Antitumor activity of 4-amino and 8-methyl-4-(3diethylamino propylamino)pyrimido[4′,5′:4,5]thieno (2,3-b) quinolines
作者： M Gopal , S Shenoy , L.S Doddamani
DOI: 10.1016/J.JPHOTOBIOL.2003.09.003
关键词:
摘要: The interaction of 4-aminopyrimido [4′,5′:4,5] thieno (2,3-b) quinoline and 8-methyl-4-(3-diethylaminopropylamino) pyrimido with DNA was studied by UV–Vis fluorescence spectrophotometry as well hydrodynamic methods. On binding to DNA, the absorption spectra underwent bathochromic hypochromic shifts quenched. These compounds are able bind an affinity about 106 M−1 for calf thymus at ionic strength 0.01 M their intercalating characteristic (lengthening DNA) depends upon length chain. Binding GC-rich Micrococcus lysodeikticus stronger than M. cytotoxicities these on leukemia HL-60, melanoma B16F10 neuro 2a cells quite similar inhibition (IC50) is in range 0.992–3.968 μM. anticancer efficacy against B16 melanoma, has provided evidence major antitumor activity 8-methyl-4-(3diethylaminopropylamino) thieno(2,3-b)quinoline. Single or multiple intraperitonial (i.p) doses drug proved high level subcutaneous (s.c) grafted significantly increasing survival (p<0.001) inhibiting tumor growth (T/C 4%). This study offers a new intercalation functional group – targeted design.
elsevier.com
sci-hub.se 参考文章(31)
Drug action at the molecular level Macmillan , University Park Press. ,(1977) , 10.1007/978-1-349-03230-3
J.M. Saucier, B. Festy, J.-B. Le Pecq, The change of the torsion of the DNA helix caused by intercalation. II. Measurement of the relative change of torsion induced by various intercalating drugs. Biochimie. ,vol. 53, pp. 973- 980 ,(1971) , 10.1016/S0300-9084(71)80065-2
François Denizot, Rita Lang, Rapid colorimetric assay for cell growth and survival. Modifications to the tetrazolium dye procedure giving improved sensitivity and reliability. Journal of Immunological Methods. ,vol. 89, pp. 271- 277 ,(1986) , 10.1016/0022-1759(86)90368-6
Françoise Guéritte-Voegelein, François Lavelle, Daniel Guénard, Marie-Christine Bissery, Experimental Antitumor Activity of Taxotere (RP 56976, NSC 628503), a Taxol Analogue Cancer Research. ,vol. 51, pp. 4845- 4852 ,(1991)
S.P. Langdon, H.R. Hendriks, B.-J.M. Braakhuis, G. Pratesi, D.P. Berger, Ø. Fodstad, H.H. Fiebig, E. Boven, Preclinical phase II studies in human tumor xenografts: A European multicenter follow-up study Annals of Oncology. ,vol. 5, pp. 415- 422 ,(1994) , 10.1093/OXFORDJOURNALS.ANNONC.A058872
Christian Auclair, Emmanuelle Voisin, Helene Banoun, Claude Paoletti, Jean Bernadou, Bernard Meunier, Potential antitumor agents: synthesis and biological properties of aliphatic amino acid 9-hydroxyellipticinium derivatives Journal of Medicinal Chemistry. ,vol. 27, pp. 1161- 1166 ,(1984) , 10.1021/JM00375A013
Adriana Baez, Fernando A. González, David Vázquez, Michael J. Waring, Interaction between A 3-nitrobenzothiazolo (3,2-a) quinolinium antitumour drug and deoxyribonucleic acid Biochemical Pharmacology. ,vol. 32, pp. 2089- 2094 ,(1983) , 10.1016/0006-2952(83)90431-8
Eva Frei, Christian A Bieler, Volker M Arlt, Manfred Wiessler, Marie Stiborová, Covalent binding of the anticancer drug ellipticine to DNA in V79 cells transfected with human cytochrome P450 enzymes Biochemical Pharmacology. ,vol. 64, pp. 289- 295 ,(2002) , 10.1016/S0006-2952(02)01072-9
Michael Waring, Variation of the supercoils in closed circular DNA by binding of antibiotics and drugs: evidence for molecular models involving intercalation. Journal of Molecular Biology. ,vol. 54, pp. 247- 279 ,(1970) , 10.1016/0022-2836(70)90429-8
Claire Ducrocq, Francoise Wendling, Jean Claude Chermann, Martine Tourbez-Perrin, Christian Rivalle, Pierre Tambourin, Francois Pochon, Emile Bisagni, Structure-activity relationship in a series of newly synthesized 1-amino-substituted ellipticine derivatives Journal of Medicinal Chemistry. ,vol. 23, pp. 1212- 1216 ,(1980) , 10.1021/JM00185A012