Antitumour agents selectivity

H. Ouadid-Ahidouch, and J. M. Garcia Fernandez, Synthesis of N-, S-, and C-glycoside castanosper-mine analogues with selective neutral a-glucosidase inhibitory activity as antitumour agents, Chem. Commun., 46 (2010) 5328-5330. 

During a synthesis of the marine antitumour agent Sarcodictyin A, selective removal of a secondary and a tertiary TES ether in the presence of a primary TIPS ether was effected by treatment with 5 equivalents of triethylamine trihy-drofluoride (Et3N 3HF)26 in THF at room temperature [Scheme 4,21 ].6... 

It should be noted that when the reaction is conducted with a chiral aldehyde and a chiral y-substituted allyltins, a matching effect when both partners impose a convergent selectivity, or a mismatching effect when the facial selectivity is divergent, may happen . Such a stereoconvergent effect was used in the synthesis of the antitumour agent azinomycin (equation 4). 

Antitumour Agents. 213. Modeling of Epipodophyllotoxin Derivatives Using Variable Selection k Nearest Neighbor QSAR Method. 

A series of avermectin analogues have been prepared with spacer arms between the disaccharide and the aglycone. Some of the products showed considerable bioactivity. This disaccharide (107) and epimers at C-4 and C-3 were made for use in the synthesis of mithramycin and related antitumour agents, and the AB disaccharide of olivomycin A, 2,6-dideoxy-3-0-(2,6-dideo qr-tf-D-fyxo-hexosyl)-Z)-it)ao-hexose was produced using the highly selective synthesis of 2-deoxyhexoses from 4-deoxy-2,3-0-isopropylidene-D-threose (Chapter 12). ... 

This class of substances inhibiting nucleic acid synthesis is often found in tissue culture cells to cause chromosome breakage and oflier alterations in the nucleus and nucleolus. They have been selected and studied because they ate powerful antibacterial or antitumour agents. Except for local applications, they are not of great therapeutic use, since they are very toxic. It is difficult to conceive a substance of this type, which would have a selective action because the most regular and vital feature of any type of cell is the presence of a double-stranded DNA, functioning normally. 

As regards hexopyranosyl systems, 5-substituted-6-azauracil nucleosides of N acetylglucosamine have been prepared, and acetobromoglucose was used as starting material to make the bis(nitroimidazole) 71, in a search for hypoxia-selective antitumour agents with two bioreductively-activated units. ... 

Bemers-Price SJ, Bowen RJ, Galettis P et al (1999) Stmctural and solution chemistry of gold(l) and silver(l) complexes of bidentate pyridyl phosphines selective antitumour agents. Coord Chem Rev 185-186 823-836... 

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