Total synthesis and biological mode of action of largazole: a potent class I histone deacetylase inhibitor
The efficient total synthesis of the recently described natural substance largazole (1) and its
active metabolite largazole thiol (2) is described. The synthesis required eight linear steps …
active metabolite largazole thiol (2) is described. The synthesis required eight linear steps …
Total synthesis and molecular target of largazole, a histone deacetylase inhibitor
Y Ying, K Taori, H Kim, J Hong… - Journal of the American …, 2008 - ACS Publications
Full details of the concise and convergent synthesis (eight steps, 19% overall yield), its
extension to the preparation of a series of key analogues, and the molecular target and …
extension to the preparation of a series of key analogues, and the molecular target and …
Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7-modified analogues
JA Souto, E Vaz, I Lepore, AC Pöppler… - Journal of medicinal …, 2010 - ACS Publications
Largazole 4a and analogues with modifications at the C7 position, as well as 2, 4′-
bithiazole 5a, have been synthesized using an acyclic cross-metathesis of the …
bithiazole 5a, have been synthesized using an acyclic cross-metathesis of the …
Largazole and analogues with modified metal-binding motifs targeting histone deacetylases: synthesis and biological evaluation
P Bhansali, CL Hanigan, RA Casero Jr… - Journal of medicinal …, 2011 - ACS Publications
The histone deacetylase inhibitor largazole 1 was synthesized by a convergent approach
that involved several efficient and high yielding single pot multistep protocols. Initial attempts …
that involved several efficient and high yielding single pot multistep protocols. Initial attempts …
Total Syntheses of the Histone Deacetylase Inhibitors Largazole and 2-epi-Largazole: Application of N-Heterocyclic Carbene Mediated Acylations in Complex …
B Wang, PH Huang, CS Chen… - The Journal of organic …, 2011 - ACS Publications
Details of the evolution of strategies toward convergent assembly of the histone deacetylase
inhibiting natural product largazole exploiting γ, δ-unsaturated-α, β-epoxy-aldehydes and a …
inhibiting natural product largazole exploiting γ, δ-unsaturated-α, β-epoxy-aldehydes and a …
Synthesis and activity of largazole analogues with linker and macrocycle modification
Y Ying, Y Liu, SR Byeon, H Kim, H Luesch… - Organic letters, 2008 - ACS Publications
To characterize largazole's structural requirements for histone deacetylase (HDAC)
inhibitory and antiproliferative activities, a series of analogues with modifications to the side …
inhibitory and antiproliferative activities, a series of analogues with modifications to the side …
Structural basis of the antiproliferative activity of largazole, a depsipeptide inhibitor of the histone deacetylases
KE Cole, DP Dowling, MA Boone… - Journal of the …, 2011 - ACS Publications
Largazole is a macrocyclic depsipeptide originally isolated from the marine cyanobacterium
Symploca sp., which is indigenous to the warm, blue-green waters of Key Largo, Florida …
Symploca sp., which is indigenous to the warm, blue-green waters of Key Largo, Florida …
Modulation of activity profiles for largazole-based HDAC inhibitors through alteration of prodrug properties
LA Salvador, H Park, FH Al-Awadhi, Y Liu… - ACS Medicinal …, 2014 - ACS Publications
Largazole is a potent and class I-selective histone deacetylase (HDAC) inhibitor purified
from marine cyanobacteria and was demonstrated to possess antitumor activity. Largazole …
from marine cyanobacteria and was demonstrated to possess antitumor activity. Largazole …
Enantioselective total synthesis of (+)-largazole, a potent inhibitor of histone deacetylase
AK Ghosh, S Kulkarni - Organic letters, 2008 - ACS Publications
An enantioselective total synthesis of the cytotoxic natural product (+)-largazole (1) is
described. It is a potent histone deacetylase inhibitor. Our synthesis is convergent and …
described. It is a potent histone deacetylase inhibitor. Our synthesis is convergent and …
Anticolon cancer activity of largazole, a marine-derived tunable histone deacetylase inhibitor
Y Liu, LA Salvador, S Byeon, Y Ying, JC Kwan… - Journal of pharmacology …, 2010 - ASPET
Histone deacetylases (HDACs) are validated targets for anticancer therapy as attested by
the approval of suberoylanilide hydroxamic acid (SAHA) and romidepsin (FK228) for treating …
the approval of suberoylanilide hydroxamic acid (SAHA) and romidepsin (FK228) for treating …
相关搜索
- deacetylase inhibitor potent class
- total synthesis potent class
- deacetylase inhibitor total synthesis
- mode of action potent class
- deacetylase inhibitor mode of action
- depsipeptide inhibitor histone deacetylases
- largazole analogues synthesis and activity
- antiproliferative activity histone deacetylases
- biological evaluation histone deacetylases
- process development potent class
- deacetylase inhibitor process development
- structural basis histone deacetylases
- process development total synthesis
- potent inhibitor histone deacetylase
- total syntheses molecule synthesis