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An overview on applications of SwissADME web tool in the design and development of anticancer, antitubercular and antimicrobial agents: a medicinal chemist's …
B Bakchi, AD Krishna, E Sreecharan… - Journal of Molecular …, 2022 - Elsevier
Recently, in silico techniques have gained tremendous popularity in the field of small
molecule drug discovery. The computational jobs include not only hit generation, lead …
molecule drug discovery. The computational jobs include not only hit generation, lead …
[HTML][HTML] Pathological role of HDAC8: cancer and beyond
JY Kim, H Cho, J Yoo, GW Kim, YH Jeon, SW Lee… - Cells, 2022 - mdpi.com
Histone deacetylase 8 (HDAC8) is a class I HDAC that catalyzes the deacetylation of histone
and non-histone proteins. As one of the best-characterized isoforms, numerous studies have …
and non-histone proteins. As one of the best-characterized isoforms, numerous studies have …
[HTML][HTML] A therapeutic perspective of HDAC8 in different diseases: an overview of selective inhibitors
Histone deacetylases (HDACs) are epigenetic enzymes which participate in transcriptional
repression and chromatin condensation mechanisms by removing the acetyl moiety from …
repression and chromatin condensation mechanisms by removing the acetyl moiety from …
[HTML][HTML] Significance of five-membered heterocycles in human histone deacetylase inhibitors
A Frühauf, M Behringer, FJ Meyer-Almes - Molecules, 2023 - mdpi.com
Five-membered heteroaromatic rings, in particular, have gained prominence in medicinal
chemistry as they offer enhanced metabolic stability, solubility and bioavailability, crucial …
chemistry as they offer enhanced metabolic stability, solubility and bioavailability, crucial …
Contribution of Knoevenagel condensation products toward the development of anticancer agents: An updated review
Knoevenagel condensation is an entrenched, prevailing, prominent arsenal following
greener principles in the generation of α, β‐unsaturated ketones/carboxylic acids by …
greener principles in the generation of α, β‐unsaturated ketones/carboxylic acids by …
Synthesis, antitumor, and apoptosis-inducing activities of novel 5-arylidenethiazolidine-2, 4-dione derivatives: histone deacetylases inhibitory activity and molecular …
The antitumor activity of the newly synthesized 5-arylidenethiazolidine-2, 4-dione derivatives
18a–f and 19a–f was investigated, compared to doxorubicin (IC 50= 4.17–8.87 μM) and …
18a–f and 19a–f was investigated, compared to doxorubicin (IC 50= 4.17–8.87 μM) and …
[HTML][HTML] Non-hydroxamate zinc-binding groups as warheads for histone deacetylases
A Frühauf, FJ Meyer-Almes - Molecules, 2021 - mdpi.com
Histone deacetylases (HDACs) remove acetyl groups from acetylated lysine residues and
have a large variety of substrates and interaction partners. Therefore, it is not surprising that …
have a large variety of substrates and interaction partners. Therefore, it is not surprising that …
Structure-based inhibitor discovery of class I histone deacetylases (HDACs)
Y Luo, H Li - International journal of molecular sciences, 2020 - mdpi.com
Class I histone deacetylases (HDACs) are promising targets for epigenetic therapies for a
range of diseases such as cancers, inflammations, infections and neurological diseases …
range of diseases such as cancers, inflammations, infections and neurological diseases …
Discovery of novel N-substituted thiazolidinediones (TZDs) as HDAC8 inhibitors: in-silico studies, synthesis, and biological evaluation
Epigenetics plays a fundamental role in cancer progression, and develo** agents that
regulate epigenetics is crucial for cancer management. Among Class I and Class II HDACs …
regulate epigenetics is crucial for cancer management. Among Class I and Class II HDACs …
Synthesis, molecular modelling and pharmacological evaluation of novel indole-thiazolidinedione based hybrid analogues as potential pancreatic lipase inhibitors
A series of novel indole-thiazolidinedione hybrid analogues (7a to 7 u) were synthesised,
characterised and evaluated for their potential Pancreatic Lipase (PL) inhibition. Amongst …
characterised and evaluated for their potential Pancreatic Lipase (PL) inhibition. Amongst …