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Exploring a cascade Heck-Suzuki reaction based route to kinase inhibitors using design of experiments

Andreas Ekebergh (Institutionen för kemi och kemiteknik, Organisk kemi) ; Christine Lingblom ; Peter Sandin (Institutionen för kemi och kemiteknik, Fysikalisk kemi) ; Christine Wennerås ; Jerker Mårtensson (Institutionen för kemi och kemiteknik, Organisk kemi)
Organic and biomolecular chemistry (1477-0520). Vol. 13 (2015), 11, p. 3382-3392.
[Artikel, refereegranskad vetenskaplig]

Design of Experiments (DoE) has been used to optimize a diversity oriented palladium catalyzed cascade Heck-Suzuki reaction for the construction of 3-alkenyl substituted cyclopenta[b]indole compounds. The obtained DoE model revealed a reaction highly dependent on the ligand. Guided by the model, an optimal ligand was chosen that selectively delivered the desired products in high yields. The conditions were applicable with a variety of boronic acids and were used to synthesize a library of 3-alkenyl derivatized compounds. Focusing on inhibition of kinases relevant for combating melanoma, the library was used in an initial structure-activity survey. In line with the observed kinase inhibition, cellular studies revealed one of the more promising derivatives to inhibit cell proliferation via an apoptotic mechanism.

Denna post skapades 2015-05-07. Senast ändrad 2017-10-03.
CPL Pubid: 216755


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Institutioner (Chalmers)

Institutionen för kemi och kemiteknik, Organisk kemi
Institutionen för biomedicin, avdelningen för infektionssjukdomar (GU)
Institutionen för kemi och kemiteknik, Fysikalisk kemi



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