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Synthesis and cytotoxic, anti-inflammatory, and anti-oxidant activities of 2',5'-dialkoxylchalcones as cancer chemopreventive agents.
Bioorg Med Chem. 2008 Aug 01; 16(15):7270-6.BM

Abstract

In an effort to develop novel anti-tumor, or cancer chemopreventive agents, a series of 2',5'-dialkoxylchalcones 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 cell lines. Selective compound 10 induced an accumulation of A549 cells in the G(2)/M phase arrest which was well correlated with inhibitory activity against tubulin polymerization. Cytotoxic compounds 3 and 12 showed significant inhibitory effects on NO production in lipopolysaccharide (LPS)-activated RAW 264.7 macrophage-like cells while cytotoxic compound 10 revealed potent inhibitory effect on TNF-alpha formation in RAW 264.7 cells in response to LPS. Compounds 3 and 10 also showed significant inhibitory effects on xanthine oxidase. The present results suggested that compounds 3 and 10 were potential to be served as cancer chemopreventive agents.

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Authors+Show Affiliations

Cheng JH
School of Pharmacy, Kaohsiung Medical University, Kaohsiung 807, Taiwan.
Hung CF
No affiliation info available
Yang SC
No affiliation info available
Wang JP
No affiliation info available
Won SJ
No affiliation info available
Lin CN
No affiliation info available

MeSH

AnimalsAnti-Inflammatory Agents, Non-SteroidalAntineoplastic AgentsAntioxidantsCell Line, TumorChalconesDose-Response Relationship, DrugDrug Delivery SystemsHumansMacrophagesMast CellsMiceMolecular StructureNeutrophilsStructure-Activity Relationship

Pub Type(s)

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

Language

eng

PubMed ID

18606546

Citation

Cheng, Jen-Hao, et al. "Synthesis and Cytotoxic, Anti-inflammatory, and Anti-oxidant Activities of 2',5'-dialkoxylchalcones as Cancer Chemopreventive Agents." Bioorganic & Medicinal Chemistry, vol. 16, no. 15, 2008, pp. 7270-6.
Cheng JH, Hung CF, Yang SC, et al. Synthesis and cytotoxic, anti-inflammatory, and anti-oxidant activities of 2',5'-dialkoxylchalcones as cancer chemopreventive agents. Bioorg Med Chem. 2008;16(15):7270-6.
Cheng, J. H., Hung, C. F., Yang, S. C., Wang, J. P., Won, S. J., & Lin, C. N. (2008). Synthesis and cytotoxic, anti-inflammatory, and anti-oxidant activities of 2',5'-dialkoxylchalcones as cancer chemopreventive agents. Bioorganic & Medicinal Chemistry, 16(15), 7270-6. https://doi.org/10.1016/j.bmc.2008.06.031
Cheng JH, et al. Synthesis and Cytotoxic, Anti-inflammatory, and Anti-oxidant Activities of 2',5'-dialkoxylchalcones as Cancer Chemopreventive Agents. Bioorg Med Chem. 2008 Aug 1;16(15):7270-6. PubMed PMID: 18606546.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis and cytotoxic, anti-inflammatory, and anti-oxidant activities of 2',5'-dialkoxylchalcones as cancer chemopreventive agents. AU - Cheng,Jen-Hao, AU - Hung,Chi-Feng, AU - Yang,Shyh-Chyun, AU - Wang,Jih-Pyang, AU - Won,Shen-Jeu, AU - Lin,Chun-Nan, Y1 - 2008/06/21/ PY - 2008/03/04/received PY - 2008/06/17/revised PY - 2008/06/18/accepted PY - 2008/7/9/pubmed PY - 2008/11/8/medline PY - 2008/7/9/entrez SP - 7270 EP - 6 JF - Bioorganic & medicinal chemistry JO - Bioorg Med Chem VL - 16 IS - 15 N2 - In an effort to develop novel anti-tumor, or cancer chemopreventive agents, a series of 2',5'-dialkoxylchalcones 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 cell lines. Selective compound 10 induced an accumulation of A549 cells in the G(2)/M phase arrest which was well correlated with inhibitory activity against tubulin polymerization. Cytotoxic compounds 3 and 12 showed significant inhibitory effects on NO production in lipopolysaccharide (LPS)-activated RAW 264.7 macrophage-like cells while cytotoxic compound 10 revealed potent inhibitory effect on TNF-alpha formation in RAW 264.7 cells in response to LPS. Compounds 3 and 10 also showed significant inhibitory effects on xanthine oxidase. The present results suggested that compounds 3 and 10 were potential to be served as cancer chemopreventive agents. SN - 1464-3391 UR - https://www.unboundmedicine.com/medline/citation/18606546/Synthesis_and_cytotoxic_anti_inflammatory_and_anti_oxidant_activities_of_2'5'_dialkoxylchalcones_as_cancer_chemopreventive_agents_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0968-0896(08)00577-4 DB - PRIME DP - Unbound Medicine ER -