Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors

AKA Bass, MS El-Zoghbi, ESM Nageeb… - European journal of …, 2021 - Elsevier
Despite the encouraging clinical progress of chemotherapeutic agents in cancer treatment,
innovation and development of new effective anticancer candidates still represents a …

Recent updates on thienopyrimidine derivatives as anticancer agents

MTM Sayed, RA Hassan, PA Halim… - Medicinal Chemistry …, 2023 - Springer
Thienopyrimidine derivatives hold a unique place between fused pyrimidine compounds.
They are important and widely represented in medicinal chemistry as they are structural …

Design, synthesis, and antibacterial evaluation of new quinoline-1, 3, 4-oxadiazole and quinoline-1, 2, 4-triazole hybrids as potential inhibitors of DNA gyrase and …

HA Hofny, MFA Mohamed, HAM Gomaa… - Bioorganic …, 2021 - Elsevier
DNA gyrase and topoisomerase IV (topo IV) inhibitors are among the most interesting
antibacterial drug classes without antibacterial pipeline representative. Twenty-four new …

Design of hydrazide-bearing HDACIs based on panobinostat and their p53 and FLT3-ITD dependency in antileukemia activity

X Li, Y Jiang, YK Peterson, T Xu… - Journal of medicinal …, 2020 - ACS Publications
Here, we present a new series of hydrazide-bearing class I selective HDAC inhibitors
designed based on panobinostat. The cap, linker, and zinc-binding group were derivatized …

Synthesis, Intramolecular Cyclization, and Anti-inflammatory Activity of Substituted 2-[2-(4-R-Benzoyl) hydrazinylidene]-4-oxobutanoic Acids

DV Lipin, EI Denisova, DA Shipilovskikh… - Russian Journal of …, 2022 - Springer
The substrate scope of the procedure for the synthesis of 2-[2-(4-R-benzoyl)
hydrazinylidene]-4-oxobutanoic acids was expanded, and their intramolecular cyclization in …

Design and synthesis of novel uracil-linked Schiff bases as dual histone deacetylase type II/topoisomerase type I inhibitors with apoptotic potential

S El-Kalyoubi, SS Elbaramawi, AG Eissa… - Future Medicinal …, 2023 - Taylor & Francis
Aim: The previously reported dual histone deacetylase type II (HDAC II)/topoisomerase type
I (Topo I) inhibitors suffer pharmacokinetic limitations because of their huge molecular …

Design, synthesis and molecular modeling of novel aryl carboximidamides and 3-aryl-1, 2, 4-oxadiazoles derived from indomethacin as potent anti-inflammatory iNOS …

MFA Mohamed, AA Marzouk, A Nafady… - Bioorganic …, 2020 - Elsevier
The development of NSAIDs/iNOS inhibitor hybrids is a new strategy for the treatment of
inflammatory diseases by suppression of the overproduction of PGE 2 and NO. A novel …

Utilization of cyanopyridine in design and synthesis of first-in-class anticancer dual acting PIM-1 kinase/HDAC inhibitors

AKA Bass, ESM Nageeb, MS El-Zoghbi… - Bioorganic …, 2022 - Elsevier
Herein, we report design and synthesis of twenty-one dual PIM-1/HDAC inhibitors utilizing 3-
cyanopyridines as a novel cap moiety linked with aliphatic/aromatic linker bearing carboxylic …

Synthesis and intramolecular cyclization of substituted 4-(Het) aryl-4-oxo-2-thienylaminobut-2-enoic acids containing nitrile group in the thiophene ring

IA Gorbunova, DA Shipilovskikh, AE Rubtsov… - Russian Journal of …, 2021 - Springer
A method for the synthesis of substituted 4-(het) aryl-4-oxo-2-thienylaminobut-2-enoic acids
containing a nitrile substituent in the thiophene ring was proposed. Intramolecular …

Hydrazides as Inhibitors of Histone Deacetylases

MC Carreiras, J Marco-Contelles - Journal of Medicinal Chemistry, 2024 - ACS Publications
In this Perspective, we have brought together available biological evidence on hydrazides
as histone deacetylase inhibitors (HDACis) and as a distinct type of Zn-binding group (ZBG) …