Matches in SemOpenAlex for { <https://semopenalex.org/work/W3181348310> ?p ?o ?g. }
- W3181348310 endingPage "6763" @default.
- W3181348310 startingPage "6748" @default.
- W3181348310 abstract "Recent evidences highlight the usefulness of small molecule (Histone deacetylase 4) HDAC4 inhibitors in the several preclinical paradigms. Major toxicity and mutagenicity issues associated with hydroxamate HDAC inhibitors, stimulated us to develop potent non-hydroxamate inhibitors. In the present work a novel series of thiazolidinedione (TZD) derivatives with pyridine as cyclic linker and TZD ring as zinc binding group was designed and screened in a panel of isoenzymes of HDACs, wherein the most potent compounds exhibiting HDAC4 IC50-values<5 μM were 5 v, 5 w, 5 y and 5 z (IC50=4.2±1 μM, 0.75±0.03 μM, 4.9±0.5 and 2.3±0.5 μM, respectively). The docking studies displayed the unique binding mode of this series of compound at active site of HDAC4, wherein TZD ring was indicated as zinc binding group. Further, 5 w and 5 y were found as the most potent antiproliferative agent in lymphoblastic leukemia (CCRF-CEM) and breast cancer MDA-MB-231 cells. Compound 5 y was found to induce the apoptosis and DNA fragmentation of CEM cells. The western blotting analysis of 5 y also showed the presence of cleaved caspases supporting their apoptotic nature. Further, Class IIa (HDAC4) selectivity of 5 y was also supported by western blotting observations, wherein 5 y caused the accumulation of acetylated H3 but not of acetylated Tubulin. Thus, our findings endorse the further investigation of this series of compounds for their potential as targeted cancer therapeutic agents." @default.
- W3181348310 created "2021-07-19" @default.
- W3181348310 creator A5010725738 @default.
- W3181348310 creator A5016919711 @default.
- W3181348310 creator A5025726643 @default.
- W3181348310 creator A5036493562 @default.
- W3181348310 creator A5042690614 @default.
- W3181348310 creator A5043828893 @default.
- W3181348310 creator A5052837765 @default.
- W3181348310 creator A5069128525 @default.
- W3181348310 creator A5083327774 @default.
- W3181348310 creator A5084076076 @default.
- W3181348310 creator A5087948421 @default.
- W3181348310 date "2021-07-12" @default.
- W3181348310 modified "2023-10-18" @default.
- W3181348310 title "HDAC4 Inhibitors with Cyclic Linker and Non‐hydroxamate Zinc Binding Group: Design, Synthesis, HDAC Screening and <i>in</i> <i>vitro</i> Cytotoxicity evaluation." @default.
- W3181348310 cites W1966906920 @default.
- W3181348310 cites W1968218944 @default.
- W3181348310 cites W1970658265 @default.
- W3181348310 cites W1979519622 @default.
- W3181348310 cites W1982619775 @default.
- W3181348310 cites W1984328540 @default.
- W3181348310 cites W1987604182 @default.
- W3181348310 cites W2010251888 @default.
- W3181348310 cites W2013093508 @default.
- W3181348310 cites W2025162481 @default.
- W3181348310 cites W2036720950 @default.
- W3181348310 cites W2038075140 @default.
- W3181348310 cites W2039842983 @default.
- W3181348310 cites W2042806682 @default.
- W3181348310 cites W2044878334 @default.
- W3181348310 cites W2045815014 @default.
- W3181348310 cites W2046467348 @default.
- W3181348310 cites W2051110697 @default.
- W3181348310 cites W2055999639 @default.
- W3181348310 cites W2059497015 @default.
- W3181348310 cites W2064959533 @default.
- W3181348310 cites W2066264051 @default.
- W3181348310 cites W2067061459 @default.
- W3181348310 cites W2070021342 @default.
- W3181348310 cites W2074636474 @default.
- W3181348310 cites W2075660408 @default.
- W3181348310 cites W2094714880 @default.
- W3181348310 cites W2095877288 @default.
- W3181348310 cites W2101127235 @default.
- W3181348310 cites W2113056756 @default.
- W3181348310 cites W2121296685 @default.
- W3181348310 cites W2123344204 @default.
- W3181348310 cites W2144109917 @default.
- W3181348310 cites W2148495272 @default.
- W3181348310 cites W2153344496 @default.
- W3181348310 cites W2158178080 @default.
- W3181348310 cites W2168368163 @default.
- W3181348310 cites W2168912846 @default.
- W3181348310 cites W2219233634 @default.
- W3181348310 cites W2342868230 @default.
- W3181348310 cites W2398540841 @default.
- W3181348310 cites W2415756592 @default.
- W3181348310 cites W2511667040 @default.
- W3181348310 cites W2528606756 @default.
- W3181348310 cites W2555896464 @default.
- W3181348310 cites W2591529202 @default.
- W3181348310 cites W2724336500 @default.
- W3181348310 cites W2886726729 @default.
- W3181348310 cites W2893586598 @default.
- W3181348310 cites W2945307627 @default.
- W3181348310 cites W2978037151 @default.
- W3181348310 cites W2996223596 @default.
- W3181348310 cites W3015561989 @default.
- W3181348310 cites W3039878944 @default.
- W3181348310 cites W3048963168 @default.
- W3181348310 cites W3163516767 @default.
- W3181348310 cites W4233823505 @default.
- W3181348310 doi "https://doi.org/10.1002/slct.202102061" @default.
- W3181348310 hasPublicationYear "2021" @default.
- W3181348310 type Work @default.
- W3181348310 sameAs 3181348310 @default.
- W3181348310 citedByCount "7" @default.
- W3181348310 countsByYear W31813483102021 @default.
- W3181348310 countsByYear W31813483102022 @default.
- W3181348310 countsByYear W31813483102023 @default.
- W3181348310 crossrefType "journal-article" @default.
- W3181348310 hasAuthorship W3181348310A5010725738 @default.
- W3181348310 hasAuthorship W3181348310A5016919711 @default.
- W3181348310 hasAuthorship W3181348310A5025726643 @default.
- W3181348310 hasAuthorship W3181348310A5036493562 @default.
- W3181348310 hasAuthorship W3181348310A5042690614 @default.
- W3181348310 hasAuthorship W3181348310A5043828893 @default.
- W3181348310 hasAuthorship W3181348310A5052837765 @default.
- W3181348310 hasAuthorship W3181348310A5069128525 @default.
- W3181348310 hasAuthorship W3181348310A5083327774 @default.
- W3181348310 hasAuthorship W3181348310A5084076076 @default.
- W3181348310 hasAuthorship W3181348310A5087948421 @default.
- W3181348310 hasConcept C109316439 @default.
- W3181348310 hasConcept C111919701 @default.
- W3181348310 hasConcept C153911025 @default.
- W3181348310 hasConcept C159110408 @default.
- W3181348310 hasConcept C185592680 @default.