FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W4207074559> ?p ?o ?g. }

• W4207074559 endingPage "105596" @default.
• W4207074559 startingPage "105596" @default.
• W4207074559 abstract "Histone lysine specific demethylase 1 (LSD1) is a promising new therapeutic target for cancer therapy. Following the work on the discovery of natural LSD1 inhibitor higenamine, we herein performed further structure-based design, synthesis, and extensive structure-activity relationship (SAR) studies, affording structurally new spirooxindole derivatives. Particularly, FY-56 was identified to be a highly potent LSD1 inhibitor (IC50 = 42 nM) and showed high selectivity over monoamine oxidases (MAO-A/B). Mechanistic studies showed that FY-56 moderately inhibited the proliferation and clone formation of leukemia cells, induced H3K4me1/2 accumulation and p53 activation as well as reduced the mRNA levels of the transcription factors HOXA9 and MEIS1. Meanwhile, FY-56 induced differentiation of MOLM-13 and MV4-11 cells, accompanied by an enhanced percentage of markers characteristic to differentiated macrophages and monocytes. Further in vivo studies showed that FY-56 obviously reduced the proportion of CD45+/CD33+ leukocytes in peripheral blood and spleen, and significantly prolonged the survival rate of mice. Collectively, FY-56 represents a structurally novel, highly potent and selective LSD1 inhibitor and exhibits therapeutic promise for AML treatment. The spirooxindole scaffold derived from FY-56 could be used to design structurally new LSD1 inhibitors for treating human diseases." @default.
• W4207074559 created "2022-01-26" @default.
• W4207074559 creator A5043063276 @default.
• W4207074559 creator A5048423176 @default.
• W4207074559 creator A5063343992 @default.
• W4207074559 creator A5070238579 @default.
• W4207074559 creator A5070685116 @default.
• W4207074559 creator A5079702764 @default.
• W4207074559 creator A5084507015 @default.
• W4207074559 date "2022-03-01" @default.
• W4207074559 modified "2023-10-11" @default.
• W4207074559 title "Discovery of natural product-like spirooxindole derivatives as highly potent and selective LSD1/KDM1A inhibitors for AML treatment" @default.
• W4207074559 cites W1954584384 @default.
• W4207074559 cites W2056903026 @default.
• W4207074559 cites W2072677280 @default.
• W4207074559 cites W2077530603 @default.
• W4207074559 cites W2088226047 @default.
• W4207074559 cites W2090982381 @default.
• W4207074559 cites W2104910696 @default.
• W4207074559 cites W2146317534 @default.
• W4207074559 cites W2147623802 @default.
• W4207074559 cites W2256742438 @default.
• W4207074559 cites W2296658645 @default.
• W4207074559 cites W2335573407 @default.
• W4207074559 cites W2509447756 @default.
• W4207074559 cites W2517571687 @default.
• W4207074559 cites W2536500264 @default.
• W4207074559 cites W2590056038 @default.
• W4207074559 cites W2736147637 @default.
• W4207074559 cites W2773791765 @default.
• W4207074559 cites W2794180511 @default.
• W4207074559 cites W2801437236 @default.
• W4207074559 cites W2883462188 @default.
• W4207074559 cites W2908449964 @default.
• W4207074559 cites W2949236218 @default.
• W4207074559 cites W2972310354 @default.
• W4207074559 cites W2980951622 @default.
• W4207074559 cites W2988094299 @default.
• W4207074559 cites W2993378407 @default.
• W4207074559 cites W3003667794 @default.
• W4207074559 cites W3011366455 @default.
• W4207074559 cites W3035878085 @default.
• W4207074559 cites W3092563979 @default.
• W4207074559 cites W3111400820 @default.
• W4207074559 cites W3127024116 @default.
• W4207074559 cites W3127639950 @default.
• W4207074559 cites W3130922855 @default.
• W4207074559 cites W4200397913 @default.
• W4207074559 cites W4212766227 @default.
• W4207074559 doi "https://doi.org/10.1016/j.bioorg.2022.105596" @default.
• W4207074559 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/35051709" @default.
• W4207074559 hasPublicationYear "2022" @default.
• W4207074559 type Work @default.
• W4207074559 citedByCount "13" @default.
• W4207074559 countsByYear W42070745592022 @default.
• W4207074559 countsByYear W42070745592023 @default.
• W4207074559 crossrefType "journal-article" @default.
• W4207074559 hasAuthorship W4207074559A5043063276 @default.
• W4207074559 hasAuthorship W4207074559A5048423176 @default.
• W4207074559 hasAuthorship W4207074559A5063343992 @default.
• W4207074559 hasAuthorship W4207074559A5070238579 @default.
• W4207074559 hasAuthorship W4207074559A5070685116 @default.
• W4207074559 hasAuthorship W4207074559A5079702764 @default.
• W4207074559 hasAuthorship W4207074559A5084507015 @default.
• W4207074559 hasConcept C104317684 @default.
• W4207074559 hasConcept C150903083 @default.
• W4207074559 hasConcept C185592680 @default.
• W4207074559 hasConcept C207001950 @default.
• W4207074559 hasConcept C2779396153 @default.
• W4207074559 hasConcept C2781364455 @default.
• W4207074559 hasConcept C502942594 @default.
• W4207074559 hasConcept C55493867 @default.
• W4207074559 hasConcept C64927066 @default.
• W4207074559 hasConcept C86803240 @default.
• W4207074559 hasConcept C98274493 @default.
• W4207074559 hasConceptScore W4207074559C104317684 @default.
• W4207074559 hasConceptScore W4207074559C150903083 @default.
• W4207074559 hasConceptScore W4207074559C185592680 @default.
• W4207074559 hasConceptScore W4207074559C207001950 @default.
• W4207074559 hasConceptScore W4207074559C2779396153 @default.
• W4207074559 hasConceptScore W4207074559C2781364455 @default.
• W4207074559 hasConceptScore W4207074559C502942594 @default.
• W4207074559 hasConceptScore W4207074559C55493867 @default.
• W4207074559 hasConceptScore W4207074559C64927066 @default.
• W4207074559 hasConceptScore W4207074559C86803240 @default.
• W4207074559 hasConceptScore W4207074559C98274493 @default.
• W4207074559 hasFunder F4320321001 @default.
• W4207074559 hasFunder F4320326279 @default.
• W4207074559 hasFunder F4320329227 @default.
• W4207074559 hasFunder F4320335563 @default.
• W4207074559 hasFunder F4320335981 @default.
• W4207074559 hasLocation W42070745591 @default.
• W4207074559 hasLocation W42070745592 @default.
• W4207074559 hasOpenAccess W4207074559 @default.
• W4207074559 hasPrimaryLocation W42070745591 @default.
• W4207074559 hasRelatedWork W1978564811 @default.
• W4207074559 hasRelatedWork W1990414540 @default.
• W4207074559 hasRelatedWork W1990453785 @default.

• next