All Outputs (8)

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

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

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 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.