Modulator agent and use thereof

Details Modulator agent and use thereof Modulator agent and use thereof

1992-06-19

1994-11-29

Waddell, Frederick E.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

A61K 3144

Patent

active

053691113

ABSTRACT:
Sensitizing tumoral cells to anticancerous drugs and/or inhibiting the tumoral cells resistance to antitumoral drugs employing as a modulator agent a vinca alkaloid dimer, analog to vinblastine or vincristine, with a low cytotoxicity or devoid of cytotoxicity, comprising at least one stereoisomerism different from that of vinblastine or vincristine in the C-14', C-16' or C-20' position. Notably, the modulator agent may have the R absolute configuration in the C-16' position.

REFERENCES:
patent: 4746665 (1988-05-01), Szantay
Inaba, M., et al, Non-Antitumor Vinca Alkaloids Reverse Multidrug Resistance in P388 Leukemia Cells in Vitro, Jpn.J.Cancer Res., (Gann), 77, 197-204; Feb. 1986.
Kuehne et al "Three Routes to the Critical C16'-C14 Part relative Stereo-Chemistry of vinblastine . . . " J. Org. Chem. 52: 4340-4349 (1987).
Borman & Kuehne "Specific alterations in the biological activities of C-20'-modified vinblastine congeners" Biochemical Pharmacology 38(5) 715-724 (Mar. 1, 1989).
"Non-antitumor vinca alkaloids reverse multidrug resistance in P388 Leukemia cells in vitro," Chemical Abstracts CA 104(21):179840q, Inaba, Published 1986.
The Pharmacological Basis of Therapeutics, Goodman and Gilman, Eds., pp. 1284-1285, Publsihed in 1975.

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