Hai Liang Zhu
Affiliation: Nanjing University
- Ren S, Wang Z, Zhu D, Zhu X, Shen F, Wu S, et al. Design, synthesis and biological evaluation of novel ferrocene-pyrazole derivatives containing nitric oxide donors as COX-2 inhibitors for cancer therapy. Eur J Med Chem. 2018;157:909-924 pubmed publisher..Most notably, 7l could dramatically suppress tumor growth in Hela cells xenografted mouse model. In summary, compound 7l may be promising candidates for cancer therapy. ..
- Yang B, Xu J, Yuan Z, Zheng D, He Z, Jiao Q, et al. A new selective fluorescence probe with a quinoxalinone structure (QP-1) for cysteine and its application in live-cell imaging. Talanta. 2018;189:629-635 pubmed publisher..Moreover, QP-1 has been successfully applied in the imaging of Cys in living cells. Finally, QP-1 has been used to detect Cys in rat urine samples. ..
- Qin Y, Wang P, Makawana J, Wang Z, Wang Z, Yan Gu -, et al. Design, synthesis and biological evaluation of metronidazole-thiazole derivatives as antibacterial inhibitors. Bioorg Med Chem Lett. 2014;: pubmed publisher..Toxicity assay of compounds 5a, 5b, 5d, 5e, 5g and 5i showed that they were noncytotoxic against human macrophage. The results revealed that these compounds offered remarkable viability. ..
- Zhao M, Yin Y, Yu X, Sangani C, Wang S, Lu A, et al. Synthesis, biological evaluation and 3D-QSAR study of novel 4,5-dihydro-1H-pyrazole thiazole derivatives as BRAF(Vâ¶â°â°E) inhibitors. Bioorg Med Chem. 2015;23:46-54 pubmed publisher..4 cells in a dose dependent manner. Furthermore, docking simulation of inhibitor analogues and 3D-QSAR modeling provided potential binding model and further knowledge of pharmacophore. ..
- Lv P, Zhu H. Nitroimidazole derivatives: a patent review of US 2014/0141084 A1. Expert Opin Ther Pat. 2015;25:489-92 pubmed publisher..In this patent (US 2014/0141084 A1), amphiphilic polymers were designed and prepared based on nitroimidazole derivatives and carboxymethyl dextran, which can be used for the hypoxia-selective release of diagnostics or drugs. ..
- Wang S, Zhu Y, Zhu P, Makawana J, Zhang Y, Zhao M, et al. Design, synthesis and biological evaluation of novel 5-phenyl-1H-pyrazole derivatives as potential BRAF(V600E) inhibitors. Bioorg Med Chem. 2014;22:6201-8 pubmed publisher..Furthermore, molecular docking and 3D QSAR study by means of DS 3.5 (Discovery Studio 3.5, Accelrys, Co. Ltd) explored the binding modes and the structure and activity relationship (SAR) of these derivatives. ..
- Wang S, Yin Y, Zhang Y, Mi S, Zhao M, Lv P, et al. Synthesis, biological evaluation and 3D-QSAR studies of novel 5-phenyl-1H-pyrazol cinnamamide derivatives as novel antitubulin agents. Eur J Med Chem. 2015;93:291-9 pubmed publisher..3D-QSAR model was also built to provide more pharmacophore understanding that could be used to design new agents with more potent tubulin inhibitory activity. ..
- Qin Y, Li Y, Jiang A, Yang M, Zhu Q, Dong H, et al. Design, synthesis and biological evaluation of novel pyrazoline-containing derivatives as potential tubulin assembling inhibitors. Eur J Med Chem. 2015;94:447-57 pubmed publisher..These studies, along with molecular docking, provided a new molecular scaffold for the further development of antitumor agents that target tubulin. ..
- Liu Q, Shi W, Ren S, Ni W, Li W, Chen H, et al. Arylamino containing hydroxamic acids as potent urease inhibitors for the treatment of Helicobacter pylori infection. Eur J Med Chem. 2018;156:126-136 pubmed publisher..pylori caused gastritis and gastric ulcer, and hence merit further studies. ..
- Ni W, Liu Q, Ren S, Li W, Yi L, Jing H, et al. The synthesis and evaluation of phenoxyacylhydroxamic acids as potential agents for Helicobacter pylori infections. Bioorg Med Chem. 2018;26:4145-4152 pubmed publisher..Non-linear fitting of experimental data (V-[S]) suggested a mixed-type inhibition mechanism and a dual site binding mode of these compounds. ..
- Wang P, Zhang Y, Wang D, Hu H, Wang Z, Xu C, et al. Design, synthesis, and biological evaluation of new B-RafV600E kinase inhibitors. Bioorg Med Chem. 2018;26:2372-2380 pubmed publisher..In addition, in vitro assays were carried out to profile the pharmacological properties of all the entities. Of all the compounds, compound 5h showed the best profile and may be used in the future study. ..
- Duan Y, Wang Z, Sang Y, Tao X, Zhu H. Exploration of structure-based on imidazole core as antibacterial agents. Curr Top Med Chem. 2013;13:3118-30 pubmed..We hope that increasing knowledge of the structure-activity relationship (SAR) will be beneficial to the rational design of new generation of small molecule antibacterial drugs. ..
- Chen K, Zhang Y, Fan J, Ma X, Qin Y, Zhu H. Novel nicotinoyl pyrazoline derivates bearing N-methyl indole moiety as antitumor agents: Design, synthesis and evaluation. Eur J Med Chem. 2018;156:722-737 pubmed publisher..52% without noticeable weight loss and tissue damage (examined by H&E staining), which was comparable to CA-4 (inhibited 59.92%). In brief, compound 28 is a promising candidate for tumor therapy as tubulin assembly inhibitor. ..
- Li H, Su M, Xu Y, Xu C, Yang Y, Zhu H. Design and biological evaluation of novel triaryl pyrazoline derivatives with dioxane moiety for selective BRAFV600E inhibition. Eur J Med Chem. 2018;155:725-735 pubmed publisher..These results brought potent BRAF inhibitors one step further to selective agents, enhancing the potential for safe medication. ..
- Liu Q, Ni W, Li Z, Bai C, Tan D, Pu C, et al. Resolution and evaluation of 3-chlorophenyl-3-hydroxypropionylhydroxamic acid as antivirulence agent with excellent eradication efficacy in Helicobacter pylori infected mice. Eur J Pharm Sci. 2018;121:293-300 pubmed publisher..These studies revealed that CPH is a promising candidate for an alternative treatment of HP-dependent conditions by targeting virulence factor urease, and CPH may be used as a raceme. ..
- Fan A, Wei J, Yang M, Zhang Q, Zhang Y, Liu Q, et al. Pharmacodynamic and pharmacokinetic characteristics of YMR-65, a tubulin inhibitor, in tumor-bearing mice. Eur J Pharm Sci. 2018;121:74-84 pubmed publisher..In brief, our results indicated that YMR-65 was a promising candidate with high antitumor efficacy and low tissue damage. ..
- Yan X, Wang Z, Li Z, Wang P, Qiu H, Chen L, et al. Sulfonamide derivatives containing dihydropyrazole moieties selectively and potently inhibit MMP-2/MMP-9: Design, synthesis, inhibitory activity and 3D-QSAR analysis. Bioorg Med Chem Lett. 2015;25:4664-71 pubmed publisher..Docking simulation was further performed to position compound 3i into the MMP-2 active site to determine the probable binding model the 3D-QSAR models were built for reasonable design of MMP-2/MMP-9 inhibitors at present and in future. ..
- Guo Z, Yin Y, Wang C, Wang P, Zhang X, Wang Z, et al. Design, synthesis and molecular docking of salicylic acid derivatives containing metronidazole as a new class of antimicrobial agents. Bioorg Med Chem. 2015;23:6148-56 pubmed publisher..aureus Tyrosyl-tRNA synthetase active site to determine the probable binding model. These results suggested that compound 5r may be a promising antibacterial agent. ..
- Xiao Z, Shi W, Wang P, Wei W, Zeng X, Zhang J, et al. Synthesis and evaluation of N-analogs of 1,2-diarylethane as Helicobacter pylori urease inhibitors. Bioorg Med Chem. 2015;23:4508-13 pubmed publisher..The SAR analysis revealed that protection of 3,4-dihydroxy group of 4 as methoxy or changes of 4-NO2 will result in a moderate to dramatic decrease in potency. ..
- Wang Y, Qin Y, Yang N, Zhang Y, Liu C, Zhu H. Synthesis, biological evaluation, and molecular docking studies of novel 1-benzene acyl-2-(1-methylindol-3-yl)-benzimidazole derivatives as potential tubulin polymerization inhibitors. Eur J Med Chem. 2015;99:125-37 pubmed publisher..Docking simulation and 3D-QSAR model in these studies provided more information that could be applied to design new molecules with more potent tubulin inhibitory activity. ..
- Yin Y, Zhang Y, Jin B, Sha S, Wu X, Sangani C, et al. 6,7-Dihydrobenzo[f]benzo[4,5]imidazo[1,2-d][1,4]oxazepine derivatives as selective inhibitors of PI3KÎ±. Bioorg Med Chem. 2015;23:1231-40 pubmed publisher..It indicated the potential of developing 6,7-dihydrobenzo[f]benzo[4,5]imidazo[1,2-d][1,4]oxazepine derivatives as the new PI3KÎ± selective inhibitors for tumor treatment. ..
- Lv P, Sun J, Zhu H. Recent advances of p53-MDM2 small molecule inhibitors (2011-present). Curr Med Chem. 2015;22:618-26 pubmed
- Sangani C, Makawana J, Duan Y, Yin Y, Teraiya S, Thumar N, et al. Design, synthesis and molecular modeling of biquinoline-pyridine hybrids as a new class of potential EGFR and HER-2 kinase inhibitors. Bioorg Med Chem Lett. 2014;24:4472-4476 pubmed publisher..In the molecular modelling study, compound 9i was bound in to the active pocket of EGFR with four hydrogen bonds and two Ï€-cation interactions having minimum binding energy Î”Gb=-54.4 kcal/mol. ..
- Wei W, Shi W, Wang P, Zeng X, Li P, Zhang J, et al. Adenosine analogs as inhibitors of tyrosyl-tRNA synthetase: Design, synthesis and antibacterial evaluation. Bioorg Med Chem. 2015;23:6602-11 pubmed publisher..In comparison with isopropylidene analogs, 2',3'-deprotected compounds displayed higher inhibitory activity. Molecular dockings provided an explanation for observations in biological assays. ..
- Li X, Li J, Chen K, Zhu H. A functional scaffold in marine alkaloid: an anticancer moiety for human. Curr Med Chem. 2013;20:3903-22 pubmed..Meanwhile, an hypothesis was made correlatively to explain the different mechanisms of their anticancer activities in human cell lines. ..
- Ren S, Wang Z, Zhu X, Zhu D, Li Z, Shen F, et al. Design and biological evaluation of novel hybrids of 1, 5-diarylpyrazole and Chrysin for selective COX-2 inhibition. Bioorg Med Chem. 2018;26:4264-4275 pubmed publisher..Besides, molecular docking simulation results was further confirmed that e9 could bind well with COX-2. In summary, compound e9 may be promising candidates for cancer therapy. ..
- Wang X, Wei W, Wang P, Yi L, Shi W, Xie Y, et al. Synthesis, molecular docking and biological evaluation of 3-arylfuran-2(5H)-ones as anti-gastric ulcer agent. Bioorg Med Chem. 2015;23:4860-5 pubmed publisher..2 Î¼M) and good anti-H. pylori activity (MIC50=2.6 Î¼g/mL), and it can be used as a good candidate for discovering novel anti-gastric ulcer agent. ..
- Lv P, Zhu H. EGFR-binding peptide: a patent evaluation of WO2014002836. Expert Opin Ther Pat. 2014;24:1409-11 pubmed publisher..Some of them not only could be used as potential therapeutic agents for the treatment of EGFR-overexpressed cancers, but also show promising application in detecting cancer tissue or cancer cells that express the EGFR. ..
- Wang S, Yin Y, Wu X, Qiao F, Sha S, Lv P, et al. Synthesis, molecular docking and biological evaluation of coumarin derivatives containing piperazine skeleton as potential antibacterial agents. Bioorg Med Chem. 2014;22:5727-37 pubmed publisher..57 Î¼M. Molecular docking of 4 g into S. aureus Enoyl-ACP-reductase active site were performed to determine the probable binding mode, while the QSAR model was built to check the previous work as well as to introduce new directions. ..
- Wang C, Wang Z, Shi L, Wang Z, Zhu H. Design, synthesis, and biological evaluation of pyrazole derivatives containing acetamide bond as potential BRAFV600E inhibitors. Bioorg Med Chem Lett. 2018;28:2382-2390 pubmed publisher..Meanwhile, 3D-QSAR model suggested that these compounds may be potential anticancer inhibitors. Overall, the article provided some new molecular scaffolds for the further BRAFV600E inhibitors. ..
- Xu Y, Zhang M, Li B, Wang W, Wang B, Yang Y, et al. A fluorescence probe acted on Site I binding for Human Serum Albumin. Talanta. 2018;185:568-572 pubmed publisher..Furthermore, the fluorescence probe acted on Site I and discrimination of HSA from BSA. ..
- Makawana J, Sangani C, YAO Y, Duan Y, Lv P, Zhu H. Recent Developments of Metal and Metal Oxide Nanocatalysts in Organic Synthesis. Mini Rev Med Chem. 2016;16:1303-1320 pubmed..In the latter part, different Metal Oxide Nanoparticles, such as ZnO Nanoparticle, TiO2 Nanoparticle, and CuO Nanoparticle are discussed. ..
- Tao X, Duan Y, Chen L, Tang D, Yang M, Wang P, et al. Design, synthesis and biological evaluation of pyrazolyl-nitroimidazole derivatives as potential EGFR/HER-2 kinase inhibitors. Bioorg Med Chem Lett. 2016;26:677-683 pubmed publisher..28Î¼M for EGFR). Molecular modeling simulation studies were performed in order to predict the biological activity of the proposed compounds and activity relationship (SAR) of these pyrazole-nitroimidazole derivatives. ..
- Zhang Y, Qin Y, Tang D, Yang M, Li B, Wang Y, et al. Synthesis and Biological Evaluation of 1-Methyl-1H-indole-Pyrazoline Hybrids as Potential Tubulin Polymerization Inhibitors. ChemMedChem. 2016;11:1446-58 pubmed publisher..These studies, along with molecular docking and 3D-QSAR modeling, provide an important basis for further optimization of compound e19 as a potential anticancer agent. ..
- Chen L, Wang P, Tang D, Tao X, Man R, Qiu H, et al. Metronidazole containing pyrazole derivatives potently inhibit tyrosyl-tRNA synthetase: design, synthesis, and biological evaluation. Chem Biol Drug Des. 2016;88:592-8 pubmed publisher..98 ?g/mL) and exhibited TryRS inhibitory activity (IC50 = 0.92 ?m). Docking simulation was performed to further understand its potency. Membrane-mediated apoptosis in P. aeruginosa was verified by flow cytometry. ..
- Wang H, Yan X, Yan T, Li H, Wang Z, Zhu H. Design, Synthesis and Biological Evaluation of Benzohydrazide Derivatives Containing Dihydropyrazoles as Potential EGFR Kinase Inhibitors. Molecules. 2016;21: pubmed publisher..These results suggested that compound H20 may be a promising anticancer agent. ..
- Chen L, Wang Z, Zhu B, Man R, Liu Y, Zhang Y, et al. Design, synthesis and biological evaluation of novel benzo-?-pyrone containing piperazine derivatives as potential BRAFV600E inhibitors. Bioorg Med Chem Lett. 2016;26:4983-4991 pubmed publisher..Overall, the biological profile of 3l suggests that this compound may be developed as a potential anticancer agent. ..
- Lu X, Wang Z, Ren S, Shen F, Man R, Zhu H. Coumarin sulfonamides derivatives as potent and selective COX-2 inhibitors with efficacy in suppressing cancer proliferation and metastasis. Bioorg Med Chem Lett. 2016;26:3491-8 pubmed publisher..Docking simulations results was further indicated that compound 7t could bind well to the COX-2 active site and guided a reasonable design of selective COX-2 inhibitor with anticancer activities in future. ..
- Qiu H, Wang P, Li Z, Ma J, Wang X, Yang Y, et al. Synthesis of dihydropyrazole sulphonamide derivatives that act as anti-cancer agents through COX-2 inhibition. Pharmacol Res. 2016;104:86-96 pubmed publisher..The morphological variation of treated cells was also visualized by confocal microscopy. Overall, the biological profile of 4d suggests that this compound may be developed as a potential anticancer agent. ..
- Lin L, Zeng X, Shen Y, Zhu H, Qian Y. An ultrasensitive fluorescent probe for rapid determination of thiophenols. Talanta. 2017;165:321-325 pubmed publisher..Using this ultrasensitive probe (LOD, 1.05Ã—10-8M), we have successfully monitored and quantified highly toxic thiophenols in aqueous media and real-water samples. ..
- Wang P, Qiu H, Wang Z, Zhang Y, Wang Z, Li D, et al. Identification of novel B-RafV600E inhibitors employing FBDD strategy. Biochem Pharmacol. 2017;132:63-76 pubmed publisher..The results favored our rational design intention and hinted this new kind of inhibitors might be helpful in the further explorations of potent agents. ..
- Qiu H, Fu J, Yang M, HAN H, Wang P, Zhang Y, et al. Identification of new shikonin derivatives as STAT3 inhibitors. Biochem Pharmacol. 2017;146:74-86 pubmed publisher..The in vitro and in vivo results collectively suggest that PMMB-187 may serve as a promising lead compound for the further development of potential therapeutic anti-neoplastic agents. ..
- Sun J, Ren S, Lu X, Li J, Shen F, Xu C, et al. Discovery of a series of 1,3,4-oxadiazole-2(3H)-thione derivatives containing piperazine skeleton as potential FAK inhibitors. Bioorg Med Chem. 2017;25:2593-2600 pubmed publisher..15?M for SW1116), and its anti-FAK inhibitory activity (IC50=0.78?M) was also the best. Computational docking studies also showed that compound 5m has interaction with FAK key residues in the active site. ..
- Shi W, Deng R, Wang P, Yue Q, Liu Q, Ding K, et al. 3-Arylpropionylhydroxamic acid derivatives as Helicobacter pylori urease inhibitors: Synthesis, molecular docking and biological evaluation. Bioorg Med Chem. 2016;24:4519-4527 pubmed publisher..Non-linear fitting of kinetic data gives kinetics parameters of 0.13 and 0.12?g·mL(-1) for Ki and Ki', respectively. The plasma protein binding assays suggested that d24 exhibited moderate binding to human and rabbit plasma proteins. ..
- Wei W, Liu Q, Li Z, Shi W, Fu X, Liu J, et al. Synthesis and evaluation of adenosine containing 3-arylfuran-2(5H)-ones as tyrosyl-tRNA synthetase inhibitors. Eur J Med Chem. 2017;133:62-68 pubmed publisher..61 ± 0.04 ?M. Bacterial growth inhibition assays demonstrated that d3 showed submicromolar antibacterial potency against Escherichia coli and Pseudomonas aeruginosa, and compared to the marketed antibiotics ciprofloxacin. ..
- Yang Y, Yang B, Zou Y, Li G, Zhu H. Design, biological evaluation and 3D QSAR studies of novel dioxin-containing triaryl pyrazoline derivatives as potential B-Raf inhibitors. Bioorg Med Chem. 2016;24:3052-3061 pubmed publisher..Stretching the backbone to outer space or totally reversing the backbone are both potential orientations for future researches. ..
- YAO Y, Wang Z, Wu S, Li Q, Yu C, Liang X, et al. Identification of novel 1-indolyl acetate-5-nitroimidazole derivatives of combretastatin A-4 as potential tubulin polymerization inhibitors. Biochem Pharmacol. 2017;137:10-28 pubmed publisher..Collectively, these in vitro and in vivo results indicated that compound 3 might be a promising lead compound for further development as a potential anti-cancer drug. ..
- Shen F, Wang Z, Wu S, Ren S, Man R, Wang B, et al. Synthesis of novel hybrids of pyrazole and coumarin as dual inhibitors of COX-2 and 5-LOX. Bioorg Med Chem Lett. 2017;27:3653-3660 pubmed publisher..Our study might contribute to COX-2, 5-LOX dual inhibitors thus exploit promising novel cancer prevention agents. ..