Antitumour drug

The 1- and 3-deaza analogues (463a, 463b) of the DHFR-inhibitory antitumour drug methotrexate have also been investigated (71JOC2818). 

Platinum complexes probes of polynucleotide structure and antitumour drugs. S. J. Lippard, Acc. Chem. Res., 1978,11, 211-217 (56). 

The antitumour drug temozolomide 24 (R = Me) has been attracting attention and two new routes have been develqjed. One starts from 5-aminoimidazole-4-caiboxamide, whilst the other starts from 5-diazoimidazole-4-carboxamide which reacts with trimethylsilyl isocyanate to give 8-carbamoylimidazo[5,l-[Pg.272]

Sava, G., Bergamo, A. Dyson, P. J. Metal-based antitumour drugs in the post-genomic era what comes next Dalton Trans. 40, 9069-9075 (2011). 

The antitumour drug dacarbazine (DTIC, 214) turns pink in solution unless protected from light, and the coloured preparation causes pain at the site of injection. When the solution is carefully kept dark both during storage and administration, there is no trouble. 

Molecular mechanisms of specificity in DNA-antitumour drug interactions, 18,1... 

There has been intense interest in recent years in selective modification of functionality in baccatin III, 1, the basic diterpenoid core of paclitaxel (Taxol ) which is now established as a clinically active antitumour drug. Given the complexity of 1, rearrangements are common even under mild conditions and attempts to carry out apparently simple transformations are frequently frustrated, as shown by the following example. The 13p-chloro derivative 2 was prepared and fully characterised, then treated with sodium azide in aqueous DMF at 60°C in the expectation that the 13 a azide would be obtained. The product, however, was shown to be the ring cleaved compound 3 (71% yield). 

Analytical characteristics of selected pteridines/antitumoural drugs using a.c. stripping voltammetry on HgCFMEs... 

T. Koudriakova, E. Iatsimirskaia, S. Tulebaev, D. Spetie, I. Utkin, D. Mullet, T. Thompson, P. Vouros, and N. Gerber, In vivo disposition and metabolism by liver and enterocyte microsomes of the antitumour drug rifabutin in rats, J. Pharmacol. Exp. Therap. 279 1300-1309 (1996). 

Unfortunately this approach has not been very successful for producing site specific antitumour drugs. However, site specific prodrugs have been developed to deliver drugs to a number of sites. 

Keywords Antitumour drugs, Bioconfonner, Microtubule stabilizing agents, Paclitaxel... 

The preferential binding of the antitumour drug cisplatin (ds-diamminechloroplatinum-II) to GpG and ApG sequences in DNA has prompted the use of ab initio calculations with relativistic pseudopotentials to evaluate three important parameters for the Pt-adenine model complex [Pt(NH3)3 adenine]. These are the force constant for the Pt—N-7 bond bending out of the adenine... 

Connors TA. 1978. Antitumour drugs with latent activity. Biochimie 60 979-987. 

Oussoren, C., Eling, W. M., Crommelin, D. J., Storm, G., and Zuidema, J. (1998), The influence of the route of administration and liposome composition on the potential of liposomes to protect tissue against local toxicity of two antitumour drugs, Biochim. Biophys. Acta, 1369,159-172. 

The anthracycline antibiotic drugs approved for antitumour drug therapy include doxorubicin (adriamycin), epirubicin, daunorubicin, idarubicin, and aclarubicin. These drug substances are structurally similar and characterized by a tetracyclic aglycone linked to amino sugar moieties. Particularly in solutions, the anthracyclines are photolabile. The formation of inactive aglyconesand polymeric substances as a result of the irradiation of anthracycline solutions has been reported. 

Stevens MFC, Peaty L. Photodegradation of solutions of the antitumour drug DTIC. J Pharm Pharmacol 1978 30 47P. 

Bejnen JH, van Gijn R, Underberg WJM. Chemical stability of the antitumour drug mitomycin C in solutions for intravesical instillation. J Parent Sci Tech 1990 44 332-335. 

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