942400-07-9Relevant academic research and scientific papers
Synthesis and bioevaluation of substituted chalcones, coumaranones and other flavonoids as anti-HIV agents
Cole, Amy L.,Hossain, Sandra,Cole, Alex M.,Phanstiel, Otto
, p. 2768 - 2776 (2016)
A series of chalcone, flavone, coumaranone and other flavonoid compounds were screened for their anti HIV-1 activity in two cell culture models using TZM-bl and PM1 cells. Within the systems evaluated, the most promising compounds contained either an α- or β-hydroxy-carbonyl motif within their structure (e.g., 8 and 9). Efficacious substituents were identified and used to design new HIV inhibitors with increased potency and lower cytotoxicity. Of the scaffolds evaluated, specific chalcones were found to provide the best balance between anti-HIV potency and low host cell toxicity. Chalcone 8l was shown to inhibit different clinical isolates of HIV in a dose-dependent manner (e.g., IC50 typically ≤ 5 μM). Inhibition of HIV infection experiments using TZM-bl cells demonstrated that chalcone 8l and flavonol 9c had IC50 values of 4.7 μM and 10.4 μM, respectively. These insights were used to design new chalcones 8o and 8p. Rewardingly, chalcones 8o and 8p (at 10 μM) each gave >92% inhibition of viral propagation without impacting PM1 host cell viability. Inhibition of viral propagation significantly increased (60-90%) when PM1 cells were pre-incubated with chalcone 8o, but not with the related flavonol 9c. These results suggested that chalcone 8o may be of value as both a HIV prophylactic and therapy. In summary, O-benzyl-substituted chalcones were identified as promising anti-HIV agents for future investigation.
Introducing Seven Transition Metal Ions into Terpyridine-Based Supramolecules: Self-Assembly and Dynamic Ligand Exchange Study
Bai, Shi,Khalife, Sandra,Li, Xiaopeng,Li, Yiming,Ming, Li-June,Song, Bo,Wang, Heng,Wang, Lei,Wang, Ming,Xu, Yaping,Yu, Hao
supporting information, (2020/02/04)
In coordination-driven self-assembly, 2,2′:6′,2″-terpyridine (tpy) has gained extensive attention in constructing supramolecular architectures on the basis of a tpy-M-tpy?connectivity. In direct self-assembly of large discrete structures, however, the met
AMINE COMPOUND AND USE THEREOF FOR MEDICAL PURPOSES
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Page/Page column 62, (2008/12/08)
A novel amine compound represented by the following formula (I), which is superior in immunosuppressive action, rejection suppressive action and the like, and shows reduced side effects such as bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or hydrates thereof, or solvate, as well as a pharmaceutical composition containing this compound and a pharmaceutically acceptable carrier. wherein R is a hydrogen atom or P(=O)(OH)2, X is an oxygen atom or a sulfur atom, Y is CH2CH2 or CH=CH, R1 is cyano or alkyl having a carbon number of 1 to 4 and substituted by a halogen atom(s), R2 is alkyl having a carbon number of 1 to 4 and optionally substituted by a hydroxyl group(s) or a halogen atom(s), R3 and R4 may be the same or different and each is a hydrogen atom or alkyl having a carbon number of 1 to 4, and n is 5 - 8.
