Current development of CBP/p300 inhibitors in the last decade

ZX He, BF Wei, X Zhang, YP Gong, LY Ma… - European Journal of …, 2021 - Elsevier
CBP/p300, functioning as histone acetyltransferases and transcriptional co-factors,
represents an attractive target for various diseases, including malignant tumor. The …

Histone acetyltransferase inhibitors: An overview in synthesis, structure-activity relationship and molecular mechanism

M Huang, J Huang, Y Zheng, Q Sun - European Journal of Medicinal …, 2019 - Elsevier
Acetylation, a key component in post-translational modification regulated by HATs and
HDACs, is relevant to many crucial cellular contexts in organisms. Based on crucial …

Lysine acetyltransferase inhibitors from natural sources

F Fiorentino, A Mai, D Rotili - Frontiers in Pharmacology, 2020 - frontiersin.org
Acetylation of histone and non-histone protein lysine residues has been widely described as
a critical modulator of several cell functions in humans. Lysine acetyltransferases (KATs) …

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

NJ Basha, SM Basavarajaiah - Chemical Biology & Drug …, 2022 - Wiley Online Library
Histone‐modifying enzymes are the key regulators involved in the post‐translational
modification of histone and non‐histone. These enzymes are responsible for the epigenetic …

First-in-class selective inhibitors of the lysine acetyltransferase KAT8

F Fiorentino, S Sementilli, M Menna… - Journal of Medicinal …, 2023 - ACS Publications
KAT8 is a lysine acetyltransferase primarily catalyzing the acetylation of Lys16 of histone H4
(H4K16). KAT8 dysregulation is linked to the development and metastatization of many …

Anticancer potential of bioactive molecule luteolin and its analogs: an update

NJ Basha, SM Basavarajaiah - Polycyclic Aromatic Compounds, 2023 - Taylor & Francis
Literature evidence that natural products are potential bioactive components for lead
compounds in drug discovery. These molecules have distinctive chemical structures that …

Quinoline: Synthesis to application

RK Mittal, M Aggarwal, K Khatana… - Medicinal …, 2023 - ingentaconnect.com
This review aims to provide a comprehensive report on the quinoline ring with respect to its
synthesis, reactivity, and therapeutic values. The reactivity of quinoline for the metal …

Cascade Knoevenagel and aza-Wittig reactions for the synthesis of substituted quinolines and quinolin-4-ols

X Zhang, X Ma, W Qiu, J Evans, W Zhang - Green Chemistry, 2019 - pubs.rsc.org
A [4+ 2] annulation involving cascade Knoevenagel, aza-Wittig and dehydrofluorination
reactions is developed for the synthesis of substituted quinolin-4-ols including analogs …

Evaluation of a large library of (thiazol-2-yl) hydrazones and analogues as histone acetyltransferase inhibitors: enzyme and cellular studies

S Carradori, D Rotili, C De Monte, A Lenoci… - European journal of …, 2014 - Elsevier
Recently we described some (thiazol-2-yl) hydrazones as antiprotozoal, antifungal and anti-
MAO agents as well as Gcn5 HAT inhibitors. Among these last compounds, CPTH2 and …

[HTML][HTML] Histone acetyltransferase inhibitor CPTH6 preferentially targets lung cancer stem-like cells

M Di Martile, M Desideri, T De Luca, C Gabellini… - Oncotarget, 2016 - ncbi.nlm.nih.gov
Cancer stem cells (CSCs) play an important role in tumor initiation, progression, therapeutic
failure and tumor relapse. In this study, we evaluated the efficacy of the thiazole derivative 3 …