136440-70-5
Chemical Structure
CP-115953
- CAS No.: 136440-70-5
- Formula:C19H13F2NO4
- Molecular Weight:357.31
IUPAC Name: 1-cyclopropyl-6,8-difluoro-7-(4-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
InChIKey: ISQTYKAFNUVODK-UHFFFAOYSA-N
SMILES: O=C(C1=CN(C2CC2)C3=C(C=C(F)C(C4=CC=C(O)C=C4)=C3F)C1=O)O
Biological Activity: CP-115953 is an antitumor fluoroquinolone compound that targets eukaryotic topoisomerase II and Escherichia coli DNA gyrase. CP-115953 inhibits ATP hydrolysis and DNA relaxation by stimulating enzyme-mediated DNA cleavage, and enhances the expression of immune-related cytokines. CP-115953 is applicable for research on human cancers[1][2][3][4][5][6][7].
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CP-115953 | CP-115953 is an antitumor fluoroquinolone compound that targets eukaryotic topoisomerase II and Escherichia coli DNA gyrase. CP-115953 inhibits ATP hydrolysis and DNA relaxation by stimulating enzyme-mediated DNA cleavage, and enhances the expression of immune-related cytokines. CP-115953 is applicable for research on human cancers. | |||||||||||||||||||||
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References
- [1]. Robinson MJ, et al. Effects of quinolone derivatives on eukaryotic topoisomerase II. A novel mechanism for enhancement of enzyme-mediated DNA cleavage. J Biol Chem. 1991 Aug 5;266(22):14585-92. [Content Brief]
- [2]. Robinson MJ, et al. Effects of novel fluoroquinolones on the catalytic activities of eukaryotic topoisomerase II: Influence of the C-8 fluorine group. Antimicrobial agents and chemotherapy. 1992 Apr;36(4):751-6.
- [3]. Robinson MJ, et al. Effects of topoisomerase II-targeted drugs on enzyme-mediated DNA cleavage and ATP hydrolysis: evidence for distinct drug interaction domains on topoisomerase II. Biochemistry. 1993 Apr 13;32(14):3638-43.
- [4]. Elsea SH, et al. Drug features that contribute to the activity of quinolones against mammalian topoisomerase II and cultured cells: correlation between enhancement of enzyme-mediated DNA cleavage in vitro and cytotoxic potential. Antimicrobial agents and chemotherapy. 1993 Oct;37(10):2179-86.
- [5]. Elsea SH, et al. Quinolones share a common interaction domain on topoisomerase II with other DNA cleavage-enhancing antineoplastic drugs. Biochemistry. 1997 Mar 11;36(10):2919-24. [Content Brief]
- [6]. Riesbeck K, et al. CP-115,953 stimulates cytokine production by lymphocytes. Antimicrob Agents Chemother. 1995 Feb;39(2):476-83.
- [7]. Elsea SH, et al. A yeast type II topoisomerase selected for resistance to quinolones. Mutation of histidine 1012 to tyrosine confers resistance to nonintercalative drugs but hypersensitivity to ellipticine. J Biol Chem. 1995 Jan 27;270(4):1913-20.
