 @default.
- W2020163306 cites W2017896209 @default.
- W2020163306 cites W2032925662 @default.
- W2020163306 cites W2037479280 @default.
- W2020163306 cites W2045040068 @default.
- W2020163306 cites W2062949189 @default.
- W2020163306 cites W2066518128 @default.
- W2020163306 cites W2077301757 @default.
- W2020163306 cites W2091149475 @default.
- W2020163306 cites W2099477169 @default.
- W2020163306 cites W2101605468 @default.
- W2020163306 cites W2101606728 @default.
- W2020163306 cites W2116458141 @default.
- W2020163306 cites W2125139539 @default.
- W2020163306 cites W2130690545 @default.
- W2020163306 cites W2136750233 @default.
- W2020163306 cites W2138873293 @default.
- W2020163306 cites W2141569270 @default.
- W2020163306 cites W2150609534 @default.
- W2020163306 cites W2158734599 @default.
- W2020163306 cites W2165823301 @default.
- W2020163306 cites W2167749314 @default.
- W2020163306 cites W2171041379 @default.
- W2020163306 cites W2171585055 @default.
- W2020163306 cites W2412673684 @default.
- W2020163306 cites W4213037422 @default.
- W2020163306 cites W4250779219 @default.
- W2020163306 doi "https://doi.org/10.1016/j.bmcl.2011.01.010" @default.
- W2020163306 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3057412" @default.
- W2020163306 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/21277203" @default.
- W2020163306 hasPublicationYear "2011" @default.
- W2020163306 type Work @default.
- W2020163306 sameAs 2020163306 @default.
- W2020163306 citedByCount "40" @default.
- W2020163306 countsByYear W20201633062012 @default.
- W2020163306 countsByYear W20201633062013 @default.
- W2020163306 countsByYear W20201633062014 @default.
- W2020163306 countsByYear W20201633062015 @default.
- W2020163306 countsByYear W20201633062016 @default.
- W2020163306 countsByYear W20201633062017 @default.
- W2020163306 countsByYear W20201633062018 @default.
- W2020163306 countsByYear W20201633062019 @default.
- W2020163306 countsByYear W20201633062020 @default.
- W2020163306 countsByYear W20201633062022 @default.
- W2020163306 countsByYear W20201633062023 @default.
- W2020163306 crossrefType "journal-article" @default.
- W2020163306 hasAuthorship W2020163306A5003915964 @default.
- W2020163306 hasAuthorship W2020163306A5019174025 @default.
- W2020163306 hasAuthorship W2020163306A5058273955 @default.
- W2020163306 hasAuthorship W2020163306A5059737908 @default.
- W2020163306 hasAuthorship W2020163306A5061938264 @default.
- W2020163306 hasAuthorship W2020163306A5066957020 @default.
- W2020163306 hasBestOaLocation W20201633062 @default.
- W2020163306 hasConcept C118792377 @default.
- W2020163306 hasConcept C161790260 @default.
- W2020163306 hasConcept C181199279 @default.
- W2020163306 hasConcept C185592680 @default.
- W2020163306 hasConcept C202751555 @default.
- W2020163306 hasConcept C2776317432 @default.
- W2020163306 hasConcept C2777752497 @default.
- W2020163306 hasConcept C2777911890 @default.
- W2020163306 hasConcept C2778844314 @default.
- W2020163306 hasConcept C2781067048 @default.
- W2020163306 hasConcept C55493867 @default.
- W2020163306 hasConcept C57992300 @default.
- W2020163306 hasConcept C71240020 @default.
- W2020163306 hasConcept C71315377 @default.
- W2020163306 hasConceptScore W2020163306C118792377 @default.
- W2020163306 hasConceptScore W2020163306C161790260 @default.
- W2020163306 hasConceptScore W2020163306C181199279 @default.
- W2020163306 hasConceptScore W2020163306C185592680 @default.
- W2020163306 hasConceptScore W2020163306C202751555 @default.
- W2020163306 hasConceptScore W2020163306C2776317432 @default.
- W2020163306 hasConceptScore W2020163306C2777752497 @default.
- W2020163306 hasConceptScore W2020163306C2777911890 @default.
- W2020163306 hasConceptScore W2020163306C2778844314 @default.
- W2020163306 hasConceptScore W2020163306C2781067048 @default.
- W2020163306 hasConceptScore W2020163306C55493867 @default.