Adriamycin , anticancer drug

Yokoyama, M., Miyauchi, M., Yamada, N., Okano, T., Sakurai, Y, Kataoka, K., and Inoue, S. Characterization and anticancer activity of the micelle-forming polymeric anticancer drug adriamycin-conjugated poly(ethylene glycol)-poly(aspartic acid) block copolymer. Cancer Res., 1990, 50, 1693-1700. 

Fig. 10b. A scheme of its synthesis. First, a reactive comonomer. Af-methacryloylglycyl-phenylalanylleucylgycine p-nitrophenyl ester was synthesized. In the second step a polymeric precursor is prepared by copolymerization of the reactive comonomer with A-(2-hydroxyp-ropyl)methacrylamide. After purification and characterization of the polymeric precursor, the anticancer drug (adriamycin) and targeting moiety (galactosamine) are attached by consecutive aminolysis. For details see, e.g., [169]...

Tertiary amine oxides and hydroxy la mines are also reduced by cytochromes P-450. Hydroxylamines, as well as being reduced by cytochromes P-450, are also reduced by a flavoprotein, which is part of a system, which requires NADH and includes NADH cytochrome b5 reductase and cytochrome b5. Quinones, such as the anticancer drug adriamycin (doxorubicin) and menadione, can undergo one-electron reduction catalyzed by NADPH cytochrome P-450 reductase. The semiquinone product may be oxidized back to the quinone with the concomitant production of superoxide anion radical, giving rise to redox cycling and potential cytotoxicity. This underlies the cardiac toxicity of adriamycin (see chap. 6). 

Figure 5-23 Stereoscopic drawing showing a molecule of daunomycin (Fig. 5-22) intercalated between two base pairs in a molecule of double-helical DNA, d(CGTACG). Nitrogen and oxygen atoms are shown as dots. From Quigley et al.220 Both daunomycin and adriamycin (doxorubicin 14-hydroxy-daunomycin) are important but seriously toxic anticancer drugs.

This anticancer drug causes the scission of single-strand DNA amongst its various biological properties. Here, too, the reaction involves binding of Fe11 by adriamycin and the reduction of... 

Next, some typical examples will be presented of how a DNA-electrochemical biosensor is appropriate to investigate the DNA damage caused by different types of substances, such as the antioxidant agent quercetin (Scheme 20.1), an anticancer drug adriamycin (Scheme 20.2) and nitric oxide. In all cases, the dsDNA damage is detected by changes in the electrochemical behaviour of the immobilized dsDNA, specifically through modifications of the purinic base oxidation peak current [3,5,40]. 

Some common anticancer drug combinations and the types of cancer in which they are used are listed in Table 36-8. These drug combinations are often indicated by an acronym of the drug names. For instance, FAC indicates a regimen of fluorouracil, doxorubicin (Adriamycin), and cyclophosphamide. These abbreviations are used to summarize drug therapy in a patient s medical chart, so therapists should be aware of the more common chemotherapy combinations. 

TFP (5) was the first phenothiazine demonstrated to modulate MDR in drug-resistant P338 murine leukemia cells. TFP (5) enhanced intracellular accumulation of vincristine and adriamycin (77) in resistant tumor cells by inhibiting outward transport of these anticancer drugs [167]. Studies per-... 

A variety of plant substances with planar, polycyclic, aromatic structures can intercalate with DNA, examples being the quinoline alkaloid camptothecin and the furanocoumarin phenolic psoralen (Table 12.1). A variety of plant-derived anthraquinones and naphthoquinones bind to DNA and it is notable that the structurally related anthraquinones mitox-antrone and adriamycin are clinically employed as anticancer drugs (Table 12.1). DNA-binding compounds that interfere with DNA repair, DNA replication and gene expression are cytotoxic and have potential as anticancer agents (see Chapter 9). 

Frederick CA, Williams LD, Ughetto G, Van der Marel GA, Van 76. Boom JH, Rich A, Wang AHJ. Structural comparison of anticancer drug-DNA complexes adriamycin and daunomycin. Biochemistry... 

Furthermore, there are reports that dipyridamole (see ref 182 and literature cited therein) and mopidamol (RA-233 2, R1 = H) 183 - 1 86 inhibit the growth of certain tumor cells, increases the cytotoxicity of several anticancer drugs, and restores the sensitivity to adriamycin in drug resistant cells. The inhibitory activities towards platelet aggregation of dipyridamole derivatives such as copolymers with /V-vinylpyrrolidone187 and dipyridamole esters188 have also been studied. Piperidinoamino-substituted pyrimido[5,4- f]pyrimidines are also useful as blood-... 

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