Matches in SemOpenAlex for { <https://semopenalex.org/work/W3020928512> ?p ?o ?g. }
- W3020928512 endingPage "2177" @default.
- W3020928512 startingPage "2177" @default.
- W3020928512 abstract "Induction of apoptosis is a common chemotherapeutic mechanism to kill cancer cells The thiazole system has been reported over the past decades as a building block for the preparation of anticancer agents. A novel series of 2-arylalkylamino-4-amino-5-(3′,4′,5′-trimethoxybenzoyl)-thiazole derivatives designed as dual inhibitors of tubulin and cyclin-dependent kinases (CDKs) were synthesized and evaluated for their antiproliferative activity in vitro against two cancer cell lines and, for selected highly active compounds, for interactions with tubulin and cyclin-dependent kinases and for cell cycle and apoptosis effects. Structure-activity relationships were elucidated for various substituents at the 2-position of the thiazole skeleton. Among the synthesized compounds, the most active analogues were found to be the p-chlorobenzylamino derivative 8e as well as the p-chloro and p-methoxyphenethylamino analogues 8f and 8k, respectively, which inhibited the growth of U-937 and SK-MEL-1 cancer cell lines with IC50 values ranging from 5.7 to 12.2 μM. On U-937 cells, the tested compounds 8f and 8k induced apoptosis in a time and concentration dependent manner. These two latter molecules did not affect tubulin polymerization (IC50 > 20 μM) nor CDK activity at a single concentration of 10 μM, suggesting alternative targets than tubulin and CDK for the compounds." @default.
- W3020928512 created "2020-05-13" @default.
- W3020928512 creator A5003110719 @default.
- W3020928512 creator A5017758211 @default.
- W3020928512 creator A5032954885 @default.
- W3020928512 creator A5035565106 @default.
- W3020928512 creator A5041567500 @default.
- W3020928512 creator A5043145057 @default.
- W3020928512 creator A5047429620 @default.
- W3020928512 creator A5053376200 @default.
- W3020928512 creator A5065365203 @default.
- W3020928512 creator A5088149477 @default.
- W3020928512 creator A5088645883 @default.
- W3020928512 date "2020-05-06" @default.
- W3020928512 modified "2023-09-27" @default.
- W3020928512 title "Synthesis and Biological Evaluation of 2-Substituted Benzyl-/Phenylethylamino-4-amino-5-aroylthiazoles as Apoptosis-Inducing Anticancer Agents" @default.
- W3020928512 cites W1864174790 @default.
- W3020928512 cites W1969615301 @default.
- W3020928512 cites W1974543775 @default.
- W3020928512 cites W1976754562 @default.
- W3020928512 cites W1983134006 @default.
- W3020928512 cites W1985139403 @default.
- W3020928512 cites W1989711033 @default.
- W3020928512 cites W1999318478 @default.
- W3020928512 cites W2000163561 @default.
- W3020928512 cites W2027745162 @default.
- W3020928512 cites W2029197596 @default.
- W3020928512 cites W2038456507 @default.
- W3020928512 cites W2049856484 @default.
- W3020928512 cites W2089353165 @default.
- W3020928512 cites W2108300681 @default.
- W3020928512 cites W2114918609 @default.
- W3020928512 cites W2131644106 @default.
- W3020928512 cites W2142335883 @default.
- W3020928512 cites W2297912447 @default.
- W3020928512 cites W2402506318 @default.
- W3020928512 cites W2408954743 @default.
- W3020928512 cites W2523277769 @default.
- W3020928512 cites W2552283023 @default.
- W3020928512 cites W2586234144 @default.
- W3020928512 cites W2753841677 @default.
- W3020928512 cites W2762514363 @default.
- W3020928512 cites W2793671087 @default.
- W3020928512 cites W2795469599 @default.
- W3020928512 cites W2898544952 @default.
- W3020928512 cites W2922388086 @default.
- W3020928512 doi "https://doi.org/10.3390/molecules25092177" @default.
- W3020928512 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/7248693" @default.
- W3020928512 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/32384805" @default.
- W3020928512 hasPublicationYear "2020" @default.
- W3020928512 type Work @default.
- W3020928512 sameAs 3020928512 @default.
- W3020928512 citedByCount "5" @default.
- W3020928512 countsByYear W30209285122021 @default.
- W3020928512 countsByYear W30209285122022 @default.
- W3020928512 countsByYear W30209285122023 @default.
- W3020928512 crossrefType "journal-article" @default.
- W3020928512 hasAuthorship W3020928512A5003110719 @default.
- W3020928512 hasAuthorship W3020928512A5017758211 @default.
- W3020928512 hasAuthorship W3020928512A5032954885 @default.
- W3020928512 hasAuthorship W3020928512A5035565106 @default.
- W3020928512 hasAuthorship W3020928512A5041567500 @default.
- W3020928512 hasAuthorship W3020928512A5043145057 @default.
- W3020928512 hasAuthorship W3020928512A5047429620 @default.
- W3020928512 hasAuthorship W3020928512A5053376200 @default.
- W3020928512 hasAuthorship W3020928512A5065365203 @default.
- W3020928512 hasAuthorship W3020928512A5088149477 @default.
- W3020928512 hasAuthorship W3020928512A5088645883 @default.
- W3020928512 hasBestOaLocation W30209285121 @default.
- W3020928512 hasConcept C121608353 @default.
- W3020928512 hasConcept C124320809 @default.
- W3020928512 hasConcept C184235292 @default.
- W3020928512 hasConcept C185592680 @default.
- W3020928512 hasConcept C190283241 @default.
- W3020928512 hasConcept C20418707 @default.
- W3020928512 hasConcept C2778464347 @default.
- W3020928512 hasConcept C29537977 @default.
- W3020928512 hasConcept C54355233 @default.
- W3020928512 hasConcept C55493867 @default.
- W3020928512 hasConcept C71240020 @default.
- W3020928512 hasConcept C84425145 @default.
- W3020928512 hasConcept C86803240 @default.
- W3020928512 hasConcept C95444343 @default.
- W3020928512 hasConcept C96232424 @default.
- W3020928512 hasConceptScore W3020928512C121608353 @default.
- W3020928512 hasConceptScore W3020928512C124320809 @default.
- W3020928512 hasConceptScore W3020928512C184235292 @default.
- W3020928512 hasConceptScore W3020928512C185592680 @default.
- W3020928512 hasConceptScore W3020928512C190283241 @default.
- W3020928512 hasConceptScore W3020928512C20418707 @default.
- W3020928512 hasConceptScore W3020928512C2778464347 @default.
- W3020928512 hasConceptScore W3020928512C29537977 @default.
- W3020928512 hasConceptScore W3020928512C54355233 @default.
- W3020928512 hasConceptScore W3020928512C55493867 @default.
- W3020928512 hasConceptScore W3020928512C71240020 @default.
- W3020928512 hasConceptScore W3020928512C84425145 @default.
- W3020928512 hasConceptScore W3020928512C86803240 @default.
- W3020928512 hasConceptScore W3020928512C95444343 @default.