Vinca alkaloid photoactive analogs and their uses

Details Vinca alkaloid photoactive analogs and their uses Vinca alkaloid photoactive analogs and their uses

1986-04-03

1988-08-23

Rizzo, Nicholas S.

Drug, bio-affecting and body treating compositions

Radionuclide or intended radionuclide containing; adjuvant...

435 35, 540478, A61K 4300, C07D51904

Patent

active

047659726

ABSTRACT:
Pharmacologically active, radioactive, and photoactive vinblastine analogs are provided which can be used to bind covalently to cellular polypeptides which have high affinity for Vinca alkaloids. The compounds are N-(p-azido[3,4-.sup.3 H]benzoyl)-N'beta-aminoethylvindesine and N-p-azido-[3-.sup.125 I]-salicyl-N'-beta-aminoethylvindesine. The compounds can be used to identify cellular Vinca alkaloid receptors which may be involved in antineoplastic, cytotoxic and drug resistant mechanisms of actions. In addition to specific interaction with tubulin, these compounds specifically bind to a 150-180 kDa surface membrane glycoprotein which is overexpressed in multidrug resistant cells.

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Cornwell, et al., Chemical Abstracts, vol. 105, 108022j, (1986), abstract of Proc. Natl. Acad. Sci. U.S.A., 1986, 83(11), pp. 3847-3850.
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Safa, et al., Biochemistry, vol. 26, No. 1, pp. 97-102, (01/13/87).
Safa, et al., J. Biological Chemistry, vol. 262, No. 3, pp. 1261-1267, (01/25/87).

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