Design, synthesis, and evaluation of thiazolidine-2, 4-dione derivatives as a novel class of glutaminase inhibitors
TK Yeh, CC Kuo, YZ Lee, YY Ke, KF Chu… - Journal of Medicinal …, 2017 - ACS Publications
… in more options for developing GA inhibitors into therapeutic agents. Herein, we report a
novel class of thiazolidine-2,4-dione derived glutaminase inhibitors that preferentially inhibit the …
novel class of thiazolidine-2,4-dione derived glutaminase inhibitors that preferentially inhibit the …
Recent progress in the discovery of allosteric inhibitors of kidney-type glutaminase
SC Zimmermann, B Duvall… - Journal of medicinal …, 2018 - ACS Publications
… in the chronological order of discovery, herein we report the representative classes of
BPTES-derived GLS inhibitors in a way that allows readers to appreciate how molecular structures …
BPTES-derived GLS inhibitors in a way that allows readers to appreciate how molecular structures …
Overview of the development of glutaminase inhibitors: achievements and future directions
X Xu, Y Meng, L Li, P Xu, J Wang, Z Li… - Journal of medicinal …, 2018 - ACS Publications
… binding site for novel allosteric inhibitors which bind GLS1 at … In summary, this series of
thiazolidine-2,4-dione compounds … a novel backbone for the development of GLS inhibitors. …
thiazolidine-2,4-dione compounds … a novel backbone for the development of GLS inhibitors. …
Saturated five-membered thiazolidines and their derivatives: from synthesis to biological applications
… 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 …
applications of various thiazolidine-2,4-dione derivatives… -amylase and urease inhibitors. In this …
Novel 1, 3, 4-selenadiazole-containing kidney-type glutaminase inhibitors showed improved cellular uptake and antitumor activity
Z Chen, D Li, N Xu, J Fang, Y Yu, W Hou… - Journal of medicinal …, 2018 - ACS Publications
… 6, (9) UPGL00004, (10) thiazolidine-2,4-dione derivatives, (11) and CB839, (12) as shown
in Figure 1. Thiazolidine-2,4-dione derivatives contain a Michael acceptor and react to KGA …
in Figure 1. Thiazolidine-2,4-dione derivatives contain a Michael acceptor and react to KGA …
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). …
… of substituents derived from small molecule GLS1 inhibitors via different linkers (Fig.á2). …
Recent development of small molecule glutaminase inhibitors
M Song, SH Kim, CY Im… - Current topics in medicinal …, 2018 - ingentaconnect.com
… In this review, recent efforts to develop small molecule glutaminase inhibitors that target
glutamine metabolism in both … Design, synthesis, and evaluation of thiazolidine2,4-dione …
glutamine metabolism in both … Design, synthesis, and evaluation of thiazolidine2,4-dione …
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. …
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 …
glutaminase inhibitor with an … (37) A novel class of thiazolidine-2,4-dione-derived glutaminase …
Discovery and development of small molecule modulators targeting glutamine metabolism
L Li, Y Meng, Z Li, W Dai, X Xu, X Bi, J Bian - European journal of medicinal …, 2019 - Elsevier
… In summary, a novel series of thiazolidine-2,4-dione derivatives were designed,
synthesized, and evaluated as glutaminase inhibitors in this research. These potent analogues …
synthesized, and evaluated as glutaminase inhibitors in this research. These potent analogues …