Synthesis and biological evaluation of methoxylated analogs of the newer generation taxoids IDN5109 and IDN5390.
Starting from 10-deacetylbaccatin III (7), the 2-debenzoyl-2-m-methoxybenzoyl analogs of the newer generation taxoids IDN5109 (3) and IDN5390 (4) were synthesized. The biological evaluation of these compounds (5 and 6, respectively) showed a general increase of cytotoxicity, as observed in first-generation anticancer taxanes.
Barboni
Luciano
L
Dipartimento di Scienze Chimiche, Università di Camerino, Via S. Agostino 1, 62032 Camerino (MC), Italy. luciano.barboni@unicam.it
Ballini
Roberto
R
Giarlo
Guido
G
Appendino
Giovanni
G
Fontana
Gabriele
G
Bombardelli
Ezio
E
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001952:Bridged-Ring Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D006801:Humans; D043823:Taxoids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D000970:Antineoplastic Agents; D001952:Bridged-Ring Compounds; C459840:IDN 5390; D043823:Taxoids; C404743:IDN 5109