- New class of hybrids based on chalcone and melatonin: a promising therapeutic option for the treatment of colorectal cancer
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Considering that conventional chemotherapy provides only a limited increase of overall survival for patients with colorectal cancer (CRC), and resistance is a major cause of therapeutic failure, the emergence of new therapies is needed. Development of dif
- Arias, Juan D.,Cardona-G, Wilson,Herrera-R, Angie,Moreno, Gustavo,Yepes, Andrés F.
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p. 2240 - 2255
(2021/10/20)
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- An environment-friendly synthesis of piperonal chalcones and their cytotoxic and antioxidant evaluation
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Background: Grindstone technique has been widely used as an efficient, consistent, more environmentally benign, solvent-free protocol for the preparation of many compounds with higher atom economy. Methods: A series of fourteen piperonal chalcone compound
- Baby, Bency,Dev, Sanal,Joy, Monu,Magdy, Hendawy Omnia,Mathew, Bijo,Mathew, Githa Elizabeth,Parambi, Della Grace Thomas,Sudev, Shine
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p. 138 - 144
(2020/02/29)
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- Synthesis and Pharmacological Evaluation of 4-Aryloxyquinazoline Derivatives as Potential Cytotoxic Agents
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In the present study, novel 4-aryloxyquinazoline derivatives were synthesized and screened for in vitro cytotoxicity on human cancer cell lines at 10 μM. Some of the synthesized compounds displayed moderate to significant and selective cytotoxic activity
- Malhotra, Anjleena,Kaur, Tejinder,Bansal, Ranju
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p. 2902 - 2911
(2019/08/26)
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- Synthesis and biological evaluation of chalcone, dihydrochalcone, and 1,3-diarylpropane analogs as anti-inflammatory agents
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Twenty-one chalcones were prepared via aldol condensation and subsequent reduction of these compound led to the corresponding dihydrochalcone and 1,3-diphenylpropane derivatives. The synthetic products were examined for their effects on NO inhibition in L
- Vijaya Bhaskar Reddy, Mopur,Hung, Hsin-Yi,Kuo, Ping-Chung,Huang, Guan-Jhong,Chan, Yu-Yi,Huang, Shiow-Chyn,Wu, Shwu-Jen,Morris-Natschke, Susan L.,Lee, Kuo-Hsiung,Wu, Tian-Shung
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supporting information
p. 1547 - 1550
(2017/03/17)
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- Design, synthesis and antitumor activity of novel artemisinin derivatives using hybrid approach
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In an attempt to develop potent and selective anti-tumor agents, two novel series of artemisinin-chalcone hybrids were designed, synthesized and screened for their antitumor activities against HT-29, A549, MDA-MB-231, HeLa and H460 cell lines in vitro. Nearly all of the tested compounds showed significantly increased anti-tumor activity compared with the corresponding dihydroartemisinin (DHA). Most of the title compounds displayed good selectivity toward HT-29 and HeLa cell lines with IC50 values ranging from 0.09 to 0.85μM. Among them, the most promising compound 9c (IC50 range of 0.09-0.93μM) was 10.5- to 70-times more active than DHA (IC50 range of 5.6-15.6μM) respectively.
- Xie, Lijun,Zhai, Xin,Ren, Lixiang,Meng, Haiyan,Liu, Chun,Zhu, Wufu,Zhao, Yanfang
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experimental part
p. 984 - 990
(2011/10/09)
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- Synthesis and antidyslipidemic activity of chalcone fibrates
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A series of chalcone based PPAR-α agonists were synthesized and evaluated for their antidyslipidemic activity in high fructose high fat fed dyslipidemic Syrian golden hamsters. Most of the compounds exhibited antidyslipidemic activity. The compounds 4c an
- Shukla, Poonam,Srivastava, Swayam P.,Srivastava, Rohit,Rawat, Arun K.,Srivastava, Arvind K.,Pratap, Ram
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experimental part
p. 3475 - 3478
(2011/07/07)
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- Synthesis of a series of novel dihydroartemisinin derivatives containing a substituted chalcone with greater cytotoxic effects in leukemia cells
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Fifteen dihydroartemisinin derivatives containing a substituted chalcone linked by either ether or ester were synthesized and investigated for their cytotoxicity in human leukemia HL-60 and mouse lymphoma P388 cells. These derivatives have greater antiproliferative and cytotoxic effects in both cell lines than dihydroartemisinin. Dihydroartemisinin chalcones linked by ether are more cytotoxic than dihydroartemisinin chalcones linked by ester with apoptosis induction abilities.
- Yang, Xuelin,Wang, Wei,Tan, Jun,Song, Dandan,Li, Ming,Liu, Dan,Jing, Yongkui,Zhao, Linxiang
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experimental part
p. 4385 - 4388
(2010/04/05)
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- Synthesis and fungicidal evaluation of novel chalcone-based strobilurin analogues
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Strobilurin derivatives have become one of the most important classes of agricultural fungicide due to a novel action mode, wide fungicidal spectrum, lower toxicity toward mammalian cells, and environmentally benign characteristics. To discover new strobilurin analogues with high activity against resistant pathogens, a series of new chalcone-based strobilurin derivatives are designed and synthesized by integrating a chalcone scaffold with a strobilurin pharmacophore. The preliminary bioassay showed that some of the chalcone analogues exhibited good in vivo fungicidal activities against Pseudoperoniospora cubensis and Sphaerotheca fuliginea at the dosage of 200 μg mL-1. Two compounds, (£)-methyl 2-[2-({3-[(£)-3-(2- chlorophenyl)acryloyl]phenoxy}methyl)phenyl]-3-meth-oxyacrylate (1e) and (E)-methyl 2-[2-({3-[(E)-3-(3-bromophenyl)acryloyl]phenoxy}methyl)phenyl]-3- methoxyacrylate (11), were found to display higher fungicidal activities against P. cubensis (EC90 = 118.52 μg ml-1 for 1e and EC 90 = 113.64 μg mL-1 for 11) than Kresoxim-methyl (EC90 = 154.92 μg mL-1) and were identified as the most promising candidates for further study. The present work demonstrated that strobilurin analogues containing chalcone as a side chain could be used as a lead structure for further developing novel fungicides. To our knowledge, this is the first report about the syntheses and fungicidal activities of chalcone-based strobilurin derivatives.
- Zhao, Pei-Liang,Liu, Chang-Ling,Huang, Wei,Wang, Ya-Zhou,Yang, Guang-Fu
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p. 5697 - 5700
(2008/03/14)
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- Oxy substituted chalcones as antihyperglycemic and antidyslipidemic agents
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The present invention provides novel substituted chalcone derivatives which exhibit anti-hyperglycemic and anti-dyslipedemic activity. The invention also provides a method for treating type II diabetes and associated hyperlipidemic conditions in a mammal
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Page/Page column 7; 5
(2008/06/13)
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- Synthesis and antihyperglycemic activity of chalcone based aryloxypropanolamines
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A series of aryloxypropanolamines (5a-r) of different chalcones (3a-e) were synthesized and evaluated for antihyperglycemic activity in sucrose loaded (SLM) and streptozotocin (STZ) induced diabetic animal models. Among them compounds 5a, g, m, o, p and r
- Satyanarayana,Tiwari, Priti,Tripathi, Brajendra K.,Srivastava,Pratap, Ram
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p. 883 - 889
(2007/10/03)
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- Structure-activity relationships in a series of orally active γ- hydroxy butenolide endothelin antagonists
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The design of potent and selective non-peptide antagonists of endothelin-1 (ET-1) and its related isopeptides are important tools defining the role of ET in human diseases. In this report we will describe the detailed structure-activity relationship (SAR) studies that led to the discovery of a potent series of butenolide ET(A) selective antagonists. Starting from a micromolar screening hit, PD012527, use of Topliss decision tree analysis led to the discovery of the nanomolar ET(A) selective antagonist PD155080. Further structural modifications around the butenolide ring led directly to the subnanomolar ET(A) selective antagonist PD156707, IC50's = 0.3 (ET(A)) and 780 nM (ET(B)). This series of compounds exhibited functional activity exemplified by PD156707. This derivative inhibited the ET(A) receptor mediated release of arachidonic acid from rabbit renal artery vascular smooth muscle cells with an IC50 = 1.1 nM and also inhibited the ET-1 induced contraction of rabbit femoral artery rings (ET(A) mediated) with a pA2 = 7.6. PD156707 also displayed in vivo functional activity inhibiting the hemodynamic responses due to exogenous administration of ET-1 in rats in a dose dependent fashion. Evidence for the pH dependence of the open and closed tautomerization forms of PD156707 was demonstrated by an NMR study. X- ray crystallographic analysis of the closed butenolide form of PD156707 shows the benzylic group located on the same side of the butenolide ring as the γ- hydroxyl and the remaining two phenyl groups on the butenolide ring essentially orthogonal to the butenolide ring. Pharmacokinetic parameters for PD156707 in dogs are also presented.
- Patt, William C.,Edmunds, Jeremy J.,Repine, Joseph T.,Berryman, Kent A.,Reisdorph, Billy R.,Lee, Chet,Plummer, Mark S.,Shahripour, Aurash,Haleen, Stephen J.,Keiser, Joan A.,Flynn, Mike A.,Welch, Kathleen M.,Reynolds, Elwood E.,Rubin, Ron,Tobias, Brian,Hallak, Hussein,Doherty, Annette M.
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p. 1063 - 1074
(2007/10/03)
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