All Outputs (9)

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

Discovery of novel antitumor nitric oxide-donating ?-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 ?-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 ??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 ?-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 ??elemene through inhibiting H2O2?induced apoptosis.