scholarly journals Front Cover: Structure–Activity and Structure–Toxicity Relationships of Peptoid‐Based Histone Deacetylase Inhibitors with Dual‐Stage Antiplasmodial Activity (ChemMedChem 9/2019)

ChemMedChem ◽  
2019 ◽  
Vol 14 (9) ◽  
pp. 887-887
Author(s):  
Marcel K. W. Mackwitz ◽  
Eva Hesping ◽  
Yevgeniya Antonova‐Koch ◽  
Daniela Diedrich ◽  
Tamirat Gebru Woldearegai ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitors ◽  
Antiplasmodial Activity ◽  
Front Cover ◽  
Structure Activity ◽  
Dual Stage

scholarly journals Structure–Activity and Structure–Toxicity Relationships of Peptoid‐Based Histone Deacetylase Inhibitors with Dual‐Stage Antiplasmodial Activity

ChemMedChem ◽  
2019 ◽  
Vol 14 (9) ◽  
pp. 912-926 ◽  
Author(s):  
Marcel K. W. Mackwitz ◽  
Eva Hesping ◽  
Yevgeniya Antonova‐Koch ◽  
Daniela Diedrich ◽  
Tamirat Gebru Woldearegai ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitors ◽  
Antiplasmodial Activity ◽  
Structure Activity ◽  
Dual Stage

scholarly journals Design and Synthesis of Terephthalic Acid-Based Histone Deacetylase Inhibitors with Dual-Stage Anti-PlasmodiumActivity

ChemMedChem ◽  
2017 ◽  
Vol 12 (19) ◽  
pp. 1627-1636 ◽  
Author(s):  
Katharina Stenzel ◽  
Ming Jang Chua ◽  
Sandra Duffy ◽  
Yevgeniya Antonova-Koch ◽  
Stephan Meister ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Terephthalic Acid ◽  
Histone Deacetylase Inhibitors ◽  
Design And Synthesis ◽  
Dual Stage

Design, Synthesis and Structure-Activity Relationship Study of Pyrilamine Derivatives as Histone Deacetylase Inhibitors

Heterocycles ◽  
2020 ◽  
Vol 101 (2) ◽  
pp. 726
Author(s):  
Takaaki Sumiyoshi ◽  
Seiya Hiranaka ◽  
Mayumi Arata ◽  
Akiko Nakata ◽  
Akiko Tanaka ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitors ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Design Synthesis ◽  
Structure Activity ◽  
Relationship Study

Largazole Analogues as Histone Deacetylase Inhibitors and Anticancer Agents: An Overview of Structure-Activity Relationships

ChemMedChem ◽  
2017 ◽  
Vol 12 (23) ◽  
pp. 1917-1926 ◽  
Author(s):  
Giulio Poli ◽  
Romano Di Fabio ◽  
Luca Ferrante ◽  
Vincenzo Summa ◽  
Maurizio Botta
Keyword(s):  
Histone Deacetylase ◽  
Anticancer Agents ◽  
Histone Deacetylase Inhibitors ◽  
Structure Activity Relationships ◽  
Structure Activity

Recent advances in nanomedicine-based delivery of histone deacetylase inhibitors for cancer therapy

Nanomedicine ◽  
2021 ◽  
Author(s):  
Dina A Hafez ◽  
Islam A Hassanin ◽  
Mohamed Teleb ◽  
Sherine N Khattab ◽  
Kadria A Elkhodairy ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitors ◽  
Drug Loading ◽  
Cancer Therapeutics ◽  
Pharmacokinetic Profile ◽  
Physicochemical Characteristics ◽  
Special Focus ◽  
Stimuli Responsive ◽  
Structure Activity ◽  
Reduced Toxicity

Histone deacetylase inhibitors (HDACi) are cancer therapeutics that operate at the epigenetic level and which have recently gained wide attention. However, the applications of HDACi are generally hindered by their poor physicochemical characteristics and unfavorable pharmacokinetic profile. Inspired by the approved nanomedicine-based drugs in the market, nanocarriers could provide a resort to circumvent the limitations imposed by HDACi. Enhanced tumor targeting, improved cellular uptake and reduced toxicity are major advantages offered by HDACi-loaded nanoparticles. More importantly, site-specific drug delivery can be achieved via engineered stimuli-responsive nanosystems. In this review we elucidate the anticancer mechanisms of HDACi and their structure–activity relationships, with a special focus on their nanomedicine-based delivery, different drug loading concepts and their implications.

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