FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2893986378> ?p ?o ?g. }

• W2893986378 abstract "17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) is a promising therapeutic target known to play a pivotal role in the progression of estrogen-dependent diseases such as breast cancer, and endometriosis. This enzyme is responsible for the last step in the biosynthesis of the most potent estrogen, estradiol (E2) and its inhibition would prevent the growth of estrogen-sensitive tumors. Based on molecular modeling with docking experiments, we identified two promising C3-oxiranyl/oxiranylmethyl-estrane derivatives that would bind competitively and irreversibly in the catalytic site of 17β-HSD1. They have been synthesized in a short and efficient route and their inhibitory activities over 17β-HSD1 have been assessed by an enzymatic assay. Compound 15, with an oxiranylmethyl group at position C3, was more likely to bind the catalytic site and showed an interesting, but weak, inhibitory activity with an IC50 value of 1.3 µM (for the reduction of estrone into E2 in T-47D cells). Compound 11, with an oxiranyl at position C3, produced a lower inhibition rate, and the IC50 value cannot be determined. When tested in estrogen-sensitive T-47D cells, both compounds were also slightly estrogenic, although much less than the estrogenic hormone E2." @default.
• W2893986378 created "2018-10-05" @default.
• W2893986378 creator A5004302458 @default.
• W2893986378 creator A5034301403 @default.
• W2893986378 creator A5035454604 @default.
• W2893986378 creator A5040744081 @default.
• W2893986378 creator A5044109379 @default.
• W2893986378 creator A5046826793 @default.
• W2893986378 date "2018-12-01" @default.
• W2893986378 modified "2023-09-29" @default.
• W2893986378 title "Chemical synthesis of C3-oxiranyl/oxiranylmethyl-estrane derivatives targeted by molecular modeling and tested as potential inhibitors of 17β-hydroxysteroid dehydrogenase type 1" @default.
• W2893986378 cites W1970075541 @default.
• W2893986378 cites W1976691013 @default.
• W2893986378 cites W2003460765 @default.
• W2893986378 cites W2006746802 @default.
• W2893986378 cites W2022118060 @default.
• W2893986378 cites W2025397617 @default.
• W2893986378 cites W2030761095 @default.
• W2893986378 cites W2043360293 @default.
• W2893986378 cites W2050847082 @default.
• W2893986378 cites W2076068021 @default.
• W2893986378 cites W2081922333 @default.
• W2893986378 cites W2084005417 @default.
• W2893986378 cites W2085785716 @default.
• W2893986378 cites W2091153850 @default.
• W2893986378 cites W2095408194 @default.
• W2893986378 cites W2095569462 @default.
• W2893986378 cites W2097678737 @default.
• W2893986378 cites W2136281716 @default.
• W2893986378 cites W2145735545 @default.
• W2893986378 cites W2151970029 @default.
• W2893986378 cites W2317201616 @default.
• W2893986378 cites W2326684565 @default.
• W2893986378 cites W2412673684 @default.
• W2893986378 cites W2539722882 @default.
• W2893986378 cites W2591495114 @default.
• W2893986378 cites W2743803136 @default.
• W2893986378 cites W2771931566 @default.
• W2893986378 cites W3025410850 @default.
• W2893986378 doi "https://doi.org/10.1016/j.steroids.2018.09.009" @default.
• W2893986378 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30273695" @default.
• W2893986378 hasPublicationYear "2018" @default.
• W2893986378 type Work @default.
• W2893986378 sameAs 2893986378 @default.
• W2893986378 citedByCount "2" @default.
• W2893986378 countsByYear W28939863782020 @default.
• W2893986378 countsByYear W28939863782022 @default.
• W2893986378 crossrefType "journal-article" @default.
• W2893986378 hasAuthorship W2893986378A5004302458 @default.
• W2893986378 hasAuthorship W2893986378A5034301403 @default.
• W2893986378 hasAuthorship W2893986378A5035454604 @default.
• W2893986378 hasAuthorship W2893986378A5040744081 @default.
• W2893986378 hasAuthorship W2893986378A5044109379 @default.
• W2893986378 hasAuthorship W2893986378A5046826793 @default.
• W2893986378 hasConcept C134018914 @default.
• W2893986378 hasConcept C159110408 @default.
• W2893986378 hasConcept C181199279 @default.
• W2893986378 hasConcept C185592680 @default.
• W2893986378 hasConcept C202751555 @default.
• W2893986378 hasConcept C2776317432 @default.
• W2893986378 hasConcept C2777164284 @default.
• W2893986378 hasConcept C2777752497 @default.
• W2893986378 hasConcept C2778656385 @default.
• W2893986378 hasConcept C2781067048 @default.
• W2893986378 hasConcept C41183919 @default.
• W2893986378 hasConcept C41685203 @default.
• W2893986378 hasConcept C55493867 @default.
• W2893986378 hasConcept C71240020 @default.
• W2893986378 hasConcept C71315377 @default.
• W2893986378 hasConcept C71924100 @default.
• W2893986378 hasConcept C86803240 @default.
• W2893986378 hasConcept C98274493 @default.
• W2893986378 hasConceptScore W2893986378C134018914 @default.
• W2893986378 hasConceptScore W2893986378C159110408 @default.
• W2893986378 hasConceptScore W2893986378C181199279 @default.
• W2893986378 hasConceptScore W2893986378C185592680 @default.
• W2893986378 hasConceptScore W2893986378C202751555 @default.
• W2893986378 hasConceptScore W2893986378C2776317432 @default.
• W2893986378 hasConceptScore W2893986378C2777164284 @default.
• W2893986378 hasConceptScore W2893986378C2777752497 @default.
• W2893986378 hasConceptScore W2893986378C2778656385 @default.
• W2893986378 hasConceptScore W2893986378C2781067048 @default.
• W2893986378 hasConceptScore W2893986378C41183919 @default.
• W2893986378 hasConceptScore W2893986378C41685203 @default.
• W2893986378 hasConceptScore W2893986378C55493867 @default.
• W2893986378 hasConceptScore W2893986378C71240020 @default.
• W2893986378 hasConceptScore W2893986378C71315377 @default.
• W2893986378 hasConceptScore W2893986378C71924100 @default.
• W2893986378 hasConceptScore W2893986378C86803240 @default.
• W2893986378 hasConceptScore W2893986378C98274493 @default.
• W2893986378 hasFunder F4320322675 @default.
• W2893986378 hasLocation W28939863781 @default.
• W2893986378 hasLocation W28939863782 @default.
• W2893986378 hasOpenAccess W2893986378 @default.
• W2893986378 hasPrimaryLocation W28939863781 @default.
• W2893986378 hasRelatedWork W1182003361 @default.
• W2893986378 hasRelatedWork W2006726335 @default.
• W2893986378 hasRelatedWork W2010508685 @default.
• W2893986378 hasRelatedWork W2028916314 @default.
• W2893986378 hasRelatedWork W2032332320 @default.

• next