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Chemical Compound Review:

AC1NURAH 2-(2-chlorophenyl)-5,7- dihydroxy-8-[(3S...

Synonyms: SureCN3651, PubChem22427, ACN-S001924, CHEBI:104346, BCPP000228, ...

Kaur, G. et al., Bible, K.C. et al., Chao, S.H. et al., Worland, P.J. et al., Losiewicz, M.D. et al., et al.

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Disease relevance of Flavopiridol

BACKGROUND: Previous studies have shown that polyhydroxylated flavonoids such as quercetin and genistein can inhibit tumor cell growth in vitro, and preliminary in vivo studies of the flavone L86-8275 have shown growth inhibition of LX529 and A549 lung carcinomas [1].

High impact information on Flavopiridol

Growth inhibition with reversible cell cycle arrest of carcinoma cells by flavone L86-8275 [1].
METHODS: We studied the effects of L86-8275 on cell growth in seven breast carcinoma cell lines and five lung carcinoma cell lines [1].
When MDA468 cells released from aphidicolin-induced cell cycle arrest were exposed to 200 nM L86-8275, they completed the S phase but arrested in G2 [1].
When cells released from nocodazole-induced cell cycle arrest were exposed to 200 nM L86-8275, they completed mitosis but arrested in G1 [1].
Flavopiridol (NSC 649890, L86-8275), a potent inhibitor of cyclin-dependent kinase 1/p34cdc2 phosphorylation and kinase activity, is currently undergoing Phase I clinical testing as a potential antineoplastic agent [2].

Anatomical context of Flavopiridol

At concentrations of 25-160 nM, L86-8275 inhibited growth of human breast and lung carcinoma cell lines by 50% [1].

Associations of Flavopiridol with other chemical compounds

Flavopiridol (L86-8275, HMR1275) is a cyclin-dependent kinase (Cdk) inhibitor that is in clinical trials as a cancer treatment because of its antiproliferative properties [3].

Gene context of Flavopiridol

These data suggest L86-8275 as a lead structure for the development of inhibitors of the cyclin-dependent kinases [4].
Alteration of the phosphorylation state of p34cdc2 kinase by the flavone L86-8275 in breast carcinoma cells. Correlation with decreased H1 kinase activity [5].

Analytical, diagnostic and therapeutic context of Flavopiridol

Flavopiridol (L86-8275) is a synthetic flavone currently undergoing Phase I clinical trials [6].

References

Growth inhibition with reversible cell cycle arrest of carcinoma cells by flavone L86-8275. Kaur, G., Stetler-Stevenson, M., Sebers, S., Worland, P., Sedlacek, H., Myers, C., Czech, J., Naik, R., Sausville, E. J. Natl. Cancer Inst. (1992) [Pubmed]
Flavopiridol: a cytotoxic flavone that induces cell death in noncycling A549 human lung carcinoma cells. Bible, K.C., Kaufmann, S.H. Cancer Res. (1996) [Pubmed]
Flavopiridol inhibits P-TEFb and blocks HIV-1 replication. Chao, S.H., Fujinaga, K., Marion, J.E., Taube, R., Sausville, E.A., Senderowicz, A.M., Peterlin, B.M., Price, D.H. J. Biol. Chem. (2000) [Pubmed]
Potent inhibition of CDC2 kinase activity by the flavonoid L86-8275. Losiewicz, M.D., Carlson, B.A., Kaur, G., Sausville, E.A., Worland, P.J. Biochem. Biophys. Res. Commun. (1994) [Pubmed]
Alteration of the phosphorylation state of p34cdc2 kinase by the flavone L86-8275 in breast carcinoma cells. Correlation with decreased H1 kinase activity. Worland, P.J., Kaur, G., Stetler-Stevenson, M., Sebers, S., Sartor, O., Sausville, E.A. Biochem. Pharmacol. (1993) [Pubmed]
Potentiation of apoptosis by flavopiridol in mitomycin-C-treated gastric and breast cancer cells. Schwartz, G.K., Farsi, K., Maslak, P., Kelsen, D.P., Spriggs, D. Clin. Cancer Res. (1997) [Pubmed]

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