Analogue synthesis

Toxicity Amelioration. Cancer researchers traditionally have not focused their attention on the question of toxicity amehoration. This is partiy attributed to the lack of predictive animal models for human toxicities. For example, the preclinical rat model, used as a predictor of myelosuppression, has failed to predict myelosuppression in humans in clinical trials. In addition, reduction of one toxicity may result in the emergence of another, more serious problem. Research efforts to address the problem of toxicity amelioration has progressed in several directions. The three most prominent areas are analogue synthesis, chemoprotection, and dmg targeting. 

Cephalosporanic acid, 3 -deacetoxy-, 7, 289 Cephalosporin, 3 -deacetoxy-absorption, 7, 293 synthesis, 7, 293 Cephalosporin, 3,4-dihydro-synthesis, 7, 292 Cephalosporin, 7a-hydroxy-synthesis, 7, 290 Cephalosporin C, 7, 288 as pharmaceutical, 1, 152 total synthesis, 7, 294 Woodward s total synthesis, 7, 294 Cephalosporin C, deacetoxy-synthesis, 7, 292 Cephalosporins, 7, 267, 285-298 7-acylamino substituent configuration, 7, 290 analogues synthesis, 7, 288 as antibiotics, 2, 519 3, 1038 application, 7, 296... 

Ren RXF, Chaudhuri NC, Paris PL, Rumney S IV, Kool ET (1996) Naphthalene, phenan-threne, and pyrene as DNA base analogues synthesis, structure, and fluorescence in DNA. J Am Chem Soc 118 7671-7678... 

N Sin, L Meng, H Auth, CM Crews. Eponemycin analogues synthesis and use as probes for angiogenesis. (RC02H + TBTU + H-Ser-OR) Bioorg Med Chem 6, 1209, 1998. 

P. Nielsen, H. M. Pfundheller, and J. Wengel, A novel class of conformationally restricted oligonucleotide analogues Synthesis of 2, 3 -bridged monomers and RNA-selective hybridisation, Chem. Commun. (1997) 825-826. 

J. J. Gaudino and C. S. Wilcox, A concise approach to enantiomerically pure carbocyclic robose analogues. Synthesis of (4S, 5R, 6R, 7R)-7-(hydroxymethyl)spiro[2.4Jheptane-4,5,6-triol-... 

Research efforts to address the problem of toxicity amelioration has progressed in several directions. The three most prominent areas are analogue synthesis, chemoprotection, and drug targeting. 

S. Jarosz and A. Listkowski, Sugar derived crown ethers and their analogues Synthesis and properties, Curr. Org. Chem., 10 (2006) 643-662. 

Of course, the activities described in these paradigms are not new to the pharmaceutical and agrochemical industries. However, in the past the distinction between the three has often been less clear owing to the stepwise nature of medicinal chemistry, where new leads either came from unrelated analogue synthesis pro-... 

Csuk R, Scholz Yv (1996) Enantiomerically pure cyclopropanoid nucleoside analogues synthesis and analysis. Tetrahedron 52 6383-6396... 

Delorme and coworkers have published a stereoselective route that is effective with a wide range of amines, including those without a stereocenter on the amine (Scheme 8) [43]. Chiral reduction of the appropriate benzophe-none (as a chromium tricarbonyl complex) using Corey s oxazaborolidine approach afforded the benzhydrol with 91% ee. Treatment with tetrafluo-roboric acid followed by the piperazine gave the desired benzhydryl piperazine without any erosion of stereochemical purity after decomplexation. In addition to simplifying analogue synthesis, these two complementary routes provide a useful base for the future development of stereoselective manufacturing routes. 

Collins I, Rapid analogue synthesis of heteroaromatic compounds, J. Chem. Soc., Perkin Trans., 1 2845-2861, 2000. 

New Protecting Groups in Nucleoside and Nucleotide Chemistry. Pfleide-rer, W. Schirmeister, H. Reiner, T. Pfister, M. Charubala, R. In Biophosphates and their Analogues—Synthesis, Structure, Metabolism and Activity Bruzik, K. S Stec, W. J., Eds. Elsevier Amsterdam, 1987, pp 133-142. 

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