359630-76-5Relevant academic research and scientific papers
Structure-activity relationship of novel acridone derivatives as antiproliferative agents
Chen, Ji-Ning,Wu, Xing-Kang,Lu, Chun-Hua,Li, Xun
, (2021)
Unlike other DNA topoisomerase II (topo II) inhibitors, our recently identified acridone derivative E17 exerted strong cytotoxic activity by inhibiting topo II without causing topo II degradation and DNA damage, which promoted us to explore more analogues
Optimization of naphthalimide-imidazoacridone with potent antitumor activity leading to clinical candidate (HKH40A, RTA 502)
Hariprakasha, Humcha K.,Kosakowska-Cholody, Teresa,Meyer, Colin,Cholody, Wieslaw M.,Stinson, Sherman F.,Tarasova, Nadya I.,Michejda, Christopher J.
, p. 5557 - 5560 (2007)
Unsymmetrical bifunctional antitumor agent WMC79 was further optimized to generate compound 7b that not only inhibited the growth of many tumor cell lines, but caused rapid apoptosis. Unlike the parent compound, 7b is toxic to both p53 positive and negati
Novel inhibitors of NRH:Quinone oxidoreductase 2 (NQO2): Crystal structures, biochemical activity, and intracellular effects of imidazoacridin-6-ones
Dunstan, Mark S.,Barnes, John,Humphries, Matthew,Whitehead, Roger C.,Bryce, Richard A.,Leys, David,Stratford, Ian J.,Nolan, Karen A.
, p. 6597 - 6611 (2011/12/01)
Imidazoacridin-6-ones are shown to be potent nanomolar inhibitors of the enzyme NQO2. By use of computational molecular modeling, a reliable QSAR was established, relating inhibitory potency with calculated binding affinity. Further, crystal structures of
Triazoloacridin-6-ones as novel inhibitors of the quinone oxidoreductases NQO1 and NQO2
Nolan, Karen A.,Humphries, Matthew P.,Barnes, John,Doncaster, Jeremy R.,Caraher, Mary C.,Tirelli, Nicola,Bryce, Richard A.,Whitehead, Roger C.,Stratford, Ian J.
experimental part, p. 696 - 706 (2010/07/04)
A range of triazoloacridin-6-ones functionalized at C5 and C8 have been synthesized and evaluated for ability to inhibit NQO1 and NQO2. The compounds were computationally docked into the active site of NQO1 and NQO2, and calculated binding affinities were
1,8-NAPHTHALIMIDE IMIDAZO{4,5,1-DE}ACRIDONES WITH ANTI-TUMOR ACTIVITY
-
, (2008/06/13)
The invention provides imidazoacridone compounds of general formula (1) which have cytotoxic and anti-tumor activity. The invention also provides methods of preparing the compounds, and methods of using the compounds for the treatment of cancer or other m
