852990-46-6Relevant academic research and scientific papers
Synthesis and antitumor activity of benzils related to combretastatin A-4
Mousset, Celine,Giraud, Anne,Provot, Olivier,Hamze, Abdallah,Bignon, Jerome,Liu, Jian-Miao,Thoret, Sylviane,Dubois, Joelle,Brion, Jean-Daniel,Alami, Mouad
scheme or table, p. 3266 - 3271 (2009/04/05)
A series of benzil derivatives related to combretastatin A-4 (CA-4) have been synthesized by oxidation of diarylalkynes promoted by PdI2 in DMSO. Using this new protocol, 14 benzils were prepared in good to excellent yields and their biological
DMSO-PdI2 as a powerful oxidizing couple of alkynes into benzils: one-pot synthesis of nitrogen-containing five- or six-membered heterocycles
Mousset, Céline,Provot, Olivier,Hamze, Abdallah,Bignon, Jér?me,Brion, Jean-Daniel,Alami, Mouad
, p. 4287 - 4294 (2008/09/19)
PdI2 in DMSO promoted the oxidation of functionalized diarylalkynes into benzil derivatives in excellent yields. This new oxidation reaction was achieved with short reaction times and low loading of palladium catalyst. This efficient catalytic
Synthesis and cytotoxic evaluation of combretafurazans
Tron, Gian Cesare,Pagliai, Francesca,Del Grosso, Erika,Genazzani, Armando A.,Sorba, Giovanni
, p. 3260 - 3268 (2007/10/03)
Combretastatin A-4 is an antitumoral and antitubulin agent that is active only in its cis configuration. In the present manuscript, we have synthesized cis-locked combretastatins embodying a furazan ring (combretafurazans). To achieve this, we have developed a new strategy that exploits the dehydration of vicinal dioximes using the Mitsunobu reaction. Among the advantages of following such a strategy are the mild conditions used for the construction of the diarylfurazan derivatives, allowing for the presence of highly functionalized substrates and deactivated aromatic rings. Combretafurazans are more potent in vitro cytotoxic compounds compared to combretastatins in neuroblastoma cells, yet maintaining similar structure-activity relationship and pharmacodynamic profiles.
