Challenges in the discovery of indoleamine 2, 3-dioxygenase 1 (IDO1) inhibitors

UF Röhrig, SR Majjigapu, P Vogel… - Journal of medicinal …, 2015 - ACS Publications
Since the discovery of indoleamine 2, 3-dioxygenase 1 (IDO1) as an attractive target for
anticancer therapy in 2003, the search for inhibitors has been intensely pursued both in …

Recent advances in the discovery of indoleamine 2, 3-dioxygenase 1 (IDO1) inhibitors

XX Wang, SY Sun, QQ Dong, XX Wu, W Tang… - …, 2019 - pubs.rsc.org
Indoleamine 2, 3-dioxygenase 1 (IDO1), an important immunoregulatory enzyme
ubiquitously expressed in various tissues and cells, plays a key role in tryptophan …

Steric Blockade of Oxy-Myoglobin Oxidation by Thiosemicarbazones: Structure–Activity Relationships of the Novel PPP4pT Series

TP Wijesinghe, B Kaya, MA Gonzálvez… - Journal of Medicinal …, 2023 - ACS Publications
The di-2-pyridylketone thiosemicarbazones demonstrated marked anticancer efficacy,
prompting progression of DpC to clinical trials. However, DpC induced deleterious oxy …

Synthesis, herbicidal activity study and molecular docking of novel pyrimidine thiourea

J Li, Y Wang, Y Wu, R Li, S Liang, J Zhang… - Pesticide Biochemistry …, 2021 - Elsevier
According to the pharmacophore binding strategy and principle of bioelectronic isobaric,
used the sulfonylurea bridge as the parent structure, a series of novel thiourea compounds …

Synthesis and screening of thiosemicarbazide-dithiocarbamate conjugates for antioxidant and anticancer activities

HI Narkhede, AS Dhake, AR Surana - Bioorganic Chemistry, 2022 - Elsevier
Abstract Thiosemicarbazides (TSCs), dithiocarbamates (DTCs) and their molecular
conjugates are promising drug targets. However, hybrids of DTCs with TSCs themselves are …

Coumarin derivatives with potential anticancer and antibacterial activity: Design, synthesis, VEGFR‐2 and DNA gyrase inhibition, and in silico studies

SH Emam, RA Hassan, EO Osman… - Drug Development …, 2023 - Wiley Online Library
A series of coumarin derivatives were designed, synthesized, and evaluated for their
antiproliferative activity. Compound 3e exhibited significant antiproliferative activity and was …

Synthesis, molecular modeling and antiviral activity of novel 5-fluoro-1H-indole-2, 3-dione 3-thiosemicarbazones

ZŞ Sevinçli, GN Duran, M Özbil, N Karalı - Bioorganic Chemistry, 2020 - Elsevier
In this work, novel 5-fluoro-1-methyl/ethyl-1H-indole-2, 3-dione 3-[4-(substituted phenyl)-
thiosemicarbazones] 6a-n and 7a-n were synthesized. The antiviral effects of the …

[HTML][HTML] Novel thiosemicarbazone derivatives: In vitro and in silico evaluation as potential MAO-B inhibitors

D Osmaniye, B Kurban, BN Sağlık, S Levent, Y Özkay… - Molecules, 2021 - mdpi.com
MAO-B inhibitors are frequently used in the treatment of neurodegenerative diseases such
as Parkinson's and Alzheimer's. Due to the limited number of compounds available in this …

Synthesis, structural studies and antimicrobial activities of manganese, nickel and copper complexes of two new tridentate 2‑formylpyridine thiosemicarbazone ligands

ABM Ibrahim, MK Farh, SA El-Gyar… - Inorganic Chemistry …, 2018 - Elsevier
Two new thiosemicarbazone ligands {HL 1= 4‑(2‑chlorophenyl)‑1‑((pyridin‑2‑yl) methylene)
thiosemicarbazide and HL 2= 4‑(2‑methoxyphenyl)‑1‑((pyridin‑2‑yl) methylene) …

Pharmacomodulations of the benzoyl-thiosemicarbazide scaffold reveal antimicrobial agents targeting D-alanyl-D-alanine ligase in bacterio

A Ameryckx, L Pochet, G Wang, E Yildiz… - European Journal of …, 2020 - Elsevier
Abstract d-Alanyl-d-alanine ligase (Ddl) is a validated and attractive target among the
bacterial enzymes involved in peptidoglycan biosynthesis. In the present work, we …