Reversal of P-glycoprotein mediated multidrug resistance by novel anthranilamide derivatives

被引：150

作者：

Roe, M ^{[1
]}

Folkes, A ^{[1
]}

Ashworth, P ^{[1
]}

Brumwell, J ^{[1
]}

Chima, L ^{[1
]}

Hunjan, S ^{[1
]}

Pretswell, I ^{[1
]}

Dangerfield, W ^{[1
]}

Ryder, H ^{[1
]}

Charlton, P ^{[1
]}

机构：

[1] Xenova Ltd, Slough SL1 4EF, Berks, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 04期

关键词：

D O I：

10.1016/S0960-894X(99)00030-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have synthesised and evaluated a series of anthranilamide based modulators of P-glycoprotein. These studies have identified XR9576(2), a potent inhibitor of P-glycoprotein in vitro and in vivo. The general synthesis and the SAR of these compounds are described. (C) 1999 Elsevier Science Ltd. All rights reserved.

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页码：595 / 600

页数：6

相关论文

共 12 条

[1]

Boer Rainer, 1995, Drugs of the Future, V20, P499

[2] Reversal of P-glycoprotein-mediated multidrug resistance by XR9051, a novel diketopiperazine derivative [J].

Dale, IL ;

Tuffley, W ;

Callaghan, R ;

Holmes, JA ;

Martin, K ;

Luscombe, M ;

Mistry, P ;

Ryder, H ;

Stewart, AJ ;

Charlton, P ;

Twentyman, PR ;

Bevan, P .

BRITISH JOURNAL OF CANCER, 1998, 78 (07) :885-892

[3]

Dantzig AH, 1996, CANCER RES, V56, P4171

[4] NEW TRIAZINE DERIVATIVES AS POTENT MODULATORS OF MULTIDRUG RESISTANCE [J].

DHAINAUT, A ;

REGNIER, G ;

ATASSI, G ;

PIERRE, A ;

LEONCE, S ;

KRAUSBERTHIER, L ;

PROST, JF .

JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (13) :2481-2496

[5] SYNTHESIS AND ACTIVITY AGAINST MULTIDRUG-RESISTANCE IN CHINESE-HAMSTER OVARY CELLS OF NEW ACRIDONE-4-CARBOXAMIDES [J].

DODIC, N ;

DUMAITRE, B ;

DAUGAN, A ;

PIANETTI, P .

JOURNAL OF MEDICINAL CHEMISTRY, 1995, 38 (13) :2418-2426

[6] 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

[7] BIOCHEMISTRY OF MULTIDRUG-RESISTANCE MEDIATED BY THE MULTIDRUG TRANSPORTER [J].

GOTTESMAN, MM ;

PASTAN, I .

ANNUAL REVIEW OF BIOCHEMISTRY, 1993, 62 :385-427

[8] STRUCTURALLY DISTINCT MDR MODULATORS SHOW SPECIFIC PATTERNS OF REVERSAL AGAINST P-GLYCOPROTEINS BEARING UNIQUE MUTATIONS AT SERINE(939/941) [J].

KAJIJI, S ;

DRESLIN, JA ;

GRIZZUTI, K ;

GROS, P .

BIOCHEMISTRY, 1994, 33 (17) :5041-5048

[9]

Mistry P, 1998, ANN ONCOL, V9, P148

[10] A NEW SYNTHESIS OF LUCANTHONE (MIRACIL D, NILODIN) [J].

SHARP, TM .

JOURNAL OF THE CHEMICAL SOCIETY, 1951, (NOV) :2961-2963