Matches in SemOpenAlex for { <https://semopenalex.org/work/W2904672092> ?p ?o ?g. }
- W2904672092 endingPage "1916" @default.
- W2904672092 startingPage "1902" @default.
- W2904672092 abstract "We report the synthesis and metabolic and biological evaluation of a series of 17 novel heterocyclic derivatives of isocombretastatin-A4 (iso-CA-4) and their structure-activity relationships. Among these derivatives, the most active compound, 4f, inhibited the growth of a panel of seven cancer cell lines with an IC50 in the low nanomolar range. In addition, 4f showed interesting activity against CA-4-resistant colon-carcinoma cells and multidrug-resistant leukemia cells. It also induced G2/M cell-cycle arrest. Structural data indicated binding of 4f to the colchicine site of tubulin, likely preventing the curved-to-straight tubulin structural changes that occur during microtubule assembly. Also, 4f disrupted the blood-vessel-like assembly formed by human umbilical-vein endothelial cells in vitro, suggesting its function as a vascular-disrupting agent. An in vitro metabolism study of 4f showed its high human-microsomal stability in comparison with that of iso-CA-4. The physicochemical properties of 4f may be conducive to CNS permeability, suggesting that this compound may be a possible candidate for the treatment of glioblastoma." @default.
- W2904672092 created "2018-12-22" @default.
- W2904672092 creator A5013335730 @default.
- W2904672092 creator A5014321410 @default.
- W2904672092 creator A5020514123 @default.
- W2904672092 creator A5034114577 @default.
- W2904672092 creator A5043659163 @default.
- W2904672092 creator A5048957528 @default.
- W2904672092 creator A5060667311 @default.
- W2904672092 creator A5063609573 @default.
- W2904672092 creator A5071730193 @default.
- W2904672092 creator A5075282244 @default.
- W2904672092 creator A5076191795 @default.
- W2904672092 creator A5080593255 @default.
- W2904672092 creator A5086071913 @default.
- W2904672092 creator A5086256410 @default.
- W2904672092 date "2018-12-10" @default.
- W2904672092 modified "2023-10-18" @default.
- W2904672092 title "1,1-Diheterocyclic Ethylenes Derived from Quinaldine and Carbazole as New Tubulin-Polymerization Inhibitors: Synthesis, Metabolism, and Biological Evaluation" @default.
- W2904672092 cites W1918363244 @default.
- W2904672092 cites W1970199745 @default.
- W2904672092 cites W1970795622 @default.
- W2904672092 cites W1971579914 @default.
- W2904672092 cites W1984076336 @default.
- W2904672092 cites W1990196931 @default.
- W2904672092 cites W1994297035 @default.
- W2904672092 cites W1995523151 @default.
- W2904672092 cites W1999236504 @default.
- W2904672092 cites W2000113221 @default.
- W2904672092 cites W2000248977 @default.
- W2904672092 cites W2007302055 @default.
- W2904672092 cites W2009979602 @default.
- W2904672092 cites W2010093251 @default.
- W2904672092 cites W2014528904 @default.
- W2904672092 cites W2014636427 @default.
- W2904672092 cites W2024264494 @default.
- W2904672092 cites W2033873407 @default.
- W2904672092 cites W2039676417 @default.
- W2904672092 cites W2040044819 @default.
- W2904672092 cites W2050272098 @default.
- W2904672092 cites W2063935472 @default.
- W2904672092 cites W2064571598 @default.
- W2904672092 cites W2065061109 @default.
- W2904672092 cites W2066551127 @default.
- W2904672092 cites W2067125249 @default.
- W2904672092 cites W2083740330 @default.
- W2904672092 cites W2092352405 @default.
- W2904672092 cites W2093262365 @default.
- W2904672092 cites W2114980992 @default.
- W2904672092 cites W2122636115 @default.
- W2904672092 cites W2122726580 @default.
- W2904672092 cites W2124026197 @default.
- W2904672092 cites W2132356916 @default.
- W2904672092 cites W2132851071 @default.
- W2904672092 cites W2143538808 @default.
- W2904672092 cites W2145438844 @default.
- W2904672092 cites W2145516891 @default.
- W2904672092 cites W2152021629 @default.
- W2904672092 cites W2157674286 @default.
- W2904672092 cites W2163341755 @default.
- W2904672092 cites W2163773013 @default.
- W2904672092 cites W2164488259 @default.
- W2904672092 cites W2166600497 @default.
- W2904672092 cites W2317077597 @default.
- W2904672092 cites W2320118577 @default.
- W2904672092 cites W2404735473 @default.
- W2904672092 cites W2460192074 @default.
- W2904672092 cites W2460615260 @default.
- W2904672092 cites W2501416232 @default.
- W2904672092 cites W2531047698 @default.
- W2904672092 cites W2557059615 @default.
- W2904672092 cites W2573197589 @default.
- W2904672092 cites W2736289869 @default.
- W2904672092 cites W2782760158 @default.
- W2904672092 cites W2953110937 @default.
- W2904672092 cites W4248872320 @default.
- W2904672092 doi "https://doi.org/10.1021/acs.jmedchem.8b01386" @default.
- W2904672092 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30525602" @default.
- W2904672092 hasPublicationYear "2018" @default.
- W2904672092 type Work @default.
- W2904672092 sameAs 2904672092 @default.
- W2904672092 citedByCount "41" @default.
- W2904672092 countsByYear W29046720922019 @default.
- W2904672092 countsByYear W29046720922020 @default.
- W2904672092 countsByYear W29046720922021 @default.
- W2904672092 countsByYear W29046720922022 @default.
- W2904672092 countsByYear W29046720922023 @default.
- W2904672092 crossrefType "journal-article" @default.
- W2904672092 hasAuthorship W2904672092A5013335730 @default.
- W2904672092 hasAuthorship W2904672092A5014321410 @default.
- W2904672092 hasAuthorship W2904672092A5020514123 @default.
- W2904672092 hasAuthorship W2904672092A5034114577 @default.
- W2904672092 hasAuthorship W2904672092A5043659163 @default.
- W2904672092 hasAuthorship W2904672092A5048957528 @default.
- W2904672092 hasAuthorship W2904672092A5060667311 @default.
- W2904672092 hasAuthorship W2904672092A5063609573 @default.
- W2904672092 hasAuthorship W2904672092A5071730193 @default.
- W2904672092 hasAuthorship W2904672092A5075282244 @default.