1556858-75-3Relevant academic research and scientific papers
Rational hopping of a peptidic scaffold into non-peptidic scaffolds: Structurally novel potent proteasome inhibitors derived from a natural product, belactosin A
Kawamura, Shuhei,Unno, Yuka,Hirokawa, Takatsugu,Asai, Akira,Arisawa, Mitsuhiro,Shuto, Satoshi
supporting information, p. 2445 - 2447 (2014/03/21)
Rational scaffold hopping of a natural product belactosin A derivative was successfully achieved based on the pharmacophore model constructed. The peptidic scaffold was replaced by significantly simplified non-peptidic scaffolds, by which weak belactosin A (IC50 = 1440 nM) was converted into highly potent non-peptidic inhibitors (IC50 = 26-393 nM).
