Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1992-11-19
1994-03-22
Ivy, C. Warren
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
549214, 549510, 549511, A01N 4302, C07D30500, C07D40700
Patent
active
052965066
ABSTRACT:
In a preferred embodiment, taxol is treated with mesyl chloride to prepare a taxol derivative with a contracted A-ring, which has comparable activity to taxol in a tubulin depolymerization assay, and which shows cytotoxicity against KB cells in a cell culture assay. In an alternate preferred embodiment, taxol is treated with triethyloxonium tetrafluoroborate (Meerwein's reagent) to produce a taxol derivative with an opened oxetane ring. In another alternate preferred embodiment, reaction of taxol with acetyl chloride yields a taxol derivative in which the oxetane ring is opened and the A-ring is contracted. All of the aforementioned products show in vivo activity in KB cell culture assays. Further, the preferred compounds have different in vivo activities, which makes them ideal to form a range of standards for use in biological testing of other compounds.
REFERENCES:
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Tetrahedron vol. 48, No. 34, pp. 6965-6974, 1992, "Rearrangement Reactions of Taxanes: Structural Modifications of 10-Deacetylbaccatin III".
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Fransworth, Norman, letter to J. Pharm. Sci., IV (1977).
Kingston David G. I.
Samaranyake Gamini
Covington Raymond
Ivy C. Warren
Virginia Tech Intellectual Properties Inc.
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