949090-28-2Relevant academic research and scientific papers
Scalable Total Synthesis of (+)- And (-)-Codonopiloneolignanin A via Ti(IV)/NHC Cooperative Control Highly Enantioselective Dimerization of Multisubstituted Cinnamaldehyde
Li, Xiangxin,Yong, Huaya,Fan, Xiaohong,Zheng, Yajuan,Wang, Zhen,Xie, Zhixiang
supporting information, p. 6573 - 6577 (2021/08/18)
The first gram-scale asymmetric total synthesis of (+)- and (-)-codonopiloneolignanin A has been achieved from multisubstituted cinnamaldehyde in four steps with 37% overall yield. The synthetically challenging tricyclic [5, 3, 0, 03,8] decane skeleton was efficiently constructed via a highly enantioselective dimerization of multisubstituted cinnamaldehyde, followed by a sequence of cascade reactions including Prins cyclization, cation mediated cyclization, and deprotection. Furthermore, the scope of NHC-catalyzed/Ti(IV)-mediated synergistic control multisubstituted cinnamaldehyde dimerization was investigated. Significantly, the bioactivity of codonopiloneolignanin A and its enantiomer, particularly scarce in nature, was tested and showed good anticancer activity.
Design, Synthesis, and Structure–Activity Relationships of Bavachinin Analogues as Peroxisome Proliferator-Activated Receptor γ Agonists
Du, Guoxin,Zhao, Yuanyuan,Feng, Li,Yang, Zhuo,Shi, Jiye,Huang, Cheng,Li, Bo,Guo, Fujiang,Zhu, Weiliang,Li, Yiming
, p. 183 - 193 (2017/02/05)
Peroxisome proliferator-activated receptor γ (PPARγ) agonists have been used for the treatment of diabetes with the effect of lowering blood glucose levels and improving insulin sensitivity. Natural compounds such as flavones, flavanones, and isoflavones
CYCLOPROPANE COMPOUND
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Page/Page column 151-152, (2012/04/23)
A cyclopropane compound represented by the following formula (A) or a pharmaceutically acceptable salt thereof has orexin receptor antagonism, and therefore has a potencial of usefulness for the treatment of sleep disorder for which orexin receptor antagonism is effective, for example, insomnia: wherein Q represents —CH— or a nitrogen atom, R1a and R1b each independently represent a C1-6 alkyl group and the like, R1c represents a hydrogen atom and the like, R2a, R2b, R2c and R2d each independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group and the like, R3a, R3b and R3c each independently represent a hydrogen atom, a halogen atom and the like, and R3d represents a hydrogen atom and the like.
Epigenetic multiple ligands: Mixed histone/protein methyltransferase, acetyltransferase, and class III deacetylase (Sirtuin) inhibitors
Mai, Antonello,Cheng, Donghang,Bedford, Mark T.,Valente, Sergio,Nebbioso, Angela,Perrone, Andrea,Brosch, Gerald,Sbardella, Gianluca,De Bellis, Floriana,Miceli, Marco,Altucci, Lucia
, p. 2279 - 2290 (2008/12/22)
A number of new compounds bearing two ortho-bromo- and ortho,ortho- dibromophenol moieties linked through a saturated/unsaturated, linear/(poly)cyclic spacer (compounds 1-9) were prepared as simplified analogues of AMI-5 (eosin), a recently reported inhibitor of both protein arginine and histone lysine methyltransferases (PRMTs and HKMTs). Such compounds were tested against a panel of PRMTs (RmtA, PRMT1, and CARM1) and against human SET7 (a HKMT), using histone and nonhistone proteins as a substrate. They were also screened against HAT and SIRTs, because they are structurally related to some HAT and/or SIRT modulators. From the inhibitory data, some of tested compounds (1b, 1c, 4b, 4f, 4j, 4l, 7b, and 7f) were able to inhibit PRMTs, HKMT, HAT, and SIRTs with similar potency, thus behaving as multiple ligands for these epigenetic targets (epi-MLs). When tested on the human leukemia U937 cell line, the epi-MLs induced high apoptosis levels [i.e., 40.7% (4l) and 42.6% (7b)] and/or massive, dose-dependent cytodifferentiation [i.e., 95.2% (1c) and 96.1% (4j)], whereas the single-target inhibitors eosin, curcumin, and sirtinol were ineffective or showed a weak effect.
