geoscience.net logo
+ Resolve Article
+ Follow Us
Follow on FacebookFollow on Facebook
Follow on TwitterFollow on Twitter

+ Translate
+ Subscribe to Site Feed
GeoScience Most Shared ContentMost Shared Content

Effects of new antitumor bifunctional intercalators derived from 7H-pyridocarbazole on sensitive and resistant L 1210 cells


, : Effects of new antitumor bifunctional intercalators derived from 7H-pyridocarbazole on sensitive and resistant L 1210 cells. Cancer Research 44(10): 4355-4360

The antitumor properties of 7H-pyridocarbazole dimers, a new series of bifunctional intercalators, have recently been described (Pelaprat, D. Delbarre, A., Le Guen, I., Roques, B. P., and Le Pecq, J. B. J. Med. Chem., 23: 1336-1343, 1980; and Roques, B. P., Pelaprat, D., Le Guen, I., Porcher, G., Gosse, C., and Le Pecq, J. B. Biochem. Pharmacol., 28: 1811-1815, 1979). In order to study the mechanism of action of these compounds, an L1210 subline was made resistant to one dimer (NSC 335153; ditercalinium). Selection of resistant cells was based on an in vitro-in vivo procedure as follows. Ascitic cells were taken from a leukemic mouse and incubated in vitro with the dimer for 1 hr. They were then injected into mice. After the development of the ascites, L1210 cells were collected and the process was repeated 13 times, until establishment of the resistance. Cloned resistant cells have maintained their resistance for 18 months of in vitro culture. The effects of two dimers (NSC 335153 and NSC 335154) on cell viability, growth, colony formation, and cell cycle progression were investigated on parental and resistant L1210 cells. The cross-resistance of these two L1210 cell lines to several cytotoxic agents was estimated. Several observations indicate that the mechanism of action of these dimers might be different from that of monointercalating agents: (a) these drugs induce a delayed toxicity (growth arrest occurring five generations after drug exposure) in sensitive but not in resistant cells; (b) cells exposed to the dimers arrested almost randomly in all phases of the cell cycle, whereas the corresponding monomer provokes a block in the G2 + M phase. Resistant cells were cross-resistant to 7H-pyridocarbazole monomer, Adriamycin, and vincristine but not to 6H-pyridocarbazole monomer derivatives, actinomycin D, and methotrexate.

US$29.90

PMID: 6467197


Other references

Smith, W.H., 1969: Release of organic materials from the roots of tree seedlings. In a laboratory experiment, the root exudates of 18-day-old Pinus radiata, P. lambertiana, P. banksiana, P. rigida and Robinia pseudoacacia grown in test-tubes were analysed by thin-layer chromatography for the presence of organic materials includ...

Hesse, K.A., 1995: Ethical issues and terminal management of the old old. Journal of Geriatric Psychiatry 28(1): 75-95

Kennedy O.G.; Collignon S.J.; Protte D.J., 1981: Impact of medical information systems on health care in the usa. Lindberg, D A B And S Kaihara Ifip (International Federation For Information Processing) World Conference Series on Medical Informatics, Vol 3 Medinfo 80 Parts 1 And 2; Proceedings Of The 3rd World Conference on Medical Informatics, Tokyo, Japan, Sept 29-Oct 4, 1980 Xxxv+748p (Part 1); Xxv+630p (Part 2) North-Holland Publishing Co : Amsterdam, Netherlands; New York, N Y , Usa Illus P1058-1062, 1980

Drescher, H., 1955: Supervision of treated gynecological neoplasms. Die Medizinische 21: 773-776

Vohora, D.; Pal, S.N.; Pillai, K.K., 2001: Histaminergic H3-receptors as modulators of CNS function. There is an increasing evidence that the biogenic amine histamine acts as a neurotransmitter in mammalian brain. The discovery of the third histamine receptor and its highly potent and selective ligands have clarified various aspects of histaminer...

Revi, D.; Geetha, C.; Thekkuveettil, A.; Anilkumar, T.V., 2015: Fibroblast-loaded cholecyst-derived scaffold induces faster healing of full thickness burn wound in rabbit. Graft-assisted healing is often proposed for clinical management of large-sized third-degree cutaneous burn wounds. Skin-graft substitutes prepared by loading appropriate cell types on suitable scaffolds have been found successful. We have previou...

Bardy, G.H.; Yee, R.; Jung, W., 1996: Multicenter experience with a pectoral unipolar implantable cardioverter-defibrillator. Active Can Investigators. The purpose of this study was to prospectively examine in a multicenter study the methods of use, efficacy and complications of a unipolar cardioverter-defibrillator in patients at risk for sudden cardiac death. Implantation of cardioverter-defibr...

Magcale Macandog, D.B.; Delgado, M.E.M.; Ty, E.; Villarin, J.R.T., 2006: A GIS-based model to improve estimation of aboveground biomass of secondary forests in the Philippines. A geographic information system (GIS)-based model was developed to spatially predict the aboveground biomass of secondary forests in the Philippines. A database of the physical (soil type, slope, elevation) and climatic (agroclimate zone, annual r...

Grover, C.E.; Kim, H.; Wing, R.A.; Paterson, A.H.; Wendel, J.F., 2004: Incongruent patterns of local and global genome size evolution in cotton. Genome sizes in plants vary over several orders of magnitude, reflecting a combination of differentially acting local and global forces such as biases in indel accumulation and transposable element proliferation or removal. To gain insight into th...

Anonymous, 2012: Multiple Steps for OR Translocation and Activation. Odorant receptor (OR) proteins are retained in the endoplasmic reticulum when heterologously expressed in cultured cells of non-olfactory origins. RTP1S is an accessory protein to mammalian ORs and facilitates their trafficking to the cell-surface...