All Outputs (60)

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., …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., …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, 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., …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., …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.

Discovery of novel quinazolines as potential anti-tubulin agents occupying three zones of colchicine domain (2018)
Journal Article
Li, W., Yin, Y., Shuai, W., Xu, F., Yao, H., Liu, J., …Xu, S. (2019). Discovery of novel quinazolines as potential anti-tubulin agents occupying three zones of colchicine domain. Bioorganic Chemistry, 83, 380-390. https://doi.org/10.1016/j.bioorg.2018.10.027

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., …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 4-Arylisochromenes as Anticancer Agents Inhibiting Tubulin Polymerization (2018)
Journal Article
Li, W., Shuai, W., Xu, F., Sun, H., Xu, S., Yao, H., …Xu, J. (2018). Discovery of Novel 4-Arylisochromenes as Anticancer Agents Inhibiting Tubulin Polymerization. ACS Medicinal Chemistry Letters, 9(10), 974-979. https://doi.org/10.1021/acsmedchemlett.8b00217

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., …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., …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., …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.

Identification, characterization, and quantification of impurities of safinamide mesilate: Process-related impurities and degradation products (2017)
Journal Article
Zou, L., Sun, L., Zhang, H., Hui, W., Zou, Q., & Zhu, Z. (2017). Identification, characterization, and quantification of impurities of safinamide mesilate: Process-related impurities and degradation products. Journal of AOAC INTERNATIONAL, 100(4), 1029-1037. https://doi.org/10.5740/jaoacint.16-0218

The characterization of process-related impurities and degradation products of safinamide mesilate (SAFM) in bulk drug and a stability-indicating HPLC method for the separation and quantification of all the impurities were investigated. Four process-... Read More about Identification, characterization, and quantification of impurities of safinamide mesilate: Process-related impurities and degradation products.

Novel hybrids of natural β-elemene bearing isopropanolamine moieties: synthesis, enhanced anticancer profile, and improved aqueous solubility (2017)
Journal Article
Chen, J., Wang, T., Xu, S., Aijun, L., Yao, H., Xie, W., …Xu, J. (2017). Novel hybrids of natural β-elemene bearing isopropanolamine moieties: synthesis, enhanced anticancer profile, and improved aqueous solubility. Fitoterapia, 120, https://doi.org/10.1016/j.fitote.2017.05.002

A series of novel β-elemene isopropanolamine derivatives were synthesized and evaluated for their antitumor activity. The results indicated that all of the compounds showed stronger antiproliferative activities than β-elemene as well as improved aque... Read More about Novel hybrids of natural β-elemene bearing isopropanolamine moieties: synthesis, enhanced anticancer profile, and improved aqueous solubility.

Discovery of novel antitumor nitric oxide-donating β-elemene hybrids through inhibiting the PI3K/Akt pathway (2017)
Journal Article
Chen, J., Wang, T., Xu, S., Zhang, P., Lin, A., Wu, L., …Xu, J. (2017). Discovery of novel antitumor nitric oxide-donating β-elemene hybrids through inhibiting the PI3K/Akt pathway. European Journal of Medicinal Chemistry, 135, https://doi.org/10.1016/j.ejmech.2017.04.045

A series of novel furoxan-based NO-donating b-elemene hybrids were designed and synthesized to improve the anticancer efficacy of natural b-elemene. The bioassay results indicated that all of the target compounds exhibited significantly improved anti... Read More about Discovery of novel antitumor nitric oxide-donating β-elemene hybrids through inhibiting the PI3K/Akt pathway.

Design, synthesis, and biological evaluation of NAD(P)H: quinone oxidoreductase (NQO1)-targeted oridonin prodrugs possessing indolequinone moiety for hypoxia-selective activation (2017)
Journal Article
Xu, S., Yao, H., Pei, L., Hu, M., Li, D., Qiu, Y., …Xu, J. (2017). Design, synthesis, and biological evaluation of NAD(P)H: quinone oxidoreductase (NQO1)-targeted oridonin prodrugs possessing indolequinone moiety for hypoxia-selective activation. European Journal of Medicinal Chemistry, 132, https://doi.org/10.1016/j.ejmech.2017.03.055

The enzyme NQO1 is a potential target for selective cancer therapy due to its overexpression in certain hypoxic tumors. A series of prodrugs possessing a variety of cytotoxic diterpenoids (oridonin and its analogues) as the leaving groups activated b... Read More about Design, synthesis, and biological evaluation of NAD(P)H: quinone oxidoreductase (NQO1)-targeted oridonin prodrugs possessing indolequinone moiety for hypoxia-selective activation.

Design, synthesis and biological evaluation of novel nitric oxidedonating protoberberine derivatives as antitumor agents (2017)
Journal Article
Chen, J., Wang, T., Xu, S., Lin, A., Yao, H., Xie, W., …Xu, J. (2017). Design, synthesis and biological evaluation of novel nitric oxidedonating protoberberine derivatives as antitumor agents. European Journal of Medicinal Chemistry, 132, https://doi.org/10.1016/j.ejmech.2017.03.027

A novel class of NO-donating protoberberine derivatives were synthesized and initially evaluated for their anti-hepatocellular carcinoma activities. Most of the compounds exhibited more potent activity against HepG2 cells than parent compounds berber... Read More about Design, synthesis and biological evaluation of novel nitric oxidedonating protoberberine derivatives as antitumor agents.

Antioxidant properties of novel dimers derived from natural β‑elemene through inhibiting H2O2‑induced apoptosis (2017)
Journal Article
Chen, J., Wang, R., Wang, T., Ding, Q., Khalil, A., Xu, S., …Xu, J. (in press). Antioxidant properties of novel dimers derived from natural β‑elemene through inhibiting H2O2‑induced apoptosis. ACS Medicinal Chemistry Letters, 8(4), https://doi.org/10.1021/acsmedchemlett.7b00035

A series of novel β-elemene dimer derivatives were synthesized and evaluated for their antioxidant activities. The results indicated that most of the target compounds showed more potent cytoprotective effects than positive control vitamin E. In parti... Read More about Antioxidant properties of novel dimers derived from natural β‑elemene through inhibiting H2O2‑induced apoptosis.

The structural modification of natural products for novel drug discovery (2016)
Journal Article
Yao, H., Liu, J., Xu, S., Zhu, Z., & Xu, J. (in press). The structural modification of natural products for novel drug discovery. Expert Opinion on Drug Discovery, 12(2), https://doi.org/10.1080/17460441.2016.1272757

Introduction: Throughout history, natural products (NPs) have provided a rich source of compounds that have wide applications in the fields of medicine, health sciences, pharmacy and biology. Although naturally active substances are good lead compoun... Read More about The structural modification of natural products for novel drug discovery.