An insight into therapeutic efficacy of heterocycles as histone‐modifying enzyme inhibitors that targets cancer epigenetic pathways

Abstract

The word histone modification refers to variable and heritable phenotype of histone without DNA sequence transformation (Macchia et al., 2021;Morgan & Shilatifard, 2020;Sun et al., 2021). This post-translational modification involves acetylation, methylation, phosphorylation, and ubiquitinoylation. These biochemical mechanisms require histone-modifying enzymes, histone acetyltransferases (HAT), deacetylases (HDAC), methyltransferases (HMT), demethylases (HDM), DNA methyltransferases (DNMT), and Kinases, to play a vital role in germ cell development and embryo formation (

Insight on Heterocycles as p53‐MDM2 Protein‐Protein Interaction Inhibitors: Molecular Mechanism for p53 Activation

“…With the best of our experience, we have included heterocycles derived from natural sources that affect this transcription factor. [32][33][34][35][36][37] Heterocycles, as potent p53-MDM2 interaction inhibitors and p53 activators listed in the Table 1.…”

Synthesis and Antiviral Efficacy of Pyrimidine Analogs Targeting Viral Pathways

“…Further, most of the antivirals belong to the class of pyrimidines, fused pyrimidines, and their nucleoside analogs [146,147] . Like safe vaccine development, there are challenges for antiviral drugs like low bioavailability, toxicity, and non‐specificity [148–150] . We are involved in the design, synthesis, and biological activities of substituted pyrimidines and other heterocycles that target epigenetic pathways responsible for disorders such as cancer, inflammation, and viral infection [151,152] .…”

“…Like safe vaccine development, there are challenges for antiviral drugs like low bioavailability, toxicity, and non-specificity. [148][149][150] We are involved in the design, synthesis, and biological activities of substituted pyrimidines and other heterocycles that target epigenetic pathways responsible for disorders such as cancer, inflammation, and viral infection. [151,152] Herein, we cover in this review the antiviral significance of pyrimidines and provide a diverse platform for the researchers to develop potent analogs to overcome the problems associated with present hybrids as medicinal drugs and vaccination for the benefit of society.…”

Synthesis, Antimicrobial Activity, and Drug-likeness profiles of 5-Phenylselenanyl-2-benzylthiopyrimidine Analogs

“…Whereas-other nitrogen and sulfurcontaining 5-membered heterocycles like thiazolidinone are also known for their diverse biological activities [7][8][9]. In continuation of our research work on isolation and synthesis of potent molecules derived from either natural products or by synthetic route [10][11][12][13] and also because of a literature survey on the importance of pyrimidine-bearing thiazolidinone [14], here in reporting synthesis and antimicrobial activity of (5-phenylselenanyl-2-benzylthio-pyrimidin-4-yl) thiazolidin-4-one analogs 4 (a, b).…”