178445-82-4Relevant academic research and scientific papers
Synthesis, biological evaluation, and docking studies of gigantol analogs as calmodulin inhibitors
Reyes-Ramírez, Adelfo,Leyte-Lugo, Martha,Figueroa, Mario,Serrano-Alba, Trinidad,González-Andrade, Martín,Mata, Rachel
experimental part, p. 2699 - 2708 (2011/07/08)
Several analogs of gigantol (1) were synthesized to evaluate their effect on the complexes Ca2+-calmodulin (CaM) and Ca2+-CaM-CaM sensitive phosphodiesterase 1 (PDE1). The compounds belong to four structural groups including, 1,2-dip
Synthesis and fungicidal evaluation of novel chalcone-based strobilurin analogues
Zhao, Pei-Liang,Liu, Chang-Ling,Huang, Wei,Wang, Ya-Zhou,Yang, Guang-Fu
, p. 5697 - 5700 (2008/03/14)
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.
Oxy substituted chalcones as antihyperglycemic and antidyslipidemic agents
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Page/Page column 7; 5; 6, (2008/06/13)
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
Synthetic multimerizing agents
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, (2008/06/13)
New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formulaM-L-Qwhere M is a synthetic ligand for an FKBP protein
Synthesis and activity of bivalent FKBP12 ligands for the regulated dimerization of proteins
Keenan, Terence,Yaeger, David R.,Courage, Nancy L.,Rollins, Carl T.,Pavone, Mary Ellen,Rivera, Victor M.,Yang, Wu,Guo, Tao,Amara, Jane F.,Clackson, Tim,Gilman, Michael,Holt, Dennis A.
, p. 1309 - 1335 (2007/10/03)
The total synthesis and in vitro activities of a series of chemical inducers of dimerization (CIDs) is described. The use of small-molecule CIDs to control the dimerization of engineered FKBP12-containing fusion proteins has been demonstrated to have broad utility in biological research as well as potential medical applications in gene and cell therapies. The facility and flexibility of preparation make this new class of wholly synthetic compounds exceptionally versatile tools for the study of intracellular signaling events mediated by protein-protein interactions or protein localization. While some congeners possess potency comparable to or better than the first generation natural product-derived CID, FK1012, structure-activity relationships are complex and underscore the need for application-specific compound optimizations. Copyright (C) 1998 Elsevier Science Ltd.
