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      Anti-cancer chalcones: Structural and molecular target perspectives.

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          Abstract

          Chalcone or (E)-1,3-diphenyl-2-propene-1-one scaffold remained a fascination among researchers in the 21st century due to its simple chemistry, ease of synthesis and a wide variety of promising biological activities. Several natural and (semi) synthetic chalcones have shown anti-cancer activity due to their inhibitory potential against various targets namely ABCG2/P-gp/BCRP, 5α-reductase, aromatase, 17-β-hydroxysteroid dehydrogenase, HDAC/Situin-1, proteasome, VEGF, VEGFR-2 kinase, MMP-2/9, JAK/STAT signaling pathways, CDC25B, tubulin, cathepsin-K, topoisomerase-II, Wnt, NF-κB, B-Raf and mTOR etc. In this review, a comprehensive study on molecular targets/pathways involved in carcinogenesis, mechanism of actions (MOAs), structure activity relationships (SARs) and patents granted have been highlighted. With the knowledge of molecular targets, structural insights and SARs, this review may be helpful for (medicinal) chemists to design more potent, safe, selective and cost effective anti-cancer chalcones.

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          Author and article information

          Journal
          Eur J Med Chem
          European journal of medicinal chemistry
          1768-3254
          0223-5234
          Jun 15 2015
          : 98
          Affiliations
          [1 ] Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur 495009, Chhattisgarh, India.
          [2 ] Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur 495009, Chhattisgarh, India. Electronic address: skbharti.ggu@gmail.com.
          Article
          S0223-5234(15)30035-0
          10.1016/j.ejmech.2015.05.004
          26005917
          e54cecf8-727f-4dd6-b630-e0d20cbefec2
          Copyright © 2015 Elsevier Masson SAS. All rights reserved.
          History

          Angiogenesis,Anti-proliferative,Cancer,Cell lines,Chalcone,Targets

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