PMID- 28914193 OWN - NLM STAT- MEDLINE DCOM- 20171213 LR - 20180605 IS - 1873-4294 (Electronic) IS - 1568-0266 (Linking) VI - 17 IP - 28 DP - 2017 Nov 20 TI - Chalcone Derivatives: Anti-inflammatory Potential and Molecular Targets Perspectives. PG - 3146-3169 LID - 10.2174/1568026617666170914160446 [doi] AB - Chalcone or (E)-1,3-diphenyl-2-propene-1-one scaffold has gained considerable scientific interest in medicinal chemistry owing to its simple chemistry, ease in synthesizing a variety of derivatives and exhibiting a broad range of promising pharmacological activities by modulating several molecular targets. A number of natural and (semi-) synthetic chalcone derivatives have demonstrated admirable anti-inflammatory activity due to their inhibitory potential against various therapeutic targets like Cyclooxygenase (COX), Lipooxygenase (LOX), Interleukins (IL), Prostaglandins (PGs), Nitric Oxide Synthase (NOS), Leukotriene D4 (LTD4), Nuclear Factor-kappaB (NF- kappaB), Intracellular Cell Adhesion Molecule-1 (ICAM-1), Vascular Cell Adhesion Molecule-1 (VCAM-1), Monocyte Chemoattractant Protein-1 (MCP-1) and TLR4/MD-2, etc. The chalcone scaffold with hydroxyl, methoxyl, carboxyl, prenyl group and/or heterocyclic ring substitution like thiophene/furan/indole showed promising anti-inflammatory activity. In this review, a comprehensive study (from the year 1991 to 2016) on multi-targets of inflammatory interest, related inflammation reactions and their treatment by chalcone-based inhibitors acting on various molecular targets entailed in inflammation, Structure-Activity Relationships (SARs), Mechanism of Actions (MOAs), and patents are highlighted. CI - Copyright(c) Bentham Science Publishers; For any queries, please email at epub@benthamscience.org. FAU - Mahapatra, Debarshi Kar AU - Mahapatra DK AD - Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur - 495009, Chhattisgarh, India. FAU - Bharti, Sanjay Kumar AU - Bharti SK AD - Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur - 495009, Chhattisgarh, India. FAU - Asati, Vivek AU - Asati V AD - Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur - 495009, Chhattisgarh, India. LA - eng PT - Journal Article PT - Review PL - United Arab Emirates TA - Curr Top Med Chem JT - Current topics in medicinal chemistry JID - 101119673 RN - 0 (Anti-Inflammatory Agents, Non-Steroidal) RN - 5S5A2Q39HX (Chalcone) SB - IM MH - Animals MH - Anti-Inflammatory Agents, Non-Steroidal/chemical synthesis/chemistry/*pharmacology MH - Chalcone/chemical synthesis/chemistry/*pharmacology MH - Humans MH - Molecular Structure OTO - NOTNLM OT - Chalcone OT - inflammatory OT - inhibitor OT - patent OT - pathway OT - target. EDAT- 2017/09/16 06:00 MHDA- 2017/12/14 06:00 CRDT- 2017/09/16 06:00 PHST- 2016/11/01 00:00 [received] PHST- 2017/04/21 00:00 [revised] PHST- 2017/04/25 00:00 [accepted] PHST- 2017/09/16 06:00 [pubmed] PHST- 2017/12/14 06:00 [medline] PHST- 2017/09/16 06:00 [entrez] AID - CTMC-EPUB-85784 [pii] AID - 10.2174/1568026617666170914160446 [doi] PST - ppublish SO - Curr Top Med Chem. 2017 Nov 20;17(28):3146-3169. doi: 10.2174/1568026617666170914160446.