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.
Battaglia
Arturo
A
Istituto CNR per La Sintesi Organica e Fotoreattività "I.S.O.F.", via Gobetti 101, 40129 Bologna, Italy. battaglia@area.bo.cnr.it
Bernacki
Ralph J
RJ
Bertucci
Carlo
C
Bombardelli
Ezio
E
Cimitan
Samanta
S
Ferlini
Cristiano
C
Fontana
Gabriele
G
Guerrini
Andrea
A
Riva
Antonella
A
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