Design, synthesis, and biological evaluation of truncated deguelin derivatives as Hsp90 inhibitors

Yao, Hong; Xu, Feijie; Wang, Guangyu; Xie, Shaowen; Li, Wenlong; Yao, Hequan; Ma, Cong; Zhu, Zheying; Xu, Jinyi; Xu, Shengtao

doi:10.1016/j.ejmech.2019.02.014

All Outputs (6)

Design, synthesis and molecular modeling of isothiochromanone derivatives as acetylcholinesterase inhibitors (2019)
Journal Article

A series of novel isothio- and isoselenochromanone derivatives bearing N-benzyl pyridinium moiety were designed, synthesized and evaluated as acetylcholinesterase (AChE) inhibitors. Results: Most of the target compounds exhibited potent anti-AChE act... Read More about Design, synthesis and molecular modeling of isothiochromanone derivatives as acetylcholinesterase inhibitors.

Synthesis, biological evaluation and mechanism studies of C-23 modified 23-hydroxybetulinic acid derivatives as anticancer agents (2019)
Journal Article

A series of C-23 modified 23-hydroxybetulinic acid (HBA) derivatives were synthesized and evaluated for their antiproliferative activity against a panel of cancer cell lines (A2780, A375, B16, MCF-7 and HepG2). The biological screening results showed... Read More about Synthesis, biological evaluation and mechanism studies of C-23 modified 23-hydroxybetulinic acid derivatives as anticancer agents.

Multi-target design strategies for the improved treatment of Alzheimer's disease (2019)
Journal Article

Alzheimer's disease (AD) is a multifactorial syndrome resulting in profound misery and poses a substantial burden on human health, economy, and society throughout the world. Based on the numerous AD-related targets in the disease network, multi-targe... Read More about Multi-target design strategies for the improved treatment of Alzheimer's disease.

Controllable thioester-based hydrogen sulfide slow-releasing donors as cardioprotective agents (2019)
Journal Article

Hydrogen sulfide (H2S) is an important signaling molecule with promising protective effects in many physiological and pathological processes. However, the study of H2S has been impeded by the lack of appropriate H2S donors that could mimic its slow-r... Read More about Controllable thioester-based hydrogen sulfide slow-releasing donors as cardioprotective agents.

Design, synthesis and biological evaluation of pyridine-chalcone derivatives as novel microtubule-destabilizing agents (2019)
Journal Article

Further optimization of the trimethoxyphenyl scaffold of parent chalcone compound (2a) by introducing a pyridine ring afforded a series of novel pyridine-chalcone derivatives as potential anti-tubulin agents. All the target compounds were evaluated f... Read More about Design, synthesis and biological evaluation of pyridine-chalcone derivatives as novel microtubule-destabilizing agents.

Design, synthesis, and biological evaluation of truncated deguelin derivatives as Hsp90 inhibitors (2019)
Journal Article

A series of novel B and C-rings truncated deguelin derivatives have been designed and synthesized in the present study as heat shock protein 90 (Hsp90) inhibitors. The synthesized compounds exhibited micromolar antiproliferative potency toward a pane... Read More about Design, synthesis, and biological evaluation of truncated deguelin derivatives as Hsp90 inhibitors.