Synthesis and biology of 3'-N-acyl-N-debenzoylpaclitaxel analogues.
The, 3'-N-acyl-N-debenzoylpaclitaxel analogues 1a-d were synthesized and evaluated on biological systems. Some of the analogues 1a-d exhibited higher cytotoxicities (up to 20-fold) and stronger abilities to induce apoptosis than paclitaxel. In an in vivo experiment against i.p. implanted B16 melanoma, the most cytotoxic compound 1b in vitro caused tumor growth inhibition more than paclitaxel.
Roh
E J
EJ
Life Sciences Division, Korea Institute of Science and Technology, Seoul, South Korea.
Song
C E
CE
Kim
D
D
Pae
H O
HO
Chung
H T
HT
Lee
K S
KS
Chai
K B
KB
Lee
C O
CO
Choi
S U
SU
D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002455:Cell Division / Q000187:drug effects; D018922:HL-60 Cells; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008546:Melanoma, Experimental / Q000473:pathology; D017239:Paclitaxel / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D016339:Spectrometry, Mass, Fast Atom Bombardment
D000972:Antineoplastic Agents, Phytogenic; D017239:Paclitaxel