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Synthetic 2',5'-dimethoxychalcones as G(2)/M arrest-mediated apoptosis-inducing agents and inhibitors of nitric oxide production in rat macrophages.
Eur J Med Chem. 2007 May; 42(5):660-8.EJ

Abstract

In an effort to develop novel antitumor or chemopreventive agents, a series of 2',5'-dimethoxychalcone derivatives were prepared by Claisen-Schmidt condensation of appropriate acetophenones with suitable aromatic aldehyde. In vitro screening revealed low micromolar activity (IC(50)) against several human cancer lines. Activity in MCF-7 cells correlated with the ability to induce G(2)/M arrest-mediated apoptosis following drug treatment by the most potent agent, 8, an observation further reinforced by fluorescence microscopy. Compounds 3, 8, and 10 showed potent inhibitory effect on NO production in lipopolysaccharide (LPS)-activated RAW 264.7 macrophage-like cells. The present results demonstrated that 3, 8, and 10 are potential anti-inflammatory and cancer chemopreventive agents.

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Authors+Show Affiliations

Wei BL
Institute of Life Science, National Taitung University, Taitung, Taiwan.
Teng CH
No affiliation info available
Wang JP
No affiliation info available
Won SJ
No affiliation info available
Lin CN
No affiliation info available

MeSH

AnimalsApoptosisCell DivisionCell Line, TumorChalconesG2 PhaseHumansMacrophagesMagnetic Resonance SpectroscopyMicroscopy, FluorescenceNitric OxideRatsSpectrometry, Mass, Electrospray IonizationSpectrophotometry, Infrared

Pub Type(s)

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

Language

eng

PubMed ID

17320246

Citation

Wei, Bai-Luh, et al. "Synthetic 2',5'-dimethoxychalcones as G(2)/M Arrest-mediated Apoptosis-inducing Agents and Inhibitors of Nitric Oxide Production in Rat Macrophages." European Journal of Medicinal Chemistry, vol. 42, no. 5, 2007, pp. 660-8.
Wei BL, Teng CH, Wang JP, et al. Synthetic 2',5'-dimethoxychalcones as G(2)/M arrest-mediated apoptosis-inducing agents and inhibitors of nitric oxide production in rat macrophages. Eur J Med Chem. 2007;42(5):660-8.
Wei, B. L., Teng, C. H., Wang, J. P., Won, S. J., & Lin, C. N. (2007). Synthetic 2',5'-dimethoxychalcones as G(2)/M arrest-mediated apoptosis-inducing agents and inhibitors of nitric oxide production in rat macrophages. European Journal of Medicinal Chemistry, 42(5), 660-8.
Wei BL, et al. Synthetic 2',5'-dimethoxychalcones as G(2)/M Arrest-mediated Apoptosis-inducing Agents and Inhibitors of Nitric Oxide Production in Rat Macrophages. Eur J Med Chem. 2007;42(5):660-8. PubMed PMID: 17320246.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthetic 2',5'-dimethoxychalcones as G(2)/M arrest-mediated apoptosis-inducing agents and inhibitors of nitric oxide production in rat macrophages. AU - Wei,Bai-Luh, AU - Teng,Chi-Huang, AU - Wang,Jih-Pyang, AU - Won,Shen-Jeu, AU - Lin,Chun-Nan, Y1 - 2007/01/09/ PY - 2006/08/16/received PY - 2006/11/28/revised PY - 2006/12/05/accepted PY - 2007/2/27/pubmed PY - 2007/7/11/medline PY - 2007/2/27/entrez SP - 660 EP - 8 JF - European journal of medicinal chemistry JO - Eur J Med Chem VL - 42 IS - 5 N2 - In an effort to develop novel antitumor or chemopreventive agents, a series of 2',5'-dimethoxychalcone derivatives were prepared by Claisen-Schmidt condensation of appropriate acetophenones with suitable aromatic aldehyde. In vitro screening revealed low micromolar activity (IC(50)) against several human cancer lines. Activity in MCF-7 cells correlated with the ability to induce G(2)/M arrest-mediated apoptosis following drug treatment by the most potent agent, 8, an observation further reinforced by fluorescence microscopy. Compounds 3, 8, and 10 showed potent inhibitory effect on NO production in lipopolysaccharide (LPS)-activated RAW 264.7 macrophage-like cells. The present results demonstrated that 3, 8, and 10 are potential anti-inflammatory and cancer chemopreventive agents. SN - 0223-5234 UR - https://www.unboundmedicine.com/medline/citation/17320246/Synthetic_2'5'_dimethoxychalcones_as_G_2_/M_arrest_mediated_apoptosis_inducing_agents_and_inhibitors_of_nitric_oxide_production_in_rat_macrophages_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0223-5234(07)00008-6 DB - PRIME DP - Unbound Medicine ER -