A spirolactone with anti-tumor activity is formed during the reaction of paraformaldehyde with 17-deacetylvinblastine. The compound was identified by NMR techniques. The chemotherapeutic activity was assessed.
the 0th: esters of valine ( 2 1 , leucine (31, isoleucine (41, tryptophane ( 5 ) and valine-tryptophane (6).We describe the synthesis of amides between 17-deacetylvlnblastine (1) and
Considerable attention has bean given to the alkaloids of the Uadagascar periwinkle (Catharanthus roseus G. Don) because of their antitumor activity'.It seenu that this activity can be augmented or oriented by the introduction of certain amino acids or peptide chains2-'. This could be achievad by replacing the methylester on C-16 in vinblastine by the amide formed with the chosen amino acids (2)-(6). In the present paper we describe the results of this approach with 17-deacetyl vinblastine5. the caapounds synthesized in the present study the ' H NUR spectrum of vinblas-tine6-8 was chosen as reference. the study of the changes occurring on derivatizing vinblastine.
For confirmation of tho structures of ' H NnR is a sufficiently sensitive tool for
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