Matches in SemOpenAlex for { <https://semopenalex.org/work/W2893498107> ?p ?o ?g. }
Showing items 1 to 99 of
99
with 100 items per page.
- W2893498107 abstract "Abstract Triazole derivatives of melampomagnolide B (MMB) have been synthesized via click chemistry methodologies and screened against a panel of 60 human cancer cell lines. Several derivatives showed promising anti-cancer activity, affording growth inhibition (GI50) values in the nanomolar range (GI50 = 0.02–0.99 μM). Lead compound 7h exhibited EC50 values of 400 nM and 700 nM, respectively, against two AML clinical specimens. Compound 7h was significantly more potent than parthenolide as an inhibitor of p65 phosphorylation in both hematological and solid tumor cell lines, indicating its ability to inhibit the NF-κB pathway. In TMD-231 breast cancer cells, treatment with 7h reduced DNA binding activity of NF-κB through inhibition of IKK-β mediated p65 phosphorylation and caused elevation of basal IκBα levels through inhibition of constitutive IκBα turnover and NF-κB activation. Molecular docking and dynamic modeling studies indicated that 7h interacts with the kinase domain of the monomeric IKKβ subunit, leading to inhibition of IKKβ activation, and compromising phosphorylation of downstream targets of the NF-κB pathway; dynamic modeling studies show that this interaction also causes unwinding of the α-helix of the NEMO binding site on IKKβ. Molecular docking studies with 10, a water-soluble analog of 7h, demonstrate that this analog interacts with the dimerization/oligomerization domain of monomeric IKKβ and may inhibit oligomer formation and subsequent autophosphorylation. Sesquiterpene lactones 7h and 10 are considered ideal candidates for potential clinical development." @default.
- W2893498107 created "2018-10-05" @default.
- W2893498107 creator A5013419890 @default.
- W2893498107 creator A5016741414 @default.
- W2893498107 creator A5019832718 @default.
- W2893498107 creator A5038867429 @default.
- W2893498107 creator A5062144523 @default.
- W2893498107 creator A5077524140 @default.
- W2893498107 creator A5077837457 @default.
- W2893498107 creator A5083049265 @default.
- W2893498107 date "2018-09-01" @default.
- W2893498107 modified "2023-09-26" @default.
- W2893498107 title "MMB triazole analogs are potent NF-κB inhibitors and anti-cancer agents against both hematological and solid tumor cells" @default.
- W2893498107 hasPublicationYear "2018" @default.
- W2893498107 type Work @default.
- W2893498107 sameAs 2893498107 @default.
- W2893498107 citedByCount "0" @default.
- W2893498107 crossrefType "book-chapter" @default.
- W2893498107 hasAuthorship W2893498107A5013419890 @default.
- W2893498107 hasAuthorship W2893498107A5016741414 @default.
- W2893498107 hasAuthorship W2893498107A5019832718 @default.
- W2893498107 hasAuthorship W2893498107A5038867429 @default.
- W2893498107 hasAuthorship W2893498107A5062144523 @default.
- W2893498107 hasAuthorship W2893498107A5077524140 @default.
- W2893498107 hasAuthorship W2893498107A5077837457 @default.
- W2893498107 hasAuthorship W2893498107A5083049265 @default.
- W2893498107 hasConcept C100175707 @default.
- W2893498107 hasConcept C104317684 @default.
- W2893498107 hasConcept C11960822 @default.
- W2893498107 hasConcept C121608353 @default.
- W2893498107 hasConcept C143065580 @default.
- W2893498107 hasConcept C150109051 @default.
- W2893498107 hasConcept C159110408 @default.
- W2893498107 hasConcept C184235292 @default.
- W2893498107 hasConcept C185592680 @default.
- W2893498107 hasConcept C190283241 @default.
- W2893498107 hasConcept C2777730290 @default.
- W2893498107 hasConcept C2779730028 @default.
- W2893498107 hasConcept C2780321935 @default.
- W2893498107 hasConcept C32619005 @default.
- W2893498107 hasConcept C41685203 @default.
- W2893498107 hasConcept C502942594 @default.
- W2893498107 hasConcept C54355233 @default.
- W2893498107 hasConcept C55493867 @default.
- W2893498107 hasConcept C62478195 @default.
- W2893498107 hasConcept C71924100 @default.
- W2893498107 hasConcept C86803240 @default.
- W2893498107 hasConcept C96232424 @default.
- W2893498107 hasConcept C97029542 @default.
- W2893498107 hasConceptScore W2893498107C100175707 @default.
- W2893498107 hasConceptScore W2893498107C104317684 @default.
- W2893498107 hasConceptScore W2893498107C11960822 @default.
- W2893498107 hasConceptScore W2893498107C121608353 @default.
- W2893498107 hasConceptScore W2893498107C143065580 @default.
- W2893498107 hasConceptScore W2893498107C150109051 @default.
- W2893498107 hasConceptScore W2893498107C159110408 @default.
- W2893498107 hasConceptScore W2893498107C184235292 @default.
- W2893498107 hasConceptScore W2893498107C185592680 @default.
- W2893498107 hasConceptScore W2893498107C190283241 @default.
- W2893498107 hasConceptScore W2893498107C2777730290 @default.
- W2893498107 hasConceptScore W2893498107C2779730028 @default.
- W2893498107 hasConceptScore W2893498107C2780321935 @default.
- W2893498107 hasConceptScore W2893498107C32619005 @default.
- W2893498107 hasConceptScore W2893498107C41685203 @default.
- W2893498107 hasConceptScore W2893498107C502942594 @default.
- W2893498107 hasConceptScore W2893498107C54355233 @default.
- W2893498107 hasConceptScore W2893498107C55493867 @default.
- W2893498107 hasConceptScore W2893498107C62478195 @default.
- W2893498107 hasConceptScore W2893498107C71924100 @default.
- W2893498107 hasConceptScore W2893498107C86803240 @default.
- W2893498107 hasConceptScore W2893498107C96232424 @default.
- W2893498107 hasConceptScore W2893498107C97029542 @default.
- W2893498107 hasLocation W28934981071 @default.
- W2893498107 hasOpenAccess W2893498107 @default.
- W2893498107 hasPrimaryLocation W28934981071 @default.
- W2893498107 hasRelatedWork W1121537454 @default.
- W2893498107 hasRelatedWork W1985382792 @default.
- W2893498107 hasRelatedWork W2019371417 @default.
- W2893498107 hasRelatedWork W2069325539 @default.
- W2893498107 hasRelatedWork W2092142031 @default.
- W2893498107 hasRelatedWork W2096298245 @default.
- W2893498107 hasRelatedWork W2236061800 @default.
- W2893498107 hasRelatedWork W2237100413 @default.
- W2893498107 hasRelatedWork W2551912396 @default.
- W2893498107 hasRelatedWork W2606558956 @default.
- W2893498107 hasRelatedWork W2783191436 @default.
- W2893498107 hasRelatedWork W2885312582 @default.
- W2893498107 hasRelatedWork W2962450952 @default.
- W2893498107 hasRelatedWork W2972591560 @default.
- W2893498107 hasRelatedWork W3020558783 @default.
- W2893498107 hasRelatedWork W3042678060 @default.
- W2893498107 hasRelatedWork W3134408619 @default.
- W2893498107 hasRelatedWork W3139099488 @default.
- W2893498107 hasRelatedWork W3159460424 @default.
- W2893498107 hasRelatedWork W3209325055 @default.
- W2893498107 isParatext "false" @default.
- W2893498107 isRetracted "false" @default.
- W2893498107 magId "2893498107" @default.
- W2893498107 workType "book-chapter" @default.