About: New hydrazonoindolin-2-ones: Synthesis, exploration of the possible anti-proliferative mechanism of action and encapsulation into PLGA microspheres

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About: New hydrazonoindolin-2-ones: Synthesis, exploration of the possible anti-proliferative mechanism of action and encapsulation into PLGA microspheres Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : covidontheweb.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	New hydrazonoindolin-2-ones: Synthesis, exploration of the possible anti-proliferative mechanism of action and encapsulation into PLGA microspheres
Creator	Attia, Mohamed Abdel-Aziz, Hatem Afifi, Samar Eldehna, Wagdy Keeton, Adam Piazza, Gary
Source	PMC
abstract	The synthesis and molecular characterization of new isatin-based hydrazonoindolin-2-ones 4a-o and 7a-e are reported. The in vitro anti-proliferative potential of the synthesized compounds 4a-o and 7a-e was examined against HT-29 (colon), ZR-75 (breast) and A549 (lung) human cancer cell lines. Compounds 7b, 7d and 7e were the most active congeners against the tested human cancer cell lines with average IC(50) values of 4.77, 3.39 and 2.37 μM, respectively, as compared with the reference isatin-based drug, sunitinib, which exhibited an average IC(50) value of 8.11 μM. Compound 7e was selected for further pharmacological evaluation in order to gain insight into its possible mechanism of action. It increased caspase 3/7 activity by 2.4- and 1.85-fold between 4 and 8 h of treatment, respectively, at 10 μM and it caused a decrease in the percentage of cells in the G1 phase of the cell cycle with a corresponding increase in the S-phase. In addition, compound 7e increased phosphorylated tyrosine (p-Tyr) levels nearly two-fold with an apparent IC(50) value of 3.8 μM. The 7e-loaded PLGA microspheres were prepared using a modified emulsion-solvent diffusion method. The average encapsulation efficiency of the 7e-loaded PLGA microspheres was 85% ± 1.3. While, the in vitro release profile of the 7e-loaded microspheres was characterized by slow and continuous release of compound 7e during 21 days and the release curve was fitted to zero order kinetics. Incorporation of 7e into PLGA microspheres improved its in vitro anti-proliferative activity toward the human cancer cell line A549 after 120 h incubation period with an IC(50) value less than 0.8 μM.
has issue date	2017-07-25(xsd:dateTime)
bibo:doi	10.1371/journal.pone.0181241
bibo:pmid	28742842
has license	cc-by
sha1sum (hex)	c1903895a3fc53a43a81d310f7567181bdee782f
schema:url	https://doi.org/10.1371/journal.pone.0181241
resource representing a document's title	New hydrazonoindolin-2-ones: Synthesis, exploration of the possible anti-proliferative mechanism of action and encapsulation into PLGA microspheres
has PubMed Central identifier	PMC5526551
has PubMed identifier	28742842
schema:publication	PLoS One
resource representing a document's body	covid:c1903895a3fc53a43a81d310f7567181bdee782f#body_text
is schema:about of	named entity 'G1 phase' named entity 'HT-29' named entity 'cell cycle' named entity 'pharmacological' named entity 'active' named entity 'MICROSPHERES' named entity 'POSSIBLE' named entity 'S-PHASE' named entity 'AVERAGE' named entity 'NEARLY' named entity 'BASED' named entity 'ZERO ORDER' named entity 'INCUBATION PERIOD' named entity 'DIFFUSION METHOD' named entity 'DECREASE' named entity 'HUMAN' named entity 'ACTIVITY' named entity 'REFERENCE' named entity 'A549' named entity 'MODIFIED' named entity 'EXAMINED' named entity 'CHARACTERIZATION' named entity 'INSIGHT' named entity 'SYNTHESIS' named entity 'PERCENTAGE' named entity 'CELLS' named entity 'APPARENT' named entity 'SELECTED' named entity 'CELL CYCLE' named entity 'INCREASED' named entity 'AT 10' named entity 'MECHANISM OF ACTION' named entity 'G1 PHASE' named entity '1.3' named entity 'HT-29' named entity 'POTENTIAL' named entity 'HUMAN CANCER CELL LINE' named entity 'VALUE' named entity 'ISATIN' named entity 'CONGENERS' named entity 'LEVELS' named entity 'RELEASE' named entity 'TYR' named entity 'POSSIBLE' named entity 'PROLIFERATIVE' named entity 'CAUSED' named entity 'VALUES' named entity 'USING' named entity 'SLOW' named entity 'PHOSPHORYLATED' named entity 'LOADED' named entity 'EXPLORATION' named entity 'ENCAPSULATION' named entity 'MOLECULAR' named entity 'PREPARED' named entity 'CASPASE 3' named entity 'BCM' named entity 'MICROSPHERES' named entity 'ADDITION' named entity 'DAYS' named entity 'CANCER CELL LINES' named entity 'CONTINUOUS' named entity 'PROFILE' named entity 'ITS' named entity 'PLGA' named entity 'PROLIFERATIVE' named entity 'TREATMENT' named entity 'SYNTHESIS' named entity 'NEW' named entity 'ENCAPSULATION EFFICIENCY' named entity 'IN VITRO' named entity 'IMPROVED' named entity 'IN VITRO RELEASE' named entity 'TESTED' named entity 'PHARMACOLOGICAL' named entity 'TYROSINE'

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