FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2912331103> ?p ?o ?g. }

• W2912331103 endingPage "244" @default.
• W2912331103 startingPage "226" @default.
• W2912331103 abstract "A series of new pyranocarbazole derivatives were synthesized via semi-synthetic modification of koenimbine (1a) and koenidine (1b) isolated from the leaves of Murraya koenigii. Among all, compound 3bg displayed significant anti-cancer activity against MDA-MB-231, DU145 and PC3 cell lines with the IC50 values of 3.8, 7.6 and 5.8 μM, respectively. It was also observed that the halogenated-benzyl substitution at N-9 position, C-3 Methyl and C-7 methoxy group on carbazole motif are favoured for anti-cancer activity. The detailed investigation was carried out with compound 3bg and its SEDDS (self-emulsifying drug delivery systems) formulation 3bgF. The in vivo drug release behavior study showed that the formulation enhanced slow release and better bioavailability at a tumor site. Compound 3bg and its formulation (3bgF) significantly inhibited cell proliferation and colony formation, induced G2/M arrest, reduced cellular ROS generation and induced caspase-dependent apoptosis in MDA-MB-231 cells. 3bg also induced significant alteration of Bax/Bcl expression ratio suggesting involvement of mitochondrial apoptosis. Additionally, 3bg caused down-regulation of mTOR/Akt survival pathway. 3bg do not bind to DNA, but interacts with tubulin as observed with in silico molecular docking studies. This interaction results in stabilization of tubulin polymerization similar to paclitaxel as detected in cell-free assay. Oral administration of 3bgF for 30 days at dose rate of 10 and 20 mg/kg body weight significantly reduced tumor growth in syngenic rat LA-7 mammary tumor model. These results indicated that the pyranocarbazole natural product based N-substituted analogues can act as potential anti-cancer lead." @default.
• W2912331103 created "2019-02-21" @default.
• W2912331103 creator A5000759047 @default.
• W2912331103 creator A5006519161 @default.
• W2912331103 creator A5019008348 @default.
• W2912331103 creator A5025634322 @default.
• W2912331103 creator A5043660092 @default.
• W2912331103 creator A5055333667 @default.
• W2912331103 creator A5084093973 @default.
• W2912331103 creator A5089061722 @default.
• W2912331103 date "2019-04-01" @default.
• W2912331103 modified "2023-10-16" @default.
• W2912331103 title "Pyranocarbazole derivatives as potent anti-cancer agents triggering tubulin polymerization stabilization induced activation of caspase-dependent apoptosis and downregulation of Akt/mTOR in breast cancer cells" @default.
• W2912331103 cites W1491968011 @default.
• W2912331103 cites W1595815978 @default.
• W2912331103 cites W1840048214 @default.
• W2912331103 cites W1872036705 @default.
• W2912331103 cites W1966144887 @default.
• W2912331103 cites W1967790685 @default.
• W2912331103 cites W1976952839 @default.
• W2912331103 cites W1982728268 @default.
• W2912331103 cites W1983609335 @default.
• W2912331103 cites W1988369885 @default.
• W2912331103 cites W1994345832 @default.
• W2912331103 cites W1998236197 @default.
• W2912331103 cites W2008757142 @default.
• W2912331103 cites W2016876678 @default.
• W2912331103 cites W2018618642 @default.
• W2912331103 cites W2019086054 @default.
• W2912331103 cites W2021159172 @default.
• W2912331103 cites W2024105041 @default.
• W2912331103 cites W2030172604 @default.
• W2912331103 cites W2041301244 @default.
• W2912331103 cites W2044752471 @default.
• W2912331103 cites W2057795561 @default.
• W2912331103 cites W2059740626 @default.
• W2912331103 cites W2068413127 @default.
• W2912331103 cites W2070732456 @default.
• W2912331103 cites W2073075985 @default.
• W2912331103 cites W2075606691 @default.
• W2912331103 cites W2076243878 @default.
• W2912331103 cites W2079094089 @default.
• W2912331103 cites W2083592534 @default.
• W2912331103 cites W2087667264 @default.
• W2912331103 cites W2088226047 @default.
• W2912331103 cites W2101297940 @default.
• W2912331103 cites W2101741807 @default.
• W2912331103 cites W2109528706 @default.
• W2912331103 cites W2118731822 @default.
• W2912331103 cites W2122001735 @default.
• W2912331103 cites W2129778797 @default.
• W2912331103 cites W2133190342 @default.
• W2912331103 cites W2136906178 @default.
• W2912331103 cites W2137035181 @default.
• W2912331103 cites W2141125222 @default.
• W2912331103 cites W2141474275 @default.
• W2912331103 cites W2142583550 @default.
• W2912331103 cites W2146450987 @default.
• W2912331103 cites W2152590519 @default.
• W2912331103 cites W2165721689 @default.
• W2912331103 cites W2182637937 @default.
• W2912331103 cites W2184899792 @default.
• W2912331103 cites W2185500533 @default.
• W2912331103 cites W2233674810 @default.
• W2912331103 cites W2256742438 @default.
• W2912331103 cites W2281736151 @default.
• W2912331103 cites W2306701052 @default.
• W2912331103 cites W2321452523 @default.
• W2912331103 cites W2322446758 @default.
• W2912331103 cites W2331097026 @default.
• W2912331103 cites W2341742415 @default.
• W2912331103 cites W2344733175 @default.
• W2912331103 cites W2345198528 @default.
• W2912331103 cites W2345594272 @default.
• W2912331103 cites W2388163742 @default.
• W2912331103 cites W2418244228 @default.
• W2912331103 cites W2473272113 @default.
• W2912331103 cites W2507101261 @default.
• W2912331103 cites W2511223268 @default.
• W2912331103 cites W2512200361 @default.
• W2912331103 cites W2513009842 @default.
• W2912331103 cites W2554935789 @default.
• W2912331103 cites W2562406896 @default.
• W2912331103 cites W2570915324 @default.
• W2912331103 cites W2726638980 @default.
• W2912331103 cites W2744845007 @default.
• W2912331103 cites W2775330397 @default.
• W2912331103 cites W2782301747 @default.
• W2912331103 cites W2793138419 @default.
• W2912331103 cites W2885769722 @default.
• W2912331103 cites W40302552 @default.
• W2912331103 cites W4294214970 @default.
• W2912331103 cites W433963279 @default.
• W2912331103 cites W839644325 @default.
• W2912331103 doi "https://doi.org/10.1016/j.ejmech.2019.02.003" @default.
• W2912331103 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30772606" @default.
• W2912331103 hasPublicationYear "2019" @default.
• W2912331103 type Work @default.

• next