Saturated five-membered thiazolidines and their derivatives: from synthesis to biological applications

N Sahiba, A Sethiya, J Soni, DK Agarwal… - Topics in Current …, 2020 - Springer
derivatives from 2000 to 2011. In 2013, Jain and coauthors [56] reviewed the multifarious
applications of various thiazolidine-2,4-dione derivatives… -amylase and urease inhibitors. In this …

Discovery and optimization of withangulatin A derivatives as novel glutaminase 1 inhibitors for the treatment of triple-negative breast cancer

WX Zhou, C Chen, XQ Liu, Y Li, YL Lin, XT Wu… - European Journal of …, 2021 - Elsevier
… for novel antitumor GLS1 inhibitors with higher potency, we designed a series of WA derivatives
… of substituents derived from small molecule GLS1 inhibitors via different linkers (Fig.á2). …

Targeting the Subpocket Enables the Discovery of Thiadiazole–Pyridazine Derivatives as Glutaminase C Inhibitors

H Sun, T Du, M Yang, X Liu, X Xue… - ACS Medicinal …, 2023 - ACS Publications
… of the inhibitors in the allosteric pocket (Figure 2b). Inspired by this discovery, we hypothesized
that rationally designed GAC inhibitors would form polar interactions with the P3 hotspot. …

High-throughput screening reveals new glutaminase inhibitor molecules

RK E. Costa, CT Rodrigues… - ACS Pharmacology & …, 2021 - ACS Publications
… in vitro and cellular glutaminase-inhibiting activity. In summary, we discovered a new
glutaminase inhibitor with an … (37) A novel class of thiazolidine-2,4-dione-derived glutaminase

[HTML][HTML] Recent advances in development of glutaminase inhibitors as Anticancer Agents

G Kim, H Joo, JW Jung - Yakhak Hoeji, 2021 - yakhak.org
… developing glutaminase inhibitors as anticancer agents. This review paper described the
current understanding of … Thiazolidine-2,4-dione derivatives KGA 선택적 glutaminase 억제제인 …

Targeting glutaminase 1 (GLS1) by small molecules for anticancer therapeutics

Y Chen, L Tan, J Gao, C Lin, F Wu, Y Li… - European Journal of …, 2023 - Elsevier
… remain the main trend for future research on allosteric inhibitors. However, it is … thiazolidine-2,
4-dione scaffold compounds for the development of GLS1 allosteric inhibitors with novel

[HTML][HTML] Targeting glutaminolysis: new perspectives to understand cancer development and novel strategies for potential target therapies

Z Wang, F Liu, N Fan, C Zhou, D Li, T Macvicar… - Frontiers in …, 2020 - frontiersin.org
… Furthermore, we highlight the glutaminase inhibitor based metabolic therapy strategy and …
Yeh et al. reported a class of thiazolidine-2,4-dione compounds targeting both GLS1 and GLS2…

Alone and together: current approaches to targeting glutaminase enzymes as part of anti-cancer therapies

TTT Nguyen, WP Katt, RA Cerione - Future Drug Discovery, 2023 - Future Science
… lead compounds from other classes of inhibitors that target glutaminase enzymes, many of …
Thiazolidine-2,4-dione derivatives [77] possess unique structures from the previous classes of …

Therapeutic targeting of glutaminolysis as a novel strategy to combat cancer stem cells

TW Kao, YC Chuang, HL Lee, CC Kuo… - International journal of …, 2022 - mdpi.com
… [92], compound 27 (IPN60090) [93], alkyl benzoquinones [94], and thiazolidine-2,4-dione
survived after glutaminase inhibition depend on glycolysis and glycogen synthesis for energy …

The anticancer and EGFR-TK/CDK-9 dual inhibitory potentials of new synthetic pyranopyrazole and pyrazolone derivatives: X-ray crystallography, in vitro, and in silico …

A Musa, SK Ihmaid, DL Hughes, MA Said… - Journal of …, 2023 - Taylor & Francis
… 19 and 20 in both groups are more effective inhibitors than the bromo derivatives; this emphasizes
the … Evaluation of antitumor activity of glutaminase-free periplasmic asparaginase from …