Matches in SemOpenAlex for { <https://semopenalex.org/work/W3157236941> ?p ?o ?g. }
- W3157236941 endingPage "113526" @default.
- W3157236941 startingPage "113526" @default.
- W3157236941 abstract "HDAC6 isoform selective inhibitors can be pursued as an alternative to pan-HDACs inhibitors due to their therapeutic effect and low toxicity. Efforts of the structure optimization of our previous compound 10c (IC50 = 4.4 nM) resulted in a new series of 3, 4-disubstituted-imidazolidine-2, 5-dione based HDAC6 inhibitors with better HDAC6 inhibitory activities and improved selectivities. The most potent compound 71 exhibited a low nanomolar HDAC6 inhibitory activity (IC50 = 2.1 nM) and showed 5545-fold, 5864-fold as well as 1638-fold selectivity relative to HDAC1, HDAC2 and HDAC8, respectively. Western blot analysis further confirmed that compound 71 selectively increased the acetylation level of α-tubulin without affecting histone H3. Moreover, compound 71 also possesses good properties in term of caspase-3 activation, apoptosis induction, anti-proliferative activity, cytotoxicity and plasma stability. Therefore, compound 71 can be applied in cancer therapy or used as a lead compound to develop more potent HDAC6 selective inhibitor." @default.
- W3157236941 created "2021-05-10" @default.
- W3157236941 creator A5006999939 @default.
- W3157236941 creator A5011352874 @default.
- W3157236941 creator A5013861294 @default.
- W3157236941 creator A5022242605 @default.
- W3157236941 creator A5038166418 @default.
- W3157236941 creator A5060898939 @default.
- W3157236941 creator A5080780781 @default.
- W3157236941 date "2021-10-01" @default.
- W3157236941 modified "2023-10-15" @default.
- W3157236941 title "Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors" @default.
- W3157236941 cites W1943317445 @default.
- W3157236941 cites W1972149587 @default.
- W3157236941 cites W1995150044 @default.
- W3157236941 cites W2018950938 @default.
- W3157236941 cites W2034614265 @default.
- W3157236941 cites W2078211225 @default.
- W3157236941 cites W2081094284 @default.
- W3157236941 cites W2084893501 @default.
- W3157236941 cites W2087966689 @default.
- W3157236941 cites W2118335184 @default.
- W3157236941 cites W2122701468 @default.
- W3157236941 cites W2128986224 @default.
- W3157236941 cites W2156712995 @default.
- W3157236941 cites W2162787110 @default.
- W3157236941 cites W2165638033 @default.
- W3157236941 cites W2176988486 @default.
- W3157236941 cites W2255564941 @default.
- W3157236941 cites W2276640786 @default.
- W3157236941 cites W2404368222 @default.
- W3157236941 cites W2511667040 @default.
- W3157236941 cites W2529259746 @default.
- W3157236941 cites W2593904759 @default.
- W3157236941 cites W2604286547 @default.
- W3157236941 cites W2611454845 @default.
- W3157236941 cites W2734080602 @default.
- W3157236941 cites W2734610696 @default.
- W3157236941 cites W2761494335 @default.
- W3157236941 cites W2769759747 @default.
- W3157236941 cites W2803560272 @default.
- W3157236941 cites W2902799643 @default.
- W3157236941 cites W2953409632 @default.
- W3157236941 cites W3039236515 @default.
- W3157236941 cites W3127412029 @default.
- W3157236941 doi "https://doi.org/10.1016/j.ejmech.2021.113526" @default.
- W3157236941 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/33992929" @default.
- W3157236941 hasPublicationYear "2021" @default.
- W3157236941 type Work @default.
- W3157236941 sameAs 3157236941 @default.
- W3157236941 citedByCount "7" @default.
- W3157236941 countsByYear W31572369412022 @default.
- W3157236941 countsByYear W31572369412023 @default.
- W3157236941 crossrefType "journal-article" @default.
- W3157236941 hasAuthorship W3157236941A5006999939 @default.
- W3157236941 hasAuthorship W3157236941A5011352874 @default.
- W3157236941 hasAuthorship W3157236941A5013861294 @default.
- W3157236941 hasAuthorship W3157236941A5022242605 @default.
- W3157236941 hasAuthorship W3157236941A5038166418 @default.
- W3157236941 hasAuthorship W3157236941A5060898939 @default.
- W3157236941 hasAuthorship W3157236941A5080780781 @default.
- W3157236941 hasConcept C104317684 @default.
- W3157236941 hasConcept C109316439 @default.
- W3157236941 hasConcept C118792377 @default.
- W3157236941 hasConcept C119157956 @default.
- W3157236941 hasConcept C161790260 @default.
- W3157236941 hasConcept C185592680 @default.
- W3157236941 hasConcept C202751555 @default.
- W3157236941 hasConcept C23681527 @default.
- W3157236941 hasConcept C25737173 @default.
- W3157236941 hasConcept C2776775700 @default.
- W3157236941 hasConcept C2777752112 @default.
- W3157236941 hasConcept C2777752497 @default.
- W3157236941 hasConcept C2778305200 @default.
- W3157236941 hasConcept C55493867 @default.
- W3157236941 hasConcept C56428682 @default.
- W3157236941 hasConcept C64927066 @default.
- W3157236941 hasConcept C71240020 @default.
- W3157236941 hasConcept C71924100 @default.
- W3157236941 hasConcept C85240754 @default.
- W3157236941 hasConcept C98274493 @default.
- W3157236941 hasConceptScore W3157236941C104317684 @default.
- W3157236941 hasConceptScore W3157236941C109316439 @default.
- W3157236941 hasConceptScore W3157236941C118792377 @default.
- W3157236941 hasConceptScore W3157236941C119157956 @default.
- W3157236941 hasConceptScore W3157236941C161790260 @default.
- W3157236941 hasConceptScore W3157236941C185592680 @default.
- W3157236941 hasConceptScore W3157236941C202751555 @default.
- W3157236941 hasConceptScore W3157236941C23681527 @default.
- W3157236941 hasConceptScore W3157236941C25737173 @default.
- W3157236941 hasConceptScore W3157236941C2776775700 @default.
- W3157236941 hasConceptScore W3157236941C2777752112 @default.
- W3157236941 hasConceptScore W3157236941C2777752497 @default.
- W3157236941 hasConceptScore W3157236941C2778305200 @default.
- W3157236941 hasConceptScore W3157236941C55493867 @default.
- W3157236941 hasConceptScore W3157236941C56428682 @default.
- W3157236941 hasConceptScore W3157236941C64927066 @default.
- W3157236941 hasConceptScore W3157236941C71240020 @default.