Matches in SemOpenAlex for { <https://semopenalex.org/work/W4313890010> ?p ?o ?g. }
Showing items 1 to 94 of
94
with 100 items per page.
- W4313890010 abstract "Introduction: Development of Poly (ADP-ribose) polymerase (PARP) inhibitors has been extensively studied in cancer treatment. Olaparib, the first approved PARP inhibitor, showed potency in the inhibition of both BRCA (breast cancer associated)-mutated and BRCA-unmutated cancers. Methods: Aiming to the discovery of olaparib analogs for the treatment of cancer, structural modifications were performed based on the scaffold of olaparib. In the first series, reduction of carbonyl group to CH 2 led to decrease of PARP1 inhibitory activity. Preserving the original carbonyl group, molecules with potent PARP1 inhibitory activities were derived by introduction of hydrazide and aromatic nitrogen mustard groups. The synthesized compounds were evaluated in the in the PARP1 enzyme inhibitory screening, cancer cell based antiproliferative assay, cell cycle arrest and apoptosis studies. Results: It is remarkable that, molecule C2 with chlorambucil substitution, exhibited potent PARP1 inhibitory activity and a broad-spectrum of anticancer potency in the in vitro antiproliferative assay. Compared with olaparib and chlorambucil, molecule C2 also showed significant potency in inhibition of a variety of BRCA-unmutated cell lines. Further analysis revealed the effects of C2 in induction of G2/M phase cell cycle arrest and promotion of apoptosis. Discussion: Collectively, the olaparib-chlorambucil hybrid molecule (C2) could be utilized as a lead compound for further drug design." @default.
- W4313890010 created "2023-01-10" @default.
- W4313890010 creator A5009942594 @default.
- W4313890010 creator A5051970233 @default.
- W4313890010 creator A5057209439 @default.
- W4313890010 creator A5058818476 @default.
- W4313890010 creator A5071798264 @default.
- W4313890010 creator A5086948504 @default.
- W4313890010 date "2023-01-09" @default.
- W4313890010 modified "2023-10-18" @default.
- W4313890010 title "Discovery of a potent olaparib–chlorambucil hybrid inhibitor of PARP1 for the treatment of cancer" @default.
- W4313890010 cites W1992397774 @default.
- W4313890010 cites W2009007206 @default.
- W4313890010 cites W2014035904 @default.
- W4313890010 cites W2062154047 @default.
- W4313890010 cites W2086688857 @default.
- W4313890010 cites W2117692326 @default.
- W4313890010 cites W2117964602 @default.
- W4313890010 cites W2147154862 @default.
- W4313890010 cites W2165091409 @default.
- W4313890010 cites W2165912346 @default.
- W4313890010 cites W2169322031 @default.
- W4313890010 cites W2323969866 @default.
- W4313890010 cites W2415408705 @default.
- W4313890010 cites W2472990710 @default.
- W4313890010 cites W2688973277 @default.
- W4313890010 cites W2732346161 @default.
- W4313890010 cites W2904303838 @default.
- W4313890010 cites W2975529099 @default.
- W4313890010 cites W2987630388 @default.
- W4313890010 cites W3084114043 @default.
- W4313890010 doi "https://doi.org/10.3389/fphar.2022.1054616" @default.
- W4313890010 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/36699082" @default.
- W4313890010 hasPublicationYear "2023" @default.
- W4313890010 type Work @default.
- W4313890010 citedByCount "2" @default.
- W4313890010 crossrefType "journal-article" @default.
- W4313890010 hasAuthorship W4313890010A5009942594 @default.
- W4313890010 hasAuthorship W4313890010A5051970233 @default.
- W4313890010 hasAuthorship W4313890010A5057209439 @default.
- W4313890010 hasAuthorship W4313890010A5058818476 @default.
- W4313890010 hasAuthorship W4313890010A5071798264 @default.
- W4313890010 hasAuthorship W4313890010A5086948504 @default.
- W4313890010 hasBestOaLocation W43138900101 @default.
- W4313890010 hasConcept C126322002 @default.
- W4313890010 hasConcept C181199279 @default.
- W4313890010 hasConcept C182979987 @default.
- W4313890010 hasConcept C185592680 @default.
- W4313890010 hasConcept C2776694085 @default.
- W4313890010 hasConcept C2776755627 @default.
- W4313890010 hasConcept C2777866208 @default.
- W4313890010 hasConcept C2778480876 @default.
- W4313890010 hasConcept C2779138821 @default.
- W4313890010 hasConcept C2779962180 @default.
- W4313890010 hasConcept C502942594 @default.
- W4313890010 hasConcept C55493867 @default.
- W4313890010 hasConcept C71924100 @default.
- W4313890010 hasConcept C82381507 @default.
- W4313890010 hasConcept C98274493 @default.
- W4313890010 hasConceptScore W4313890010C126322002 @default.
- W4313890010 hasConceptScore W4313890010C181199279 @default.
- W4313890010 hasConceptScore W4313890010C182979987 @default.
- W4313890010 hasConceptScore W4313890010C185592680 @default.
- W4313890010 hasConceptScore W4313890010C2776694085 @default.
- W4313890010 hasConceptScore W4313890010C2776755627 @default.
- W4313890010 hasConceptScore W4313890010C2777866208 @default.
- W4313890010 hasConceptScore W4313890010C2778480876 @default.
- W4313890010 hasConceptScore W4313890010C2779138821 @default.
- W4313890010 hasConceptScore W4313890010C2779962180 @default.
- W4313890010 hasConceptScore W4313890010C502942594 @default.
- W4313890010 hasConceptScore W4313890010C55493867 @default.
- W4313890010 hasConceptScore W4313890010C71924100 @default.
- W4313890010 hasConceptScore W4313890010C82381507 @default.
- W4313890010 hasConceptScore W4313890010C98274493 @default.
- W4313890010 hasFunder F4320336653 @default.
- W4313890010 hasLocation W43138900101 @default.
- W4313890010 hasLocation W43138900102 @default.
- W4313890010 hasLocation W43138900103 @default.
- W4313890010 hasOpenAccess W4313890010 @default.
- W4313890010 hasPrimaryLocation W43138900101 @default.
- W4313890010 hasRelatedWork W2001870355 @default.
- W4313890010 hasRelatedWork W2190095121 @default.
- W4313890010 hasRelatedWork W2283134145 @default.
- W4313890010 hasRelatedWork W2319395988 @default.
- W4313890010 hasRelatedWork W2769445989 @default.
- W4313890010 hasRelatedWork W2883804409 @default.
- W4313890010 hasRelatedWork W3023457002 @default.
- W4313890010 hasRelatedWork W4302773693 @default.
- W4313890010 hasRelatedWork W4361946037 @default.
- W4313890010 hasRelatedWork W4361952441 @default.
- W4313890010 hasVolume "13" @default.
- W4313890010 isParatext "false" @default.
- W4313890010 isRetracted "false" @default.
- W4313890010 workType "article" @default.