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Your search keyword '"Chunqi Hu"' showing total 3 results
Start Over Author "Chunqi Hu" Journal bioorganicmedicinal chemistry
3 results on '"Chunqi Hu"'

1. Design, synthesis and biological evaluation of novel 3,4,5-trisubstituted aminothiophenes as inhibitors of p53-MDM2 interaction. Part 1

Author

Weisi Wang, Lei Zhang, Yongzhou Hu, Chunqi Hu, Ni Qiu, and Shihao Shangguan

Subjects
Clinical Biochemistry, Pharmaceutical Science, Antineoplastic Agents, Thiophenes, Biochemistry, Sensitivity and Specificity, P53 mdm2, chemistry.chemical_compound, Inhibitory Concentration 50, Structure-Activity Relationship, Cell Line, Tumor, Drug Discovery, P53 status, Structure–activity relationship, Humans, Molecular Biology, Biological evaluation, Cell Proliferation, Organic Chemistry, Proto-Oncogene Proteins c-mdm2, Combinatorial chemistry, Molecular Docking Simulation, Kinetics, chemistry, Design synthesis, Cell culture, Drug Design, Molecular Medicine, Drug Screening Assays, Antitumor, Tumor Suppressor Protein p53, Selectivity, Lead compound, Protein Binding
Abstract

A series of 3,4,5-trisubstituted aminothiophenes were designed, synthesized, and evaluated for their p53-MDM2 binding inhibitory potency and anti-proliferation activities against A549 and PC3 tumor cell lines. Fourteen compounds had appreciably improved MDM2 binding affinities than lead compound MCL0527 (3) and a few compounds showed comparable activities to that of Nutlin-3. Meanwhile, most of the 3,4,5-trisubstituted aminothiophenes displayed better or equivalent anti-proliferation activities against wild-type p53 cell line A549 compared to that of Nutlin-3. Over ten compounds exhibited desirable selective profiles of p53 status. Particularly, compounds 9, 16 and 18 displayed 22-, 6- and 22-fold selectivity of p53 status, respectively, much better than that of Nutlin-3 (fourfold).

Published
2013

2. Design, synthesis and biological evaluation of novel 3,4,5-trisubstituted aminothiophenes as inhibitors of p53-MDM2 interaction. Part 2

Author

Weisi Wang, Ni Qiu, Chunqi Hu, Lei Zhang, Yongzhou Hu, and Dan Lv

Subjects
Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Tumor cells, Antineoplastic Agents, Thiophenes, Biochemistry, Sensitivity and Specificity, P53 mdm2, Inhibitory Concentration 50, Structure-Activity Relationship, Cell Line, Tumor, Drug Discovery, Ic50 values, Humans, Molecular Biology, P53 expression, Biological evaluation, Cell Proliferation, Chemistry, Organic Chemistry, Molecular Docking Analysis, Proto-Oncogene Proteins c-mdm2, Combinatorial chemistry, Molecular Docking Simulation, Kinetics, Design synthesis, Cell culture, Drug Design, Molecular Medicine, Drug Screening Assays, Antitumor, Tumor Suppressor Protein p53, Protein Binding
Abstract

Five series of novel 3,4,5-trisubstituted aminothiophene derivatives and analogs were designed and synthesized based on our previous studies. All target compounds were evaluated for their p53–MDM2 binding inhibitory activities and anti-proliferation activities against A549 and PC3 tumor cell lines. Twelve compounds displayed comparable p53–MDM2 binding inhibitory activities to that of Nutlin-3. Among them, compound 7a exhibited marked binding affinity (IC50 = 0.086 μM). In addition, most target compounds showed potent anti-proliferation activities with IC50 values at low micromolar level. A good selective profile for wild-type p53 expression cell line was also observed. Molecular docking analysis was performed as well to predict possible binding modes of target compounds with MDM2.

Published
2013

3. Design, synthesis, and biological evaluation of imidazoline derivatives as p53-MDM2 binding inhibitors

Author

Chunqi Hu, Xin Li, Lulu Tao, Yongzhou Hu, Weisi Wang, Xiaowu Dong, Bo Yang, Lei Zhang, and Rong Sheng

Subjects
Models, Molecular, Cell Survival, Clinical Biochemistry, Pharmaceutical Science, Imidazoline receptor, Antineoplastic Agents, Imidazoline derivatives, Pharmacology, Inhibitory postsynaptic potential, Crystallography, X-Ray, Biochemistry, P53 mdm2, chemistry.chemical_compound, Structure-Activity Relationship, Cell Line, Tumor, Drug Discovery, Humans, Imidazolines, neoplasms, Molecular Biology, Biological evaluation, Cell Proliferation, Dose-Response Relationship, Drug, Molecular Structure, Chemistry, Organic Chemistry, Proto-Oncogene Proteins c-mdm2, Stereoisomerism, Nutlin, Flow Cytometry, Inhibitory potency, Design synthesis, Drug Design, Molecular Medicine, Drug Screening Assays, Antitumor, Tumor Suppressor Protein p53
Abstract

Three series of novel imidazoline derivatives were designed, synthesized, and evaluated for their p53–MDM2 binding inhibitory activities, and anti-proliferation activities against PC3, A549, KB, and HCT116 cancer cell lines. Five of the tested compounds showed enhanced p53–MDM2 binding inhibitory potency and anti-proliferation activities in comparison with that of Nutlin-1. Flow cytometric analysis indicated that compound 7c, one of the most potent p53–MDM2 binding inhibitors with a Ki value of 0.6 μM, showed its ability to arrest cell cycle progression.

Published
2011

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