Preparation and cytotoxicity toward cancer cells of mono(arylimino) derivatives of β-lapachone

A regio- and stereospecific synthesis of monoarylimino o-quinones derived from β-lapachone (1) was achieved by treatment of the quinone with a slight excess of an arylamine in the presence of an excess of triethylamine/titanium tetrachloride 4:1. Imine formation occurred exclusively at position 6, g...

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Autor principal: Di Chenna, P.H
Otros Autores: Benedetti-Doctorovich, V., Baggio, R.F, Garland, M.T, Burton, G.
Formato: Capítulo de libro
Lenguaje:Inglés
Publicado: 2001
Acceso en línea:Registro en Scopus
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024 7 |2 scopus  |a 2-s2.0-0035913050 
024 7 |2 cas  |a 2,2-dimethyl-6-(4-methylphenylimino)-3,4,5,6-tetrahydro-2H-naphtho(1,2-b)oxin-5-one; 2,2-dimethyl-6-phenylimino-3,4,5,6-tetrahydro-2H-naphtho(1,2-b)oxin-5-one, 0; Antineoplastic Agents; Imines; Naphthalenes; Naphthoquinones; Pyrans; beta-lapachone, 4707-32-8 
040 |a Scopus  |b spa  |c AR-BaUEN  |d AR-BaUEN 
030 |a JMCMA 
100 1 |a Di Chenna, P.H. 
245 1 0 |a Preparation and cytotoxicity toward cancer cells of mono(arylimino) derivatives of β-lapachone 
260 |c 2001 
270 1 0 |m Burton, G.; Depto. de Quimica Orgánica, Facultad de Ciencias Exactas, Universidad de Buenos Aires, Pabellón 2, (1428) Buenos Aires, Argentina 
506 |2 openaire  |e Política editorial 
504 |a Burnett, A.R., Thomson, R.H., Naturally occurring quinones. Part X. The quinonoid constituents of tabebuia avellanedae (bignoniaceae) (1967) J. Chem. Soc. C, pp. 2100-2104 
504 |a Díaz, F., Medina, J.D., Furanonaphthoquinones from tabebuia ochracea ssp. neochrysanta (1996) J. Nat. Prod., 59, pp. 423-424 
504 |a Planchon, S.M., Wuerzberger, S., Frydman, B., Witiak, D.T., Hutson, P., Church, D.R., Wilding, G., Boothman, D.A., β-Lapachone-mediated apoptosis in human promyelocytic leukemia (HL-60) and human prostate cancer cells: A p53-independent response (1995) Cancer Res., 55, pp. 3706-3711 
504 |a Li, C.J., Wang, C., Pardee, A.B., Induction of apoptosis by β-lapachone in human prostate cancer cells (1995) Cancer Res., 55, pp. 3712-3715 
504 |a Boothman, D.A., Greer, S., Pardee, A.B., Potentiation of halogenated pyrimidine radiosensitizers in human carcinoma cells by β-lapachone (3,4-dihydro-2,2-dimethyl-2h-naphthol-[1,2-b]pyran-5,6-dione) a novel DNA repair inhibitor (1987) Cancer Res., 47, pp. 5361-5366 
504 |a Li, C.J., Averboukh, L., Pardee, A.B., β-lapachone, a novel DNA topoisomerase I inhibitor with a mode of action different from camptothecin (1993) J. Biol. Chem., 268, pp. 22463-22468 
504 |a Frydman, B., Marton, L.J., Sun, J.S., Neder, K., Witiak, D.T., Liu, A.A., Wang, H.-M., Liu, L.F., Induction of DNA topoisomerase II-mediated DNA cleavage by β-lapachone and related naphthoquinones (1997) Cancer Res., 57, pp. 620-627 
504 |a Li, C.J., Li, Y.-Z., Ventura Pinto, A., Pardee, A.B., Potent inhibition of tumor survival in vivo by β-lapachone plus taxol: Combining drugs imposes different artificial checkpoints (1999) Proc. Natl. Acad. Sci. U.S.A., 96, pp. 13369-13374 
504 |a Pink, J.J., Planchon, S.M., Tagliarino, C., Varnes, M.E., Siegel, D., Boothman, D.A., NAD(P)H:Quinone oxidoreductase activity is the principal determinant of β-lapachone cytotoxicity (2000) J. Biol. Chem., 275, pp. 5416-5424 
504 |a Schaffner-Sabba, K., Schmidt-Ruppin, K.H., Wehrli, W., Schuerch, A.R., Wasley, J.W.F., β-Lapachone: Synthesis of derivatives and activities in tumor models (1984) J. Med. Chem., 27, pp. 990-994 
504 |a Dolan, M.E., Frydman, B., Thompson, C.B., Diamond, A.M., Garbiras, B.J., Safa, A.R., Beck, W.T., Marton, L.J., Effects of 1,2-naphthoquinones on human tumor cell growth and lack of cross-resistance with other anticancer agents (1998) Anticancer Drugs, 9, pp. 437-448 
504 |a Muller, K., Sellmer, A., Wiergrebe, W., Potential antipsoriatic agents: Lapacho compounds as potent inhibitors of HaCaT cell growth (1999) J. Nat. Prod., 62, pp. 1134-1136 
504 |a Lown, J.W., Chen, H.-H., Plambeck, J.A., Acton, E.M., Diminished superoxide anion generation by reduced 5-iminodaunorubicin relative to daunorubicin and the relationship to cardiotoxicity of the anthracycline antitumor agents (1979) Biochem. Pharmacol., 28, pp. 2563-2568 
504 |a Benedetti-Doctorovich, V., Burgess, E.M., Lambropoulos, J., Lednicer, D., Van Derveer, D., Zalkow, L., Synthesis of 2-methyl-(z)-4-(phenylimino)naphth[2,3,d]oxazol-9-one, a monoimine quinone with selective toxicity toward cancer cells (1994) J. Med. Chem., 37, pp. 710-712 
504 |a Benedetti-Doctorovich, V., Escola, N., Burton, G., Preparation and NMR characterization of new substituted benzo[a]phenazines (1998) Magn. Reson. Chem., 36, pp. 529-532 
504 |a Boyd, M.R., Paull, K.D., Some practical considerations and applications of the national cancer institute in vitro anticancer drug discovery screen (1995) Drug Dev. Res., 34, pp. 91-109 
504 |a http://dtp.nci.nih.gov; Hollingshead, M.G., Alley, M.C., Camalier, R.F., Abbott, B.J., Mayo, J.G., Malspeis, L., Grever, M.R., In vivo cultivation of tumor cells in hollow fibers (1995) Life Sci., 57, pp. 131-141 
504 |a note; Frisch, M.J., Trucks, G.W., Schlegel, H.B., Scuseria, G.E., Robb, M.A., Cheeseman, J.R., Zakrzewski, V.G., Pople, J.A., (1998) Gaussian 98, revision A.7, , Gaussian, Inc.: Pittsburgh, PA 
504 |a Sheldrick, G.M., (1997) SHELXS-97. Program for Structure Resolution, , University of Göttingen, Germany 
504 |a Sheldrick, G.M., (1997) SHELXL-97. Program for Structure Refinement, , University of Göttingen, Germany 
504 |a Sheldrick, G.M., SHELXTL-PC, version 5.0, p. 1994. , Siemens Analytical X-ray Instruments, Inc.: Madison, WI 
504 |a Hooker, S.C., The Constitution of Lapachic Acid (Lapachol) and Synthesis of β-Lapachone (1892) J. Chem. Soc., pp. 611-650 
520 3 |a A regio- and stereospecific synthesis of monoarylimino o-quinones derived from β-lapachone (1) was achieved by treatment of the quinone with a slight excess of an arylamine in the presence of an excess of triethylamine/titanium tetrachloride 4:1. Imine formation occurred exclusively at position 6, giving the Z diastereomer, as determined by single-crystal X-ray analysis. In vitro tests for cytotoxicity in 55 human cancer cell cultures showed a substantial loss in activity for the p-nitrophenylimine (5), whereas the phenylimine (2), p-methylphenylimine (3), and p-methoxyphenylimine (4) retained (or bettered) most of the cytotoxicity and selectivity of the parent quinone. Preliminary in vivo testing in hollow fiber assays against a standard panel of 12 human tumor cell lines showed that although β-lapachone failed, compounds 2 and 3 had good scores with net cell kills.  |l eng 
593 |a Departamento de Química Orgánica, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Pabellón 2, (1428) Buenos Aires, Argentina 
593 |a Departamento de Física, Facultad de Ciencias Físicas y Matemáticas, Universidad de Chile, Avenida Blanco Encalada 2008, Casilla 487-3, Santiago, Chile 
593 |a Departamento de Física, Comisión Nacional de Energía Atómica, Avenida del Libertador 8250, (1429) Buenos Aires, Argentina 
690 1 0 |a 2,2 DIMETHYL 6 (4 METHYLPHENYLIMINO) 3,4,5,6 TETRAHYDRO 2H NAPHTHO[1,2 B]OXIN 5 ONE 
690 1 0 |a 2,2 DIMETHYL 6 PHENYLIMINO 3,4,5,6 TETRAHYDRO 2H NAPHTHO[1,2 B]OXIN 5 ONE 
690 1 0 |a ANTINEOPLASTIC AGENT 
690 1 0 |a BETA LAPACHONE DERIVATIVE 
690 1 0 |a UNCLASSIFIED DRUG 
690 1 0 |a ANTINEOPLASTIC ACTIVITY 
690 1 0 |a ARTICLE 
690 1 0 |a CANCER CELL CULTURE 
690 1 0 |a CANCER INHIBITION 
690 1 0 |a CONTROLLED STUDY 
690 1 0 |a CYTOTOXICITY 
690 1 0 |a DRUG MECHANISM 
690 1 0 |a DRUG STRUCTURE 
690 1 0 |a DRUG SYNTHESIS 
690 1 0 |a HUMAN 
690 1 0 |a HUMAN CELL 
690 1 0 |a ANTINEOPLASTIC AGENTS 
690 1 0 |a CRYSTALLOGRAPHY, X-RAY 
690 1 0 |a DRUG SCREENING ASSAYS, ANTITUMOR 
690 1 0 |a HUMANS 
690 1 0 |a IMINES 
690 1 0 |a MAGNETIC RESONANCE SPECTROSCOPY 
690 1 0 |a NAPHTHALENES 
690 1 0 |a NAPHTHOQUINONES 
690 1 0 |a PYRANS 
690 1 0 |a STEREOISOMERISM 
690 1 0 |a STRUCTURE-ACTIVITY RELATIONSHIP 
690 1 0 |a TUMOR CELLS, CULTURED 
700 1 |a Benedetti-Doctorovich, V. 
700 1 |a Baggio, R.F. 
700 1 |a Garland, M.T. 
700 1 |a Burton, G. 
773 0 |d 2001  |g v. 44  |h pp. 2486-2489  |k n. 15  |p J. Med. Chem.  |x 00222623  |w (AR-BaUEN)CENRE-686  |t Journal of Medicinal Chemistry 
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856 4 0 |u https://doi.org/10.1021/jm010050u  |y DOI 
856 4 0 |u https://hdl.handle.net/20.500.12110/paper_00222623_v44_n15_p2486_DiChenna  |y Handle 
856 4 0 |u https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00222623_v44_n15_p2486_DiChenna  |y Registro en la Biblioteca Digital 
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