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Dr ZHEYING ZHU's Outputs (67)

Corrigendum to “Design, synthesis and anticancer properties of isocombretapyridines as potent colchicine binding site inhibitors” [Eur. J. Med. Chem. 197 (2020) 112308] (European Journal of Medicinal Chemistry (2020) 197, (S0223523420302774), (10.1016/j.ejmech.2020.112308)) (2020)
Journal Article
Shuai, W., Li, X., Li, W., Xu, F., Lu, L., Yao, H., Yang, L., Zhu, H., Xu, S., Zhu, Z., & Xu, J. (2020). Corrigendum to “Design, synthesis and anticancer properties of isocombretapyridines as potent colchicine binding site inhibitors” [Eur. J. Med. Chem. 197 (2020) 112308] (European Journal of Medicinal Chemistry (2020) 197, (S0223523420302774), (10.1016/j.ejmech.2020.112308)). European Journal of Medicinal Chemistry, 200, Article 112464. https://doi.org/10.1016/j.ejmech.2020.112464

Design, synthesis and anticancer properties of isocombretapyridines as potent colchicine binding site inhibitors (2020)
Journal Article
Shuai, W., Li, X., Li, W., Xu, F., Lu, L., Yao, H., Yang, L., Zhu, H., Xu, S., Zhu, Z., & Xu, J. (2020). Design, synthesis and anticancer properties of isocombretapyridines as potent colchicine binding site inhibitors. European Journal of Medicinal Chemistry, 197, Article 112308. https://doi.org/10.1016/j.ejmech.2020.112308

A series of novel isocombretapyridines were designed and synthesized based on a lead compound isocombretastatin A-4 (isoCA-4) by replacing 3,4,5-trimethoxylphenyl with substituent pyridine nucleus. The MTT assay results showed that compound 20a posse... Read More about Design, synthesis and anticancer properties of isocombretapyridines as potent colchicine binding site inhibitors.

Design, synthesis and molecular modeling of isothiochromanone derivatives as acetylcholinesterase inhibitors (2019)
Journal Article
Shuai, W., Li, W., Yin, Y., Yang, L., Xu, F., Xu, S., Yao, H., Zhu, Z., & Xu, J. (2019). Design, synthesis and molecular modeling of isothiochromanone derivatives as acetylcholinesterase inhibitors. Future Medicinal Chemistry, 11(20), 2687-2699. https://doi.org/10.4155/fmc-2019-0125

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
Lu, L., Zhang, H., Liu, J., Liu, Y., Wang, Y., Xu, S., Zhu, Z., & Xu, J. (2019). Synthesis, biological evaluation and mechanism studies of C-23 modified 23-hydroxybetulinic acid derivatives as anticancer agents. European Journal of Medicinal Chemistry, 182, Article 111659. https://doi.org/10.1016/j.ejmech.2019.111659

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
Zhang, P., Xu, S., Zhu, Z., & Xu, J. (2019). Multi-target design strategies for the improved treatment of Alzheimer's disease. European Journal of Medicinal Chemistry, 176, 228-247. https://doi.org/10.1016/j.ejmech.2019.05.020

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.

Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates (2019)
Journal Article
Xie, S., Li, X., Yu, H., Zhang, P., Wang, J., Wang, C., Xu, S., Wu, Z., Liu, J., Zhu, Z., & Xu, J. (2019). Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates. Bioorganic and Medicinal Chemistry, 27(13), 2764-2770. https://doi.org/10.1016/j.bmc.2019.05.004

7,8 Dihydroxy 3 methyl isochromanone 4 XJP is a polyphenolic natural product with moderate antihypertensive activity. T o obtain new agents with stronger potency and safer profile , we employed XJP and naftopidil as the lead compound s t o design and... Read More about Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.

Controllable thioester-based hydrogen sulfide slow-releasing donors as cardioprotective agents (2019)
Journal Article
Yao, H., Luo, S., Liu, J., Xie, S., Liu, Y., Xu, J., Zhu, Z., & Xu, S. (2019). Controllable thioester-based hydrogen sulfide slow-releasing donors as cardioprotective agents. Chemical Communications, 55(44), 6193-6196. https://doi.org/10.1039/c9cc02829c

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
Xu, F., Li, W., Shuai, W., Yang, L., Bi, Y., Ma, C., Yao, H., Xu, S., Zhu, Z., & Xu, J. (2019). Design, synthesis and biological evaluation of pyridine-chalcone derivatives as novel microtubule-destabilizing agents. European Journal of Medicinal Chemistry, 173, 1-14. https://doi.org/10.1016/j.ejmech.2019.04.008

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
Yao, H., Xu, F., Wang, G., Xie, S., Li, W., Yao, H., Ma, C., Zhu, Z., Xu, J., & Xu, S. (2019). Design, synthesis, and biological evaluation of truncated deguelin derivatives as Hsp90 inhibitors. European Journal of Medicinal Chemistry, 167, 485-498. https://doi.org/10.1016/j.ejmech.2019.02.014

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.

Discovery of novel quinoline–chalcone derivatives as potent antitumor agents with microtubule polymerization inhibitory activity (2018)
Journal Article
Li, W., Xu, F., Shuai, W., Sun, H., Yao, H., Ma, C., Xu, S., Yao, H., Zhu, Z., Yang, D.-H., Chen, Z.-S., & Xu, J. (2019). Discovery of novel quinoline–chalcone derivatives as potent antitumor agents with microtubule polymerization inhibitory activity. Journal of Medicinal Chemistry, 62(2), 993-1013. https://doi.org/10.1021/acs.jmedchem.8b01755

© 2018 American Chemical Society. A series of novel quinoline-chalcone derivatives were designed, synthesized, and evaluated for their antiproliferative activity. Among them, compound 24d exhibited the most potent activity with IC 50 values ranging... Read More about Discovery of novel quinoline–chalcone derivatives as potent antitumor agents with microtubule polymerization inhibitory activity.

Synthesis, molecular properties prediction and biological evaluation of indole-vinyl sulfone derivatives as novel tubulin polymerization inhibitors targeting the colchicine binding site (2018)
Journal Article
Li, W., Sun, H., Xu, F., Shuai, W., Liu, J., Xu, S., Yao, H., Ma, C., Zhu, Z., & Xu, J. (2019). Synthesis, molecular properties prediction and biological evaluation of indole-vinyl sulfone derivatives as novel tubulin polymerization inhibitors targeting the colchicine binding site. Bioorganic Chemistry, 85, 49-59. https://doi.org/10.1016/j.bioorg.2018.12.015

Twenty-two novel indole-vinyl sulfone derivatives were designed, synthesized and evaluated as tubulin polymerization inhibitors. The physicochemical and drug-likeness properties of all target compounds were predicted by Osiris calculations. All compo... Read More about Synthesis, molecular properties prediction and biological evaluation of indole-vinyl sulfone derivatives as novel tubulin polymerization inhibitors targeting the colchicine binding site.

Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site (2018)
Journal Article
Li, W., Shuai, W., Sun, H., Xu, F., Bi, Y., Xu, J., Ma, C., Yao, H., Zhu, Z., & Xu, S. (2019). Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site. European Journal of Medicinal Chemistry, 163, 428-442. https://doi.org/10.1016/j.ejmech.2018.11.070

A series of novel isocombretastatin A-4 (isoCA-4) analogs were designed and synthesized by replacing 3,4,5-trimethoylphenyl and isovanillin of isoCA-4 with quinoline and indole moieties, respectively. The structure activity relationships (SARs) of th... Read More about Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.

Small molecules as inhibitors of PCSK9: current status and future challenges (2018)
Journal Article
Xu, S., Luo, S., Zhu, Z., & Xu, J. (2019). Small molecules as inhibitors of PCSK9: current status and future challenges. European Journal of Medicinal Chemistry, 162, 212-233. https://doi.org/10.1016/j.ejmech.2018.11.011

Proprotein convertase subtilisin/kexin type 9 (PCSK9) plays an important role in regulating lipoprotein metabolism by binding to low-density lipoprotein receptors (LDLRs), leading to their degradation. LDL cholesterol (LDL-C) lowering drugs that oper... Read More about Small molecules as inhibitors of PCSK9: current status and future challenges.

Synthesis, Biological Evaluation of Fluorescent 23-Hydroxybetulinic Acid Probes, and Their Cellular Localization Studies (2018)
Journal Article
Yao, H., Wei, G., Liu, Y., Yao, H., Zhu, Z., Ye, W., Wu, X., Xu, J., & Xu, S. (2018). Synthesis, Biological Evaluation of Fluorescent 23-Hydroxybetulinic Acid Probes, and Their Cellular Localization Studies. ACS Medicinal Chemistry Letters, 9(10), 1030-1034. https://doi.org/10.1021/acsmedchemlett.8b00321

© 2018 American Chemical Society. 23-Hydroxybetulinic acid (23-HBA) is a complex lupane triterpenoid, which has attracted increasing attention as an anticancer agent. However, its detailed mechanism of anticancer action remains elusive so far. To rev... Read More about Synthesis, Biological Evaluation of Fluorescent 23-Hydroxybetulinic Acid Probes, and Their Cellular Localization Studies.

Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities (2018)
Journal Article
Li, W., Yin, Y., Yao, H., Shuai, W., Sun, H., Xu, S., Liu, J., Yao, H., Zhu, Z., & Xu, J. (2018). Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities. European Journal of Medicinal Chemistry, 157, 1068-1080. https://doi.org/10.1016/j.ejmech.2018.08.074

Vinyl sulfone or sulfoxide moieties were firstly introduced to the structure of chalcone compound by replacing the carbonyl group to afford a series of novel compounds as potential anti-tubulin agents. All of the target compounds were evaluated for t... Read More about Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities.

Design, synthesis, biological evaluation and docking study of 4-isochromanone hybrids bearing N-benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors (part II) (2017)
Journal Article
Wang, J., Wang, C., Wu, Z., Li, X., Xu, S., Liu, J., Lan, Q., Zhu, Z., & Xu, J. (2018). Design, synthesis, biological evaluation and docking study of 4-isochromanone hybrids bearing N-benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors (part II). Chemical Biology and Drug Design, 91(3), 756-762. https://doi.org/10.1111/cbdd.13136

A series of novel 4-isochromanone compounds bearing N-benzyl pyridinium moiety were designed and synthesized as acetylcholinesterase (AChE) inhibitors. The biological evaluation showed that most of the target compounds exhibited potent inhibitory act... Read More about Design, synthesis, biological evaluation and docking study of 4-isochromanone hybrids bearing N-benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors (part II).

Tubulin inhibitors targeting the colchicine binding site: a perspective of privileged structures (2017)
Journal Article
Li, W., Sun, H., Xu, S., Zhu, Z., & Xu, J. (in press). Tubulin inhibitors targeting the colchicine binding site: a perspective of privileged structures. Future Medicinal Chemistry, 9(15), https://doi.org/10.4155/fmc-2017-0100

The vital roles of microtubule in mitosis and cell division make it an attractive target for antitumor therapy. Colchicine binding site of tubulin is one of the most important pockets that have been focused on to design tubulin-destabilizing agents.... Read More about Tubulin inhibitors targeting the colchicine binding site: a perspective of privileged structures.

6,7-seco-ent-kauranoids derived from oridonin as potential anticancer agents (2017)
Journal Article
Xu, S., Yao, H., Hu, M., Li, D., Zhu, Z., Xie, W., Yao, H., Wu, L., Chen, Z.-S., & Xu, J. (in press). 6,7-seco-ent-kauranoids derived from oridonin as potential anticancer agents. Journal of Natural Products, https://doi.org/10.1021/acs.jnatprod.7b00057

Structurally unique 6,7-seco-ent-kaurenes, which are widely distributed in the genus Isodon, have attracted considerable attention because of their antitumor activities. Previously, a convenient conversion of commercially available oridonin (1) to 6,... Read More about 6,7-seco-ent-kauranoids derived from oridonin as potential anticancer agents.