25983-52-2Relevant articles and documents
Synthesis and protein kinase inhibitory activity of balanol analogues with modified benzophenone subunits
Lampe, John W.,Jagdmann Jr., G. Erik,Johnson, Mary George,Lai, Yen-Shi,Lowden, Christopher T.,Lynch, Michael P.,Mendoza, José S.,Murphy, Marcia M.,Wilson, Joseph W.,Ballas, Lawrence M.,Carter, Kiyomi,Biggers, Christopher K.,Darges, James W.,Davis, Jefferson E.,Hubbard, Frederick R.,Stamper, Mark L.,Defauw, Jean M.,Foglesong, Robert J.,Hall, Steven E.,Heerding, Julia M.,Hollinshead, Sean P.,Hu, Hong,Hughes, Philip F.
, p. 2624 - 2643 (2007/10/03)
A series of analogues of the protein kinase C (PKC) inhibitory natural product balanol which bear modified benzophenone subunits are described. The analogues were designed with the goal of uncovering structure -activity features that could be used in the development of PKC inhibitors with a reduced polar character compared to balanol itself. The results of these studies suggest that most of the benzophenone features found in the natural product are important for obtaining potent PKC inhibitory compounds. However, several modifications were found to lead to selective inhibitors of the related enzyme protein kinase A (PKA), and several specific modifications to the polar structural elements of the benzophenone were found to provide potent PKC inhibitors. In particular, it was found that replacement of the benzophenone carboxylate with bioisosteric equivalents could lead to potent analogues. Further, a tolerance for lipophilic substituents on the terminal benzophenone ring was uncovered. These results are discussed in light of recently available structural information for PKA.
Chiral dendrimers with backfolding wedges
Peerlings,Trimbach,Meijer
, p. 497 - 498 (2007/10/03)
Dendritic wedges with a substitution pattern that forces the growth inwards are introduced and the use of this new building strategy is exemplified in the synthesis and chiroptical properties of a chiral dendrimer.
Synthesis and Fluorescence Properties of Selectively Metallated Diporphyrins with Electron-Accepting Moieties
Nagata, Toshi
, p. 3005 - 3016 (2007/10/02)
Synthesis of selectively metallated diporphyrins with electron-accepting moieties is described.Steady-state fluorescence spectra of these compounds showed substantial quenching of the fluorescence of the free-base porphyrin.A possible "superexchange" mechanism of long-range electron transfer is discussed.