Matches in SemOpenAlex for { <https://semopenalex.org/work/W2079461756> ?p ?o ?g. }
- W2079461756 endingPage "304" @default.
- W2079461756 startingPage "296" @default.
- W2079461756 abstract "The search for newer histone deacetylase (HDAC) inhibitors has attracted a great deal of interest of medicinal chemists worldwide, especially after the first HDAC inhibitor (Zolinza®, widely known as SAHA or Suberoylanilide hydroxamic acid) was approved by the FDA for the treatment of Tcell lymphoma in 2006. As a continuity of our ongoing research in this area, we designed and synthesized a series of 5-aryl-1,3,4-thiadiazole-based hydroxamic acids as analogues of SAHA and evaluated their biological activities. Most of the compounds in this series, e.g. compounds with 5-aryl moiety being 2- furfuryl (5a), 5-bromofuran-2-yl (5b), 5-methylfuran-2-yl (5c), thiophen-2-yl (5d), 5-methylthiophen-2-yl (5f) and pyridyl (5g-i), were found to have potent anticancer cytotoxicity with IC50 values of generally 5- to 10-fold lower than that of SAHA in 4 human cancer cell lines assayed. Those compounds with potent cytotoxicity were also found to have strong HDAC inhibition effects. Docking studies revealed that compounds 5a and 5d displayed high affinities towards HDAC2 and 8. Keywords: Histone deacetylase (HDAC) inhibitors, 5-aryl-1, 3, 4-thiadiazole, cytotoxicity, heterocycle." @default.
- W2079461756 created "2016-06-24" @default.
- W2079461756 creator A5000121767 @default.
- W2079461756 creator A5009903231 @default.
- W2079461756 creator A5011763720 @default.
- W2079461756 creator A5020344273 @default.
- W2079461756 creator A5037204409 @default.
- W2079461756 creator A5044779630 @default.
- W2079461756 creator A5046876658 @default.
- W2079461756 creator A5049032346 @default.
- W2079461756 creator A5051137028 @default.
- W2079461756 creator A5051589331 @default.
- W2079461756 creator A5065902177 @default.
- W2079461756 creator A5071093188 @default.
- W2079461756 creator A5084162116 @default.
- W2079461756 date "2015-03-31" @default.
- W2079461756 modified "2023-09-27" @default.
- W2079461756 title "5-Aryl-1,3,4-Thiadiazole-Based Hydroxamic Acids as Histone Deacetylase Inhibitors and Antitumor Agents: Synthesis, Bioevaluation and Docking Study" @default.
- W2079461756 cites W1493899251 @default.
- W2079461756 cites W1967434207 @default.
- W2079461756 cites W1971621147 @default.
- W2079461756 cites W1984947563 @default.
- W2079461756 cites W2021818563 @default.
- W2079461756 cites W2022285476 @default.
- W2079461756 cites W2029148944 @default.
- W2079461756 cites W2030517878 @default.
- W2079461756 cites W2075260362 @default.
- W2079461756 cites W2080265708 @default.
- W2079461756 cites W2107733280 @default.
- W2079461756 cites W2109689528 @default.
- W2079461756 cites W2114367386 @default.
- W2079461756 cites W2115593774 @default.
- W2079461756 cites W2134009718 @default.
- W2079461756 cites W2134967712 @default.
- W2079461756 cites W2135830745 @default.
- W2079461756 cites W2155759132 @default.
- W2079461756 cites W2162438863 @default.
- W2079461756 cites W2168607453 @default.
- W2079461756 doi "https://doi.org/10.2174/1573406410666140925153128" @default.
- W2079461756 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/25256241" @default.
- W2079461756 hasPublicationYear "2015" @default.
- W2079461756 type Work @default.
- W2079461756 sameAs 2079461756 @default.
- W2079461756 citedByCount "6" @default.
- W2079461756 countsByYear W20794617562017 @default.
- W2079461756 countsByYear W20794617562018 @default.
- W2079461756 countsByYear W20794617562019 @default.
- W2079461756 countsByYear W20794617562020 @default.
- W2079461756 countsByYear W20794617562022 @default.
- W2079461756 crossrefType "journal-article" @default.
- W2079461756 hasAuthorship W2079461756A5000121767 @default.
- W2079461756 hasAuthorship W2079461756A5009903231 @default.
- W2079461756 hasAuthorship W2079461756A5011763720 @default.
- W2079461756 hasAuthorship W2079461756A5020344273 @default.
- W2079461756 hasAuthorship W2079461756A5037204409 @default.
- W2079461756 hasAuthorship W2079461756A5044779630 @default.
- W2079461756 hasAuthorship W2079461756A5046876658 @default.
- W2079461756 hasAuthorship W2079461756A5049032346 @default.
- W2079461756 hasAuthorship W2079461756A5051137028 @default.
- W2079461756 hasAuthorship W2079461756A5051589331 @default.
- W2079461756 hasAuthorship W2079461756A5065902177 @default.
- W2079461756 hasAuthorship W2079461756A5071093188 @default.
- W2079461756 hasAuthorship W2079461756A5084162116 @default.
- W2079461756 hasConcept C104317684 @default.
- W2079461756 hasConcept C109316439 @default.
- W2079461756 hasConcept C159110408 @default.
- W2079461756 hasConcept C178790620 @default.
- W2079461756 hasConcept C185592680 @default.
- W2079461756 hasConcept C202751555 @default.
- W2079461756 hasConcept C21951064 @default.
- W2079461756 hasConcept C2776202225 @default.
- W2079461756 hasConcept C2776262904 @default.
- W2079461756 hasConcept C2776281265 @default.
- W2079461756 hasConcept C2776568683 @default.
- W2079461756 hasConcept C2778305200 @default.
- W2079461756 hasConcept C2780263894 @default.
- W2079461756 hasConcept C2781076698 @default.
- W2079461756 hasConcept C41685203 @default.
- W2079461756 hasConcept C55493867 @default.
- W2079461756 hasConcept C64927066 @default.
- W2079461756 hasConcept C71240020 @default.
- W2079461756 hasConcept C71723506 @default.
- W2079461756 hasConcept C71924100 @default.
- W2079461756 hasConcept C85240754 @default.
- W2079461756 hasConcept C86803240 @default.
- W2079461756 hasConcept C98274493 @default.
- W2079461756 hasConceptScore W2079461756C104317684 @default.
- W2079461756 hasConceptScore W2079461756C109316439 @default.
- W2079461756 hasConceptScore W2079461756C159110408 @default.
- W2079461756 hasConceptScore W2079461756C178790620 @default.
- W2079461756 hasConceptScore W2079461756C185592680 @default.
- W2079461756 hasConceptScore W2079461756C202751555 @default.
- W2079461756 hasConceptScore W2079461756C21951064 @default.
- W2079461756 hasConceptScore W2079461756C2776202225 @default.
- W2079461756 hasConceptScore W2079461756C2776262904 @default.
- W2079461756 hasConceptScore W2079461756C2776281265 @default.
- W2079461756 hasConceptScore W2079461756C2776568683 @default.
- W2079461756 hasConceptScore W2079461756C2778305200 @default.