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Rebeccamycin (NSC 655649) is a weak
topoisomerase DNA topoisomerases (or topoisomerases) are enzymes that catalyze changes in the topological state of DNA, interconverting relaxed and supercoiled forms, linked (catenated) and unlinked species, and knotted and unknotted DNA. Topological issues i ...
I inhibitor isolated from ''
Nocardia ''Nocardia'' is a genus of weakly staining Gram-positive, catalase-positive, rod-shaped bacteria. It forms partially acid-fast beaded branching filaments (acting as fungi, but being truly bacteria). It contains a total of 85 species. Some spec ...
sp.'' It is structurally similar to
staurosporine Staurosporine (antibiotic AM-2282 or STS) is a natural product originally isolated in 1977 from the bacterium ''Streptomyces staurosporeus''. It was the first of over 50 alkaloids to be isolated with this type of bis-indole chemical structure. The ...
, but does not show any inhibitory activity against
protein kinases A protein kinase is a kinase which selectively modifies other proteins by covalently adding phosphates to them (phosphorylation) as opposed to kinases which modify lipids, carbohydrates, or other molecules. Phosphorylation usually results in a fun ...
. It shows significant antitumor properties in vitro (IC50=480nM against mouse B16 melanoma cells and IC50=500nM against P388 leukemia cells). It is an antineoplastic antibiotic and an intercalating agent. Becatecarin (BMS-181176) is a synthetic analog of rebeccamycin. Rebeccamycin and becatecarin have been tested in phase II clinical trials for the treatment of lung cancer, liver cancer, breast cancer, lymphoma, retinoblastoma, kidney cancer, and ovarian cancer.


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Further reading

* * * * * Experimental cancer drugs Topoisomerase inhibitors Halogen-containing alkaloids {{antineoplastic-drug-stub