Research progress of mTOR inhibitors

Y Chen, X Zhou - European journal of medicinal chemistry, 2020 - Elsevier
Mammalian target of rapamycin (mTOR) is a highly conserved Serine/Threonine (Ser/Thr)
protein kinase, which belongs to phosphatidylinositol-3-kinase-related kinase (PIKK) protein …

Targeting the PI3K/AKT/mTOR signaling pathway in the treatment of human diseases: Current status, trends, and solutions

J Huang, L Chen, J Wu, D Ai, JQ Zhang… - Journal of medicinal …, 2022 - ACS Publications
The phosphoinositide 3-kinase (PI3K)/protein kinase B (AKT)/mammalian target of
rapamycin (mTOR) pathway is one of the most important intracellular pathways involved in …

Covalent proximity scanning of a distal cysteine to target PI3Kα

C Borsari, E Keles, JA McPhail… - Journal of the …, 2022 - ACS Publications
Covalent protein kinase inhibitors exploit currently noncatalytic cysteines in the adenosine
5′-triphosphate (ATP)-binding site via electrophiles directly appended to a reversible …

Sulfone Electrophiles in Cross-Electrophile Coupling: Nickel-Catalyzed Difluoromethylation of Aryl Bromides

BK Chi, SJ Gavin, BN Ahern, N Peperni, S Monfette… - ACS …, 2024 - ACS Publications
Fluoroalkyl fragments have played a critical role in the design of pharmaceutical and
agrochemical molecules in recent years due to the enhanced biological properties of …

Antitumor activity of s-triazine derivatives: a systematic review

Q Dai, Q Sun, X Ouyang, J Liu, L Jin, A Liu, B He, T Fan… - Molecules, 2023 - mdpi.com
1, 3, 5-triazine derivatives, also called s-triazines, are a series of containing-nitrogen
heterocyclic compounds that play an important role in anticancer drug design and …

A high affinity pan-PI3K binding module supports selective targeted protein degradation of PI3Kα

WT Jauslin, M Schild, T Schaefer, C Borsari… - Chemical …, 2024 - pubs.rsc.org
Class I phosphoinositide 3-kinases (PI3Ks) control cellular growth, but are also essential in
insulin signaling and glucose homeostasis. Pan-PI3K inhibitors thus generate substantial …

Design, synthesis and bioevaluation of novel substituted triazines as potential dual PI3K/mTOR inhibitors

TT Wu, QQ Guo, ZL Chen, LL Wang, Y Du… - European Journal of …, 2020 - Elsevier
A series of novel substituted triazines bearing a benzimidazole scaffold were designed and
synthesized based on the structures of known anti-cancer agents, namely gedatolisib and …

Discovery of novel 1, 3, 5-triazine derivatives as potent inhibitor of cervical cancer via dual inhibition of PI3K/mTOR

J Hu, Y Zhang, N Tang, Y Lu, P Guo, Z Huang - Bioorganic & Medicinal …, 2021 - Elsevier
This study describes the synthesis of novel 1, 3, 5-triazine derivatives as potent inhibitors of
cervical cancer. The compounds were initially tested for inhibition of PI3K/mTOR, where they …

Synthesis, molecular docking, in vitro and in vivo studies of novel dimorpholinoquinazoline-based potential inhibitors of PI3K/Akt/mTOR Pathway

MV Zapevalova, ES Shchegravina, IP Fonareva… - International journal of …, 2022 - mdpi.com
A (series) range of potential dimorpholinoquinazoline-based inhibitors of the PI3K/Akt/mTOR
cascade was synthesized. Several compounds exhibited cytotoxicity towards a panel of …

Synthesis and bioevaluation of diaryl urea derivatives as potential antitumor agents for the treatment of human colorectal cancer

CF Wu, QC Wang, R Chen, HL Zhou, TT Wu… - European Journal of …, 2022 - Elsevier
The development of inhibitors targeting the PI3K-Akt-mTOR signaling pathway has been
greatly hindered by the on-target AEs, such as hyperglycemia and hepatotoxicities. In this …