Synthesis and biological evaluation of 2'-methyl taxoids derived from baccatin III and 14beta-OH-baccatin III 1,14-carbonate.
A series of 2'-methyl taxoids were synthesized and essayed for growth inhibition experiments conducted in human ovarian cancer cell line A2780wt and its counterparts A2780cis, A2780tax, and A2780adr, resistant to cisplatin, paclitaxel, and doxorubicin, respectively, to test the effect of this substituent on the antitumor activity. Additional experiments were performed on MCF-7 human breast cancer cell line and MCF7-R resistant to doxorubicin. In several cases these taxoids were more active than paclitaxel showing subnanomolar IC(50) values.
Istituto CNR per La Sintesi Organica e Fotoreattività "I.S.O.F.", via Gobetti 101, 40129 Bologna, Italy. battaglia@area.bo.cnr.it
Arturo
A
Battaglia
Ralph J
RJ
Bernacki
Carlo
C
Bertucci
Ezio
E
Bombardelli
Samanta
S
Cimitan
Cristiano
C
Ferlini
Gabriele
G
Fontana
Andrea
A
Guerrini
Antonella
A
Riva
D000470:Alkaloids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D019008:Drug Resistance, Neoplasm; D006801:Humans; D013329:Structure-Activity Relationship; D043823:Taxoids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000470:Alkaloids; D000970:Antineoplastic Agents; D043823:Taxoids; C073950:baccatin III