Synthesis and antitumor activity of mechercharmycin A analogues.
Several analogues of the cytotoxic thiopeptide IB-01211 or mechercharmycin A (1) have been synthesized. The cytotoxicity of 1 and the synthesized analogues were evaluated against a panel of three human tumor cell lines. Thiopeptide 1 and the most active derivatives 2 and 3c were chosen for further studies on effects on cell cycle progression and induction of apoptosis. Interestingly, the inhibition of cell division and activation of a programmed cell death by apoptosis were detected.
Hernández
Delia
D
Institute for Research in Biomedicine, Barcelona Science Park-University of Barcelona, Baldiri Reixac 10, E-08028 Barcelona, Spain.
Altuna
Marta
M
Cuevas
Carmen
C
Aligué
Rosa
R
Albericio
Fernando
F
Alvarez
Mercedes
M