- as a
selective proteasome inhibitor. Chemically, it is a
tetrapeptide epoxyketone and an
analog of epoxomicin. It was
developed by Onyx Pharmaceuticals...
- fragmentation,
first published in 1967, is the
chemical reaction of α,β-
epoxyketones (1) with aryl
sulfonylhydrazines (2) to give
alkynes (3) and carbonyl...
- myeloma, with
Phase 1b
studies ongoing (as of
February 16, 2016).
Being an
epoxyketone derivative,
oprozomib is
structurally related to
carfilzomib and has...
-
provides a
practical application of the
Wharton olefin synthesis. An α,β-
epoxyketone reacts with
hydrazine hydrate to
yield an
allylic alcohol. In the synthesis...
- Its lead
product candidate,
carfilzomib (PR-171), is a
tetrapeptide epoxyketone for
treating multiple myeloma, a
blood cancer. The drug
carfilzomib works...
-
proteasome inhibitor via its
epoxyketone pharmacop****.
Subsequent medicinal chemistry efforts by
Crews produced the
epoxyketone-containing
proteasome inhibitor...
- doi:10.1021/ed082p1780.3 Cormier, R. A.; Francis, M. D. (1981), "The
Epoxyketone-Furan Rearrangement",
Synthetic Communications, 11 (5): 365, doi:10...
-
David F.; Dehn,
Robert L. (1967). "A
novel fragmentation reaction of α,β-
epoxyketones the
synthesis of
acetylenic ketones".
Tetrahedron Lett. 8 (40): 3943–3946...
- mitochondria.
Cyclic tetrapeptides are a
class of
drugs that
contain an α-
epoxyketone group that has the
potential to
alkylate the HDAC
active site. The HDAC...
- phenols,
photochemical electrocyclic processes, the
rearrangement of
epoxyketones to beta-****tones, ring
opening of
cyclopropyl ketones,
heterolysis of...
