All Outputs (61)

Design, synthesis and biological evaluation of novel 9-N-substituted-13-alkylberberine derivatives from Chinese medicine as anti-hepatocellular carcinoma agents (2023)
Journal Article
Chen, J., Duan, Y., Yang, K., Wang, J., Yan, J., Gu, C., …Xu, J. (2023). Design, synthesis and biological evaluation of novel 9-N-substituted-13-alkylberberine derivatives from Chinese medicine as anti-hepatocellular carcinoma agents. Bioorganic and Medicinal Chemistry, 79, Article 117156. https://doi.org/10.1016/j.bmc.2023.117156

A series of novel 9-N-substituted-13-alkylberberine derivatives from Chinese medicine were designed and synthesized with improved anti-hepatocellular carcinoma (HCC) activities. The optimal compound 4d showed strong activities against HepG2, Sk-Hep-1... Read More about Design, synthesis and biological evaluation of novel 9-N-substituted-13-alkylberberine derivatives from Chinese medicine as anti-hepatocellular carcinoma agents.

Design, synthesis, and biological evaluation of novel protopanoxadiol derivatives based PROTACs technology for the treatment of lung cancer (2022)
Journal Article
Wang, P., Zhu, H., Liu, J., xie, S., Xu, S., Chen, Y., …Xu, J. (2023). Design, synthesis, and biological evaluation of novel protopanoxadiol derivatives based PROTACs technology for the treatment of lung cancer. Bioorganic Chemistry, 131, Article 106327. https://doi.org/10.1016/j.bioorg.2022.106327

Protopanoxadiol is a key active ingredient derived from Panax ginseng that is well-known to exhibit anti-tumor activity. Previous research focused on the natural protopanaxadiol derivative AD-1 has demonstrated that it possesses broad spectrum anti-t... Read More about Design, synthesis, and biological evaluation of novel protopanoxadiol derivatives based PROTACs technology for the treatment of lung cancer.

Current development of bicyclic peptides (2022)
Journal Article
Feng, D., Liu, L., Shi, Y., Du, P., Xu, S., Zhu, Z., …Yao, H. (2023). Current development of bicyclic peptides. Chinese Chemical Letters, 34(6), Article 108026. https://doi.org/10.1016/j.cclet.2022.108026

Bicyclic peptides, a class of polypeptides with two loops within their structure, have emerged as powerful tools in the development of new peptide drugs. They have the potential to bind to challenged drug targets, with antibody-like affinity and sele... Read More about Current development of bicyclic peptides.

Mineral metabolism and ferroptosis in non-alcoholic fatty liver diseases (2022)
Journal Article
Ma, C., Han, L., Zhu, Z., Heng Pang, C., & Pan, G. (2022). Mineral metabolism and ferroptosis in non-alcoholic fatty liver diseases. Biochemical Pharmacology, 205, Article 115242. https://doi.org/10.1016/j.bcp.2022.115242

Nonalcoholic fatty liver disease (NAFLD) has become the most prevalent chronic liver disease worldwide. Minerals including iron, copper, zinc, and selenium, fulfil an essential role in various biochemical processes. Moreover, the identification of fe... Read More about Mineral metabolism and ferroptosis in non-alcoholic fatty liver diseases.

Development of novel 9-O-substituted-13-octylberberine derivatives as potential anti-hepatocellular carcinoma agents (2022)
Journal Article
Chen, J., Duan, Y., Yu, X., Zhong, J., Bai, J., Li, N. G., …Xu, J. (2022). Development of novel 9-O-substituted-13-octylberberine derivatives as potential anti-hepatocellular carcinoma agents. Journal of Enzyme Inhibition and Medicinal Chemistry, 37(1), 2423-2433. https://doi.org/10.1080/14756366.2022.2118268

A series of novel 9-O-substituted-13-octylberberine derivatives were designed, synthesised and evaluated for their anti-hepatocellular carcinoma (HCC) activities. Compound 6k showed the strongest activity against three human hepatoma cells including... Read More about Development of novel 9-O-substituted-13-octylberberine derivatives as potential anti-hepatocellular carcinoma agents.

Design and synthesis of NAD(P)H: Quinone oxidoreductase (NQO1)-activated prodrugs of 23-hydroxybetulinic acid with enhanced antitumor properties (2022)
Journal Article
Zhu, H., Lu, L., Zhu, W., Tan, Y., Duan, Y., Liu, J., …Xu, S. (2022). Design and synthesis of NAD(P)H: Quinone oxidoreductase (NQO1)-activated prodrugs of 23-hydroxybetulinic acid with enhanced antitumor properties. European Journal of Medicinal Chemistry, 240, Article 114575. https://doi.org/10.1016/j.ejmech.2022.114575

A series of NQO1 selectively activated prodrugs were designed and synthesized by introducing indolequinone moiety to the C-3, C-23 or C-28 position of 23-hydroxybetulinic acid (23-HBA) and its analogues. Among them, the representative compound 32j ex... Read More about Design and synthesis of NAD(P)H: Quinone oxidoreductase (NQO1)-activated prodrugs of 23-hydroxybetulinic acid with enhanced antitumor properties.

New Insights into Neuroinflammation Involved in Pathogenic Mechanism of Alzheimer’s Disease and Its Potential for Therapeutic Intervention (2022)
Journal Article
Li, T., Lu, L., Pember, E., Li, X., Zhang, B., & Zhu, Z. (2022). New Insights into Neuroinflammation Involved in Pathogenic Mechanism of Alzheimer’s Disease and Its Potential for Therapeutic Intervention. Cells, 11(12), Article 1925. https://doi.org/10.3390/cells11121925

Alzheimer’s disease (AD) is the most common form of dementia, affecting more than 50 million people worldwide with an estimated increase to 139 million people by 2050. The exact pathogenic mechanisms of AD remain elusive, resulting in the fact that t... Read More about New Insights into Neuroinflammation Involved in Pathogenic Mechanism of Alzheimer’s Disease and Its Potential for Therapeutic Intervention.

Novel and Potent Acetylcholinesterase Inhibitors for the Treatment of Alzheimer’s Disease from Natural (±)-7,8-Dihydroxy-3-methyl-isochroman-4-one (2022)
Journal Article
Li, X., Jia, Y., Li, J., Zhang, P., Li, T., Lu, L., …Xu, J. (2022). Novel and Potent Acetylcholinesterase Inhibitors for the Treatment of Alzheimer’s Disease from Natural (±)-7,8-Dihydroxy-3-methyl-isochroman-4-one. Molecules, 27(10), Article 3090. https://doi.org/10.3390/molecules27103090

Alzheimer’s disease (AD) is a neurodegenerative disease that causes memory and cognitive decline as well as behavioral problems. It is a progressive and well recognized complex disease; therefore, it is very urgent to develop novel and effective anti... Read More about Novel and Potent Acetylcholinesterase Inhibitors for the Treatment of Alzheimer’s Disease from Natural (±)-7,8-Dihydroxy-3-methyl-isochroman-4-one.

Molecular glues modulate protein functions by inducing protein aggregation: A promising therapeutic strategy of small molecules for disease treatment (2022)
Journal Article
Wu, H., Yao, H., He, C., Jia, Y., Zhu, Z., Xu, S., …Xu, J. (2022). Molecular glues modulate protein functions by inducing protein aggregation: A promising therapeutic strategy of small molecules for disease treatment. Acta Pharmaceutica Sinica B, 12(9), 3548-3566. https://doi.org/10.1016/j.apsb.2022.03.019

Molecular glues can specifically induce aggregation between two or more proteins to modulate biological functions. In recent years, molecular glues have been widely used as protein degraders. In addition, however, molecular glues play a variety of vi... Read More about Molecular glues modulate protein functions by inducing protein aggregation: A promising therapeutic strategy of small molecules for disease treatment.

Gastroretentive technologies in tandem with controlled-release strategies: A potent answer to oral drug bioavailability and patient compliance implications (2021)
Journal Article
Vrettos, N. N., Roberts, C. J., & Zhu, Z. (2021). Gastroretentive technologies in tandem with controlled-release strategies: A potent answer to oral drug bioavailability and patient compliance implications. Pharmaceutics, 13(10), 1-36. https://doi.org/10.3390/pharmaceutics13101591

There have been many efforts to improve oral drug bioavailability and therapeutic efficacy and patient compliance. A variety of controlled-release oral delivery systems have been developed to meet these needs. Gastroretentive drug delivery technologi... Read More about Gastroretentive technologies in tandem with controlled-release strategies: A potent answer to oral drug bioavailability and patient compliance implications.

Magnesium isoglycyrrhizinate reduces hepatic lipotoxicity through regulating metabolic abnormalities (2021)
Journal Article
Lu, L., Hao, K., Hong, Y., Liu, J., Zhu, J., Jiang, W., …Peng, Y. (2021). Magnesium isoglycyrrhizinate reduces hepatic lipotoxicity through regulating metabolic abnormalities. International Journal of Molecular Sciences, 22(11), Article 5884. https://doi.org/10.3390/ijms22115884

The excessive accumulation of lipids in hepatocytes induces a type of cytotoxicity called hepatic lipotoxicity, which is a fundamental contributor to liver metabolic diseases (such as NAFLD). Magnesium isoglycyrrhizinate (MGIG), a magnesium salt of t... Read More about Magnesium isoglycyrrhizinate reduces hepatic lipotoxicity through regulating metabolic abnormalities.

Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities (2021)
Journal Article
Zhu, H., Li, W., Shuai, W., Liu, Y., Yang, L., Tan, Y., …Xu, S. (2021). Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities. European Journal of Medicinal Chemistry, 216, Article 113316. https://doi.org/10.1016/j.ejmech.2021.113316

A series of novel N-benzylbenzamide derivatives were designed and synthesized as tubulin polymerization inhibitors. Among fifty-one target compounds, compound 20b exhibited significant antiproliferative activities with IC50 values ranging from 12 to... Read More about Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities.

In vitro and in vivo evaluation of a sustained-release once-a-day formulation of the novel antihypertensive drug MT-1207 (2021)
Journal Article
Vrettos, N.-N., Wang, P., Zhou, Y., Roberts, C. J., Xu, J., Yao, H., & Zhu, Z. (2021). In vitro and in vivo evaluation of a sustained-release once-a-day formulation of the novel antihypertensive drug MT-1207. Pharmaceutical Development and Technology, 26(3), 349-361. https://doi.org/10.1080/10837450.2021.1872087

Hypertension is one of the most common chronic cardiovascular disorders. Sustained-release formulations are developed to maintain drug therapeutic levels throughout the treatment of hypertension, to promote patient compliance and improve patient outc... Read More about In vitro and in vivo evaluation of a sustained-release once-a-day formulation of the novel antihypertensive drug MT-1207.

Design, synthesis and biological evaluation of vinyl selenone derivatives as novel microtubule polymerization inhibitors (2020)
Journal Article
Zhu, H., Sun, H., Liu, Y., Duan, Y., Liu, J., Yang, X., …Xu, J. (2020). Design, synthesis and biological evaluation of vinyl selenone derivatives as novel microtubule polymerization inhibitors. European Journal of Medicinal Chemistry, 207, Article 112716. https://doi.org/10.1016/j.ejmech.2020.112716

A series of novel vinyl selenone derivatives were designed, synthesized and evaluated as the tubulin polymerization inhibitors using a bioisosteric strategy. Among them, the representative compound 11k exhibited satisfactory anti-proliferative activi... Read More about Design, synthesis and biological evaluation of vinyl selenone derivatives as novel microtubule polymerization inhibitors.

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., …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., …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., …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., …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, 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.