Mammalian DNA topoisomerase II inhibitor and method

Details Mammalian DNA topoisomerase II inhibitor and method Mammalian DNA topoisomerase II inhibitor and method

1993-03-18

1995-06-20

Kumar, Shailendra

Organic compounds -- part of the class 532-570 series

Organic compounds

Amino nitrogen containing

564174, 564176, 564212, 564213, C07C23365

Patent

active

054262240

ABSTRACT:
A novel antiproliferative drug and methods are disclosed. The drug has the general structural formula: ##STR1## where R1=OR.sub.1 ', SR.sub.1 ', or N(R.sub.1 'R.sub.1 ").sub.2, where R.sub.1 ' and R.sub.1 " are H or lower alkyl groups, and R.sub.2 is an acylamino, or aroylamino group. The compound is useful for inhibiting cell proliferation in drug-resistant tumor cells. Also disclosed is a method of chemical converting a colchicine derivative to form an active inhibitor of DNA topisomerase II.

REFERENCES:
Brossi, A., "Bioactive Alkaloids. 4. Results of Recent Investigations with Colchicine and Physostigmine," J. Med. Chem. 33(9):2311-2319 (1990).
Capraro, H-G., and A. Brossi, "99. Simple Conversion of Colchicine into Demecolcine," Helvetica Chimica Acta 62:965-970 (1979).
D'Arpa, P., and L. F. Liu, "Topoisomerase-targeting antitumor drugs," Biochim. Biophys. Acta 989:163-177 (1989).
Liu, L. F., et al., "Cleavage of DNA by Mammalian DNA Topoisomerase II," J. Biolog. Chem. 258(24):15365-15370 (1983).
Pastan, I., and M. Gottesman, "Multiple-Drug Resistance in Human Cancer," New Eng. J. Med., May 28:1388-1399 (1987).
Rowe, T. C., et al., "DNA Damage by Antitumor Acridines Mediated by Mammalian DNA Topoisomerase II," Cancer Res. 46:2021-2026, 1986.
Tatematsu, H., et al., "Anti-AIDS Agents. 3. Inhibitory Effects of Colchicine Derivatives on HIV Replication in H9 Lymphocyte Cells," J. Nat. Prod. 54(2):632-637 (1991).
Yang, L-Y., and J. M. Trujillo, "Biological Characterization of Multidrug-resistant Human Colon Carcinoma Sublines Induced/Selected by Two methods," Cancer Res. 50:3218-3225 (1990).

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