Synthesis and evaluation of hapalosin and analogs as MDR-reversing agents

被引：29

作者：

O'Connell, CE ^{[1
]}

Salvato, KA ^{[1
]}

Meng, ZY ^{[1
]}

Littlefield, BA ^{[1
]}

Schwartz, CE ^{[1
]}

机构：

[1] Eisai Res Inst, Andover, MA 01810 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 11期

关键词：

D O I：

10.1016/S0960-894X(99)00243-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The marine natural product hapalosin and 22 analogs, which incorporated systematic substituent deletions or variations, were prepared. These compounds were evaluated in a cell-based assay for both MDR-reversing activity and general cytotoxicity. Some substituent modifications resulted in lower cytotoxicities, but most structural changes were either detrimental to or did not seriously alter the MDR-reversing activity. (C) 1999 Elsevier Science Ltd. All rights reserved.

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页码：1541 / 1546

页数：6

相关论文

共 27 条

[11] Cellular and biochemical characterization of VX-710 as a chemosensitizer: Reversal of P-glycoprotein-mediated multidrug resistance in vitro [J].

Germann, UA ;

Shlyakhter, D ;

Mason, VS ;

Zelle, RE ;

Duffy, JP ;

Galullo, V ;

Armistead, DM ;

Saunders, JO ;

Boger, J ;

Harding, MW .

ANTI-CANCER DRUGS, 1997, 8 (02) :125-140

[12]

GHOSH A, COMMUNICATION

[13] A convergent, enantioselective total synthesis of hapalosin: A drug with multidrug-resistance reversing activity [J].

Ghosh, AK ;

Liu, WM ;

Xu, YB ;

Chen, ZD .

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION IN ENGLISH, 1996, 35 (01) :74-76

[14] TOTAL SYNTHESIS OF (+/-)-PLEUROMUTILIN [J].

GIBBONS, EG .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1982, 104 (06) :1767-1769

[15] MILD CLEAVAGE OF METHOXYMETHYL (MOM) ETHERS WITH TRIMETHYLSILYL BROMIDE [J].

HANESSIAN, S ;

DELORME, D ;

DUFRESNE, Y .

TETRAHEDRON LETTERS, 1984, 25 (24) :2515-2518

[16] SYNTHETIC STUDIES OF DIDEMNINS .3. SYNTHESES OF STATINE AND ISOSTATINE STEREOISOMERS [J].

HARRIS, BD ;

JOULLIE, MM .

TETRAHEDRON, 1988, 44 (12) :3489-3500

[17] RESTORATION OF TAXOL SENSITIVITY OF MULTIDRUG-RESISTANT CELLS BY THE CYCLOSPORINE SDZ PSC-833 AND THE CYCLOPEPTOLIDE SDZ-280-446 [J].

JACHEZ, B ;

NORDMANN, R ;

LOOR, F .

JOURNAL OF THE NATIONAL CANCER INSTITUTE, 1993, 85 (06) :478-483

[18]

MERLIN JL, 1994, BLOOD, V84, P262

[19] RAPID COLORIMETRIC ASSAY FOR CELLULAR GROWTH AND SURVIVAL - APPLICATION TO PROLIFERATION AND CYTO-TOXICITY ASSAYS [J].

MOSMANN, T .

JOURNAL OF IMMUNOLOGICAL METHODS, 1983, 65 (1-2) :55-63

[20] Dendroamides, new cyclic hexapeptides from a blue-green alga. Multidrug-resistance reversing activity of dendroamide A [J].

Ogino, J ;

Moore, RE ;

Patterson, GML ;

Smith, CD .

JOURNAL OF NATURAL PRODUCTS, 1996, 59 (06) :581-586