Multidrug reversal

Recent studies on multidrug reversal in mouse lymphoma and MDR/COLO 320 cells have shown that phenothiazine derivatives, namely perphenazine (2) and prochlorperazine dimaleate (4), effectively inhibited rhodamine efflux [171]. Other phenothiazine derivatives such as promethazine (1), ox-omemazine (20), methotrimeprazine maleate (18), triflupromazine (11), and trimeprazine (17) differently modulated intracellular rhodamine accumulation in these resistant cells. The effect of some substitution in the phenothiazine ring was studied in mouse lymphoma cells expressing P-gp [172], The 3,7,8-trihydroxy- and 7,8-dihydroxychlorpromazine derivatives were effective P-gp inhibitors, whereas 7,8-diacetoxy-, 7,8-dimethoxy-, 7-semicarbazone-, and 5-oxo-chlorpromazine derivatives exerted only a moderate effect. [Pg.267]

The multidrug resistance (mdr) reversing effect of the new phenothiazine complexes were tested on mouse T cell lymphoma cell lines. Trifluoperazine (TFP) was much more effective at the same concentration than verapamil. The efficacy of some metal coordination complexes [TFP-Cu(ll) and TFP-V(IV)] exceeded the action of TFP alone. Chlorpromazine (CPZ) or CPZ-Pt(ll) complex had the same or less effect than verapamil or promethazine (Pz) used as a control. [Pg.429]

An example of a valid, easily interpretable QSAR is that relating to P-glycoprotein-regulated multidrug resistance reversal (MDRR) by phenothi-azines [43] ... [Pg.477]

Dearden JC, AI-Noobi A, Scott AC, Thomson SA. QSAR studies on P-glycoprotein-regulated multidrug resistance and on its reversal by phenothia-zines. SAR QSAR Environ Res 2003 14 447-54. [Pg.490]

As mentioned previously, the Stille reaction can also be combined with an elec-trocyclization. Trauner and coworkers [99] used this approach for the synthesis of a part of SNF4435C (6/1-190) and its natural diastereomer. SNF4435C, which was isolated from the culture broth of an Okinawan strain of Streptomyces spectabilis, acts as an immunosuppressant and multidrug resistance reversal agent [100]. In order to form the annulated cyclobutane skeleton in 6/1-190, the vinyl iodide... [Pg.390]

Williams, A.B. and Jacobs, R.S. (1993) A marine natural product, patellamide D, reverses multidrug resistance in a human leukemic cell line. Cancer Letters, 71, 97. [Pg.260]

The fungal metabolite, 5-A-acetylardeemin, possessing a hexacyclic structure with a l,4-dihydro-3,6-dioxo-pyra-zino[2,l-A]quinazoline skeleton, is the best multidrug resistance reversal agent known to date <1998MI45>. Hexahydro-3,6-dioxo-pyrazino[2,l-7]quinazolines have been claimed as endothelial nitric oxide synthetase regulators useful in the treatment of cardiovascular disorders <2004EP1471066>. [Pg.293]

Wiese, M., Pajeva, I. K., Structure-activity relationships of multidrug resistance reversers, Curr. Med. Chem. 2001, 8, 685-713. [Pg.489]

Klopman, G., Shi, L. M., Ramu, A., Quantitative structure-activity relationship of multidrug resistance reversal agents, Mol. Pharmacol. 1997, 52, 323-334. [Pg.489]

G., Raschack, M., Cappelletto, B., Gigante, M., Boiocchi, M., Structure—activity relationship of verapamil analogs and reversal of multidrug resistance, Biochem. Pharmacol. 1995, 50, 1245-1255. [Pg.492]

Ford, J. M., Prozialeck, W. C., Hait, W. N., Structural features determining activity of phenofhiazines and related drugs for inhibition of cell growth and reversal of multidrug resistance, Mol. Pharmacol. 1989, 35, 105-115. [Pg.492]

Hyafil, F., Vergely, C., Du Vignaud, P., Grand-Perret, T., In vitro and in vivo reversal of multidrug resistance by GF120918, an acridonecarboxamide derivative, Cancer Res. 1993, 53, 4595— 4602. [Pg.492]

Huet, S., Chapey, C., Robert, J., Reversal of multidrug resistance by a new lipophilic cationic molecule,... [Pg.493]

Reversal of P-glycoprotein-mediated multidrug resistance by XR9051, a novel diketopiperazine derivative, Br. [Pg.493]

Sato, W., Fukazawa, N., Nakanishi, O., Baba, M., Suzuki, T., Yano, O., Naito, M., Tsuruo, T., Reversal of multidrug resistance by a novel... [Pg.493]

Roe, M., Folkes, A., Ashworth, P., Brumwell, J., Chima, L., Hunjan, S., Pretswell, I., Dangerfield, W., Ryder, H., Charlton, P., Reversal of P-glycoprotein mediated multidrug resistance by novel anthranilamide derivatives, Bioorg. Med. Chem. Lett. 1999, 9, 595-600. [Pg.493]

J. P., Galullo, V., Armistead, D. M., Saunders, J. O., Boger, J., Harding, M. W., Cellular and biochemical characterization of VX-710 as a chemosensitizer reversal of P-glycoprotein-mediated multidrug resistance in vitro, Anticancer Drugs 1997, 8, 125-140. [Pg.493]

As described in several monographs [4], bryostatin 1 exhibits significant in vitro and in vivo antineoplastic activity against a range of tumor cell lines including murine leukemia, B-cell lymphoma, reticulum cell sarcoma, ovarian carcinoma, and melanoma. It is also effective in the modulation of apoptotic function [5], the reversal of multidrug resistance [6], and stimulation of the immune system [7]. These unique features displayed by bryostatin 1 are attributed to its high affinity for protein kinase C (PKC) isozymes and its ability to selectively modulate their functions [8]. PKCs are a type of intracellular serine and threonine kinase that... [Pg.104]

Braybrooke JP, Vallis KA, Houlbrook S, Rockett H, Ellmen J, Anttila M, Ganesan TS, Harris AL, Talbot DC (2000) Evaluation of toremifene for reversal of multidrug resistance in renal cell cancer patients treated with vinblastine. Cancer Chemother Pharmacol 46(1) 27—34... [Pg.109]

Li J, Xu LZ, Yao JJ, Guo WJ, Xia P, Chen Y (2001a) Reversal effects of droloxifene on multidrug resistance in adriamycin-resistant K562 cell line. Acta Pharmacol Sin 22(11) 1023—1027... [Pg.112]

Trump DL, Smith DC, Ellis PG, Rogers MP, Schold SC, Winer EP, Panella TJ, Jordan VC, Fine RL (1992) High-dose oral tamoxifen, a potential multidrug-resistance-reversal agent Phase I trial in combination with vinblastine. J Natl Cancer Inst 84 1811-1816... [Pg.114]

Wadleigh RW, Yu SJ (1988) Detoxification of iso thiocyanate allelochemicals by glutathione transferase in three lepidopterous species. J Chem Ecol 14 1279-1288 Werck-Reichhart D, Feyereisen R (2000) Cytochromes P450 a success story. Genome Biol 1 1-9 Williams AB, Jacobs RS (1993) A marine natural product, patellamide D, reverses multidrug resistance in a human leukemic cell line. Cancer Lett 71 97-102 Yazaki K (2006) ABC transporters involved in the transport of plant secondary metabolites. FEBS Lett 580 1183-1191... [Pg.228]

Bellamy, W.T., Dalton, W.S., Kailey, J.M., Gleason, M.C., McCloskey, T.M., Dorr, R. T. and Alberts, D.S. (1988) Verapamil reversal of doxorubicin resistance in multidrug-resistant human myeloma... [Pg.362]

Ford, J.M., Bruggemann, E.P., Pastan, I., Gottesman, M.M. and Hait, W.N. (1990) Cellular and biochemical characterization of thioxanthenes for reversal of multidrug resistance in human and murine cell lines. Cancer Research, 50, 1748-1756. [Pg.394]

Bogman K, Erne-Brand F, Alsenz J, Drewe J (2003) The role of surfactants in the reversal of active transport mediated by multidrug resistance proteins. J Pharm Sci 92 1250-1261. [Pg.207]

Y. Imai, S. Tsukahara, E. Ishikawa, T. Tsuruo, and Y. Sugimoto. Estrone and 17beta-estradiol reverse breast cancer resistance protein-mediated multidrug resistance. Jpn J Cancer Res Gann. 93 231-235 (2002). [Pg.395]

Lavie, Y., Cao, H-t., Volner, A., Lucci, A., Han, T. Y., Geffen, V., Giuhano, A. E., and Cabot, M. C., 1997, Agents that reverse multidrug resistance, tamoxifen, verapamil, and cyclosporin A, block glycosphingolipid metabohsm by inhibiting ceramide glycosylation in human cancer cells. J. Biol. Chem. 272 1682-1687. [Pg.281]

Brooks T, Minderman H, O Loughlin KL, Pera P, Ojima 1, Baer MR, Bemacki RJ. (2003) Taxane-based reversal agents modulate drug resistance mediated by P-glycoprotein, multidrug resistance protein, and breast cancer resistance protein. Mol Cancer Ther 2 1195-1205. [Pg.169]

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