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Design, synthesis, and biological evaluation of imidazoline derivatives as p53-MDM2 binding inhibitors.
Bioorg Med Chem. 2011 Sep 15; 19(18):5454-61.BM

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 K(i) value of 0.6 μM, showed its ability to arrest cell cycle progression.

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Publisher Full Text (DOI)

Authors+Show Affiliations

Hu C
ZJU-ENS Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
Li X
No affiliation info available
Wang W
No affiliation info available
Zhang L
No affiliation info available
Tao L
No affiliation info available
Dong X
No affiliation info available
Sheng R
No affiliation info available
Yang B
No affiliation info available
Hu Y
No affiliation info available

MeSH

Antineoplastic AgentsCell Line, TumorCell ProliferationCell SurvivalCrystallography, X-RayDose-Response Relationship, DrugDrug DesignDrug Screening Assays, AntitumorFlow CytometryHumansImidazolinesModels, MolecularMolecular StructureProto-Oncogene Proteins c-mdm2StereoisomerismStructure-Activity RelationshipTumor Suppressor Protein p53

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

21855354

Citation

Hu, Chunqi, et al. "Design, Synthesis, and Biological Evaluation of Imidazoline Derivatives as p53-MDM2 Binding Inhibitors." Bioorganic & Medicinal Chemistry, vol. 19, no. 18, 2011, pp. 5454-61.
Hu C, Li X, Wang W, et al. Design, synthesis, and biological evaluation of imidazoline derivatives as p53-MDM2 binding inhibitors. Bioorg Med Chem. 2011;19(18):5454-61.
Hu, C., Li, X., Wang, W., Zhang, L., Tao, L., Dong, X., Sheng, R., Yang, B., & Hu, Y. (2011). Design, synthesis, and biological evaluation of imidazoline derivatives as p53-MDM2 binding inhibitors. Bioorganic & Medicinal Chemistry, 19(18), 5454-61. https://doi.org/10.1016/j.bmc.2011.07.050
Hu C, et al. Design, Synthesis, and Biological Evaluation of Imidazoline Derivatives as p53-MDM2 Binding Inhibitors. Bioorg Med Chem. 2011 Sep 15;19(18):5454-61. PubMed PMID: 21855354.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Design, synthesis, and biological evaluation of imidazoline derivatives as p53-MDM2 binding inhibitors. AU - Hu,Chunqi, AU - Li,Xin, AU - Wang,Weisi, AU - Zhang,Lei, AU - Tao,Lulu, AU - Dong,Xiaowu, AU - Sheng,Rong, AU - Yang,Bo, AU - Hu,Yongzhou, Y1 - 2011/07/30/ PY - 2011/04/16/received PY - 2011/07/22/revised PY - 2011/07/24/accepted PY - 2011/8/23/entrez PY - 2011/8/23/pubmed PY - 2012/1/11/medline SP - 5454 EP - 61 JF - Bioorganic & medicinal chemistry JO - Bioorg Med Chem VL - 19 IS - 18 N2 - 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 K(i) value of 0.6 μM, showed its ability to arrest cell cycle progression. SN - 1464-3391 UR - https://www.unboundmedicine.com/medline/citation/21855354/Design_synthesis_and_biological_evaluation_of_imidazoline_derivatives_as_p53_MDM2_binding_inhibitors_ DB - PRIME DP - Unbound Medicine ER -