Anti-tumor agent

The protein Ras, an important intracellular signal transducer, is crucially involved in the development of tumor growth. The farnesylation of Ras, catalyzed by the enzyme Ras-farnesyl-transferase, is essential to its proper functioning in the normal and in the transformed state. Therefore, the inhibition of Ras lipidation has become a promising target for the development of new classes of anti-tumor agents. This review focuses on the different classes of Ras-farnesyl-transferase inhibitors and compares their biological properties and modes of action in vitro as well as in vivo. 

C-H activation remains an important topic for catalysis even after thirty years of intensive research. The potential shortcuts it offers for many present routes to a wide variety of chemicals that are produced will continue to inspire industrial and academic research [32], An interesting example involves the enantiospecific, coordination-directed C-H bond functionalisation in the synthesis of a natural product, rhazinilam, an anti-tumor agent. The resulting vinyl moiety obtained in the dehydrogenation was subsequently carbonylated to form a cyclic amide [33],... 

Additional anti-tumor agents exhibiting antibacterial activity are the iminophosphorane derivatives of mitomycin (41), with phenyl-, alkyl-, or... 

Enantiomerically pure trifluoromethyl- and trifluoroethylcyclopropylcarbi-nols 132 and derivatives (R=Ci 2 fluoroalkyl, alkyl, aryl) appeared useful as intermediates for enzyme inhibitors, physiological active substances and anti-tumoral agents, Eq. (53), [183]. 

Phase 1 Tolerability Safety Pharmacokinetics Pharmacodynamics Usually male healthy volunteers For inherently toxic compounds patients (e.g. anti-tumor agents)... 

There are suggestions that for the prevention of HF some agents should be better avoided, although the logic for these believes has not been proven. Many HF programs, for example, limit alcohol consumption to some extent. Smoking, the use of cocaine or amphetamines are also believed to be toxic. However it is well known that certain anti-tumor agents such as anthracyclines and also irradiation of the mediastinum may cause cardiac dysfunction. There is no clear evidence for the benefit of early treatment of these subjects, but close attention is certainly advisable. 

Kiimmeier K., T. Steger-Hartmann, and M. Meyer (1997b). Biodegradability of the anti-tumor agent ifosfomide and its occurrence in hospital effluents and sewage. Water Research 31 2705-2710. 

Hemscheidt s determination of the absolute stereochemistry of the anti-tumor agent (+)-falcarindiol highlights the utility of natural product degradation via ethenolysis (Scheme 23). Previous work had demonstrated that the stereochemistry at C8 was (3 ) however, the relative stereochemistry of the two stereocenters remained unclear. 

Arison BH, Beck JL (1973) The Structure of Compound 593A. A New Anti-tumor Agent. Tetrahedron 29 2743... 

R.F. Rekker, in Structure-Activity Relationships of Anti-tumor Agents, eds. D.N. Reinhoudt, T.A. Connors, H.M. Pinedo and K.W. van de Poll (Martinus Nijhoff Publishers, The Hague, 1983), p. 23. 

Jansen PJ, Akers MJ, Amos RM, Baertschi SW, Cooke GG, Dorman DE, Kemp CAJ, Maple SR, McCune KA. The degradation of the anti-tumor agent gemcitabine hydrochloride in an acidic aqueous solution at pH 3.2 and identification of degradation products. J Pharm Sci 2000 89(7) 885-891. 

The acridone alkaloids constitute a small group of natural products found exclusively in the Rutaceae family of higher plants. A sustained interest in this field has been due to the reported activity of acronycine a constituent of Acronnychia baueri and Vepris amphody as an anti-tumor agent. 

Radical cyclization with iodine atom transfer of a highly functionalized propiolic ester 103 using dibenzoyl peroxide as an initiator gave the a-methylene-y-butyrolactone 104 in good yield [95T11257]. The relative stereochemistry at carbon atoms 4 and 5 are established during the reaction. The intermediate 104 has been converted to the anti-tumor agent (-)-methylenolactocin 105. 

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