The titanium-mediated cyclopropanation reaction using Ti((OPr)-Pr-i)(3)Me/EtMgBr/BF3 center dot OEt2 has been applied to various 2-cyanopyrrolidines for the synthesis of functionalized 2-(1-aminocyclopropyl)pyrrolidine-3,4-diol derivatives (dideoxyiminoald ...
New derivatives of 1,4-dideoxy-1,4-imino-D-ribitol have been prepared and evaluated for their cytotoxicity on solid and haematological malignancies. 1,4-Dideoxy-5-O-[(9Z)-octadec-9-en-1-yl]-1,4-imino-Dribitol (13, IC50 similar to 2 mu M) and its C-18-analo ...
We report the total synthesis of a series of pyrrolizidine analogues of casuarine (1) and their 6-O-alpha-glucoside derivatives. The synthetic strategy is based on a totally regio- and stereoselective 1,3-dipolar cycloaddition of suitably substituted alken ...
Novel alpha-mannosidase inhibitors of the type (2R,3R,4S)-2-({[(1R)-2- hydroxy-1-arylethyl]amine}methyl) pyrrolidine-3,4-diol have been prepared and assayed for their anticancer activities. Compound 30 with the aryl group = 4-trifluoromethylbiphenyl inhibi ...
The present invention provides new dihydroxypyrrolidine derivatives for use as medicaments. The compounds are useful in the treatment in cancer, in particular non-solid neoplasms. ...
An approach to the synthesis of polyhydroxyazepane derivatives from sugar-based epoxyamides or epoxyalcohols, in which the total regioselective epoxide opening by nitrogen nucleophiles is the key step, is described. Thus, novel polyhydroxyazepane carboxami ...
3,6-Anhydro-1-(aryl or alkylamino)-1-deoxy-D-sorbitol derivatives have been prepared in four steps from isosorbide, a by-product from the starch industry. The inhibitory activities of these new compounds have been evaluated towards 13 glycosidases. A first ...
New oxathiazinane dioxides have been derived from D- and L-serine and tested for their in vitro cell growth inhibitory activity toward SKBR3 breast cancer cells. (5R)-5-(4-(4'-Bromomethyl)phenyl)benzyloxymethyl-[1,3,4]-oxathiazinane- 3,3-dioxide showed a c ...
Tumors consist of cells whose growth and morphological characteristics are markedly different from those of normal cells. Observation of human and animal models argue that tumor development proceeds via a process formally analogous to Darwinian evolution, ...
