The chem. resoln., using N-tosyl-L-proline as a chiral auxiliary, of a racemate of the pyrazole analog (±)-N-Boc-CPzI (I) of the left hand segment (CPI) of the antitumor agent CC-1065, and the cytotoxic evaluation of both enantiomers are described. The reported results further validate the direct relationship between chem. solvolytic stability of the cyclopropane ring and cytotoxicity proposed by Boger and coworkers.
Resolution of a CPzI precursor, synthesis and biological evaluation of (+) and (-)-N-Boc-CPzI: A further validation of the relationship between chemical solvolytic stability and cytotoxicity
BARALDI, Pier Giovanni;CACCIARI, Barbara;ROMAGNOLI, Romeo;SPALLUTO, Giampiero;
1999
Abstract
The chem. resoln., using N-tosyl-L-proline as a chiral auxiliary, of a racemate of the pyrazole analog (±)-N-Boc-CPzI (I) of the left hand segment (CPI) of the antitumor agent CC-1065, and the cytotoxic evaluation of both enantiomers are described. The reported results further validate the direct relationship between chem. solvolytic stability of the cyclopropane ring and cytotoxicity proposed by Boger and coworkers.File in questo prodotto:
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