title: Anti-cancer chalcones: Structural and molecular target perspectives.
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.
authors.affiliation: Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur 495009, Chhattisgarh, India.
authors.forename: Debarshi Kar
authors.initials: DK
authors.lastname: Mahapatra
authors.affiliation: Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur 495009, Chhattisgarh, India. Electronic address: skbharti.ggu@gmail.com.
authors.forename: Sanjay Kumar
authors.initials: SK
authors.lastname: Bharti
authors.affiliation: Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur 495009, Chhattisgarh, India.
authors.forename: Vivek
authors.initials: V
authors.lastname: Asati
mesh_terms: D000107:Acetylation; D020533:Angiogenesis Inhibitors / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D047188:Chalcones / Q000737:chemistry* / Q000494:pharmacology*; D012739:Gonadal Steroid Hormones / Q000037:antagonists & inhibitors; D006801:Humans; D027425:ATP-Binding Cassette, Sub-Family C Proteins / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D016159:Tumor Suppressor Protein p53 / Q000037:antagonists & inhibitors / Q000378:metabolism
chemical_list: D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents; D047188:Chalcones; D012739:Gonadal Steroid Hormones; D027425:ATP-Binding Cassette, Sub-Family C Proteins; D016159:Tumor Suppressor Protein p53
keywords: Angiogenesis; Anti-proliferative; Cancer; Cell lines; Chalcone; Targets