Design, Synthesis and Conformational Studies of Cyclic Tetrapeptides having βγ Fused Turns as HDAC Inhibitors

2021 ◽  
Vol 6 (31) ◽  
pp. 7887-7893
Author(s):  
Uttam Ghosh ◽  
Moumita Basu ◽  
Sudip Pal ◽  
Sanjeev Meena ◽  
Dipak Datta ◽  
...  
Keyword(s):  
Hdac Inhibitors ◽  
Design Synthesis ◽  
Conformational Studies ◽  
Cyclic Tetrapeptides

The Construction of New Proteins. II. Design, Synthesis and Conformational Studies of Folding Units with βαβ-Topology

1986 ◽  
Vol 41 (10) ◽  
pp. 1315-1322 ◽  
Author(s):  
Manfred Mutter ◽  
Karl-Heinz Altmann ◽  
Thomas Vorherr
Keyword(s):  
Solid Phase ◽  
Three Dimensional ◽  
Chemical Properties ◽  
Spectroscopic Studies ◽  
General Concept ◽  
Dimensional Structure ◽  
Design Synthesis ◽  
Phase Synthesis ◽  
Conformational Studies ◽  
Conformational Effects

The design, synthesis and preliminary conformational studies of two polypeptides exhibiting βαβ-type folding topologies are presented. In the design of the model peptides the general concept for the construction of new proteins developed in the preceeding paper was applied. According to this strategy, amphiphilic helices and β-sheets are linked together via hydrophilic loops to attain three-dimensional structures of higher order (‘supersecondary structures’). Com­puter-assisted molecular modelling served as a valuable tool for minimizing conformational con­straints within the molecules. The 38-residue peptide MI was synthesized using polyethylene glycol (PEG) as solubilizing polymeric support (‘Liquid-Phase synthesis'). Conformationally in­duced changes in the physico-chemical properties of the growing peptide chain stressed the significance of conformational effects in peptide synthesis reported earlier. Similar observations were made during the solid-phase synthesis of the 35-peptide MII. CD and IR spectroscopic studies revealed a high degree of secondary structure for both folding units. The present data strongly support the adoption of a three-dimensional structure for both models.

Design, synthesis and antitumor activity evaluation of novel HDAC inhibitors with tetrahydrobenzothiazole as the skeleton

2021 ◽  
Vol 108 ◽  
pp. 104652
Author(s):  
Simin Sun ◽  
Wenwen Zhao ◽  
Yongliang Li ◽  
Ziwei Chi ◽  
Xixi Fang ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Hdac Inhibitors ◽  
Design Synthesis ◽  
Activity Evaluation

Design, synthesis and bioevalution of novel benzamides derivatives as HDAC inhibitors

2013 ◽  
Vol 23 (1) ◽  
pp. 179-182 ◽  
Author(s):  
Yanyang Li ◽  
Yan Zhou ◽  
Pengyu Qian ◽  
Yongzhen Wang ◽  
Falong Jiang ◽  
...  
Keyword(s):  
Hdac Inhibitors ◽  
Design Synthesis

scholarly journals Design, synthesis and evaluation of belinostat analogs as histone deacetylase inhibitors

2019 ◽  
Vol 11 (21) ◽  
pp. 2765-2778
Author(s):  
Jie-Huan Zhang ◽  
Madhusoodanan Mottamal ◽  
Hai-Shan Jin ◽  
Shanchun Guo ◽  
Yan Gu ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Active Compound ◽  
Histone Deacetylase Inhibitors ◽  
Hdac Inhibitors ◽  
Antitumor Therapy ◽  
Design Synthesis ◽  
Inhibitory Activities ◽  
Antiproliferative Activities

Aim: Histone deacetylase (HDAC) is an attractive target for antitumor therapy. Therefore, the development of novel HDAC inhibitors is warranted. Materials & methods: A series of HDAC inhibitors based on N-hydroxycinnamamide fragment was designed as the clinically used belinostat analog using amide as the connecting unit. All target compounds were evaluated for their in vitro HDAC inhibitory activities and some selected compounds were tested for their antiproliferative activities. Conclusion: Among them, compound 7e showed an IC50 value of 11.5 nM in inhibiting the HDAC in a pan-HDAC assay, being the most active compound of the series.

Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors

2017 ◽  
Vol 27 (17) ◽  
pp. 4051-4055 ◽  
Author(s):  
Mingfeng Shao ◽  
Linhong He ◽  
Li Zheng ◽  
Lingxiao Huang ◽  
Yuanyuan Zhou ◽  
...  
Keyword(s):  
Hdac Inhibitors ◽  
Design Synthesis ◽  
Antiproliferative Effects
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