Matches in SemOpenAlex for { <https://semopenalex.org/work/W2884672240> ?p ?o ?g. }
- W2884672240 endingPage "3900" @default.
- W2884672240 startingPage "3892" @default.
- W2884672240 abstract "Multidrug resistance and toxic side effects are the major challenges in cancer treatment with microtubule-targeting agents (MTAs), and thus, there is an urgent clinical need for new therapies. Chalcone, a common simple scaffold found in many natural products, is widely used as a privileged structure in medicinal chemistry. We have previously validated tubulin as the anticancer target for chalcone derivatives. In this study, an α-methyl-substituted indole-chalcone (FC77) was synthesized and found to exhibit an excellent cytotoxicity against the NCI-60 cell lines (average concentration causing 50% growth inhibition = 6 nM). More importantly, several multidrug-resistant cancer cell lines showed no resistance to FC77, and the compound demonstrated good selective toxicity against cancer cells versus normal CD34+ blood progenitor cells. A further mechanistic study demonstrated that FC77 could arrest cells that relate to the binding to tubulin and inhibit the microtubule dynamics. The National Cancer Institute COMPARE analysis and molecular modeling indicated that FC77 had a mechanism of action similar to that of colchicine. Overall, our data demonstrate that this indole-chalcone represents a novel MTA template for further development of potential drug candidates for the treatment of multidrug-resistant cancers." @default.
- W2884672240 created "2018-08-03" @default.
- W2884672240 creator A5005969908 @default.
- W2884672240 creator A5019449054 @default.
- W2884672240 creator A5024129015 @default.
- W2884672240 creator A5028402493 @default.
- W2884672240 creator A5029667848 @default.
- W2884672240 creator A5041570474 @default.
- W2884672240 creator A5044689802 @default.
- W2884672240 creator A5047452454 @default.
- W2884672240 creator A5049872559 @default.
- W2884672240 creator A5052243927 @default.
- W2884672240 creator A5063502485 @default.
- W2884672240 creator A5073989265 @default.
- W2884672240 creator A5088610056 @default.
- W2884672240 creator A5091650806 @default.
- W2884672240 date "2018-07-26" @default.
- W2884672240 modified "2023-10-14" @default.
- W2884672240 title "An Indole–Chalcone Inhibits Multidrug-Resistant Cancer Cell Growth by Targeting Microtubules" @default.
- W2884672240 cites W1540529121 @default.
- W2884672240 cites W1595352454 @default.
- W2884672240 cites W1963878289 @default.
- W2884672240 cites W1966579150 @default.
- W2884672240 cites W1966686539 @default.
- W2884672240 cites W1968241604 @default.
- W2884672240 cites W1984764188 @default.
- W2884672240 cites W1990469915 @default.
- W2884672240 cites W1991573861 @default.
- W2884672240 cites W2039349915 @default.
- W2884672240 cites W2042701817 @default.
- W2884672240 cites W2044203934 @default.
- W2884672240 cites W2048454522 @default.
- W2884672240 cites W2048883883 @default.
- W2884672240 cites W2056772956 @default.
- W2884672240 cites W2084810520 @default.
- W2884672240 cites W2087312216 @default.
- W2884672240 cites W2093855538 @default.
- W2884672240 cites W2108432488 @default.
- W2884672240 cites W2115386682 @default.
- W2884672240 cites W2119968160 @default.
- W2884672240 cites W2147301204 @default.
- W2884672240 cites W2182137760 @default.
- W2884672240 cites W2271027226 @default.
- W2884672240 cites W2321088547 @default.
- W2884672240 cites W2327974216 @default.
- W2884672240 cites W2331125073 @default.
- W2884672240 cites W2397676076 @default.
- W2884672240 cites W2398652712 @default.
- W2884672240 cites W2398775408 @default.
- W2884672240 cites W2402522246 @default.
- W2884672240 cites W2414157683 @default.
- W2884672240 cites W2418207038 @default.
- W2884672240 cites W2550481509 @default.
- W2884672240 cites W2606557370 @default.
- W2884672240 cites W2613820968 @default.
- W2884672240 cites W2769571705 @default.
- W2884672240 cites W2783556635 @default.
- W2884672240 cites W2793145550 @default.
- W2884672240 cites W2949434301 @default.
- W2884672240 doi "https://doi.org/10.1021/acs.molpharmaceut.8b00359" @default.
- W2884672240 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/6511885" @default.
- W2884672240 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30048137" @default.
- W2884672240 hasPublicationYear "2018" @default.
- W2884672240 type Work @default.
- W2884672240 sameAs 2884672240 @default.
- W2884672240 citedByCount "32" @default.
- W2884672240 countsByYear W28846722402019 @default.
- W2884672240 countsByYear W28846722402020 @default.
- W2884672240 countsByYear W28846722402021 @default.
- W2884672240 countsByYear W28846722402022 @default.
- W2884672240 countsByYear W28846722402023 @default.
- W2884672240 crossrefType "journal-article" @default.
- W2884672240 hasAuthorship W2884672240A5005969908 @default.
- W2884672240 hasAuthorship W2884672240A5019449054 @default.
- W2884672240 hasAuthorship W2884672240A5024129015 @default.
- W2884672240 hasAuthorship W2884672240A5028402493 @default.
- W2884672240 hasAuthorship W2884672240A5029667848 @default.
- W2884672240 hasAuthorship W2884672240A5041570474 @default.
- W2884672240 hasAuthorship W2884672240A5044689802 @default.
- W2884672240 hasAuthorship W2884672240A5047452454 @default.
- W2884672240 hasAuthorship W2884672240A5049872559 @default.
- W2884672240 hasAuthorship W2884672240A5052243927 @default.
- W2884672240 hasAuthorship W2884672240A5063502485 @default.
- W2884672240 hasAuthorship W2884672240A5073989265 @default.
- W2884672240 hasAuthorship W2884672240A5088610056 @default.
- W2884672240 hasAuthorship W2884672240A5091650806 @default.
- W2884672240 hasBestOaLocation W28846722402 @default.
- W2884672240 hasConcept C109316439 @default.
- W2884672240 hasConcept C114851261 @default.
- W2884672240 hasConcept C121608353 @default.
- W2884672240 hasConcept C133936738 @default.
- W2884672240 hasConcept C185592680 @default.
- W2884672240 hasConcept C192527728 @default.
- W2884672240 hasConcept C202751555 @default.
- W2884672240 hasConcept C20418707 @default.
- W2884672240 hasConcept C2776120743 @default.
- W2884672240 hasConcept C2776636253 @default.
- W2884672240 hasConcept C2780764945 @default.