36881-42-2Relevant articles and documents
The benzoquinone derivatives and their use
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Paragraph 0118, (2016/11/17)
The invention provides a p-benzoquinone derivative and an application thereof. The p-benzoquinone derivative has the inhibitory activity on a plasminogen activator inhibitor-1 (PAI-1); on cellular level, the compound can inhibit the transfer ability of HepG2 liver cancer cells; and in-vitro experiments show that the compound has an inhibition effect on formation of fibrin clots. The p-benzoquinone derivative can be used as a medicine for treating tumors and thrombotic diseases.
Synthesis and structure-activity analysis of new phosphonium salts with potent activity against African trypanosomes
Taladriz, Andrea,Healy, Alan,Flores Pérez, Eddysson J.,Herrero García, Vanessa,Ríos Martínez, Carlos,Alkhaldi, Abdulsalam A. M.,Eze, Anthonius A.,Kaiser, Marcel,De Koning, Harry P.,Chana, Antonio,Dardonville, Christophe
supporting information; scheme or table, p. 2606 - 2622 (2012/06/01)
A series of 73 bisphosphonium salts and 10 monophosphonium salt derivatives were synthesized and tested in vitro against several wild type and resistant lines of Trypanosoma brucei (T. b. rhodesiense STIB900, T. b. brucei strain 427, TbAT1-KO, and TbB48). More than half of the compounds tested showed a submicromolar EC50 against these parasites. The compounds did not display any cross-resistance to existing diamidine therapies, such as pentamidine. In most cases, the compounds displayed a good selectivity index versus human cell lines. None of the known T. b. brucei drug transporters were required for trypanocidal activity, although some of the bisphosphonium compounds inhibited the low affinity pentamidine transporter. It was found that phosphonium drugs act slowly to clear a trypanosome population but that only a short exposure time is needed for irreversible damage to the cells. A comparative molecular field analysis model (CoMFA) was generated to gain insights into the SAR of this class of compounds, identifying key features for trypanocidal activity.
Synthesis, biological evaluation, and molecular modeling investigation of chiral 2-(4-chloro-phenoxy)-3-phenyl-propanoic acid derivatives with PPARα and PPARγ agonist activity
Fracchiolla, Giuseppe,Lavecchia, Antonio,Laghezza, Antonio,Piemontese, Luca,Trisolini, Raffaella,Carbonara, Giuseppe,Tortorella, Paolo,Novellino, Ettore,Loiodice, Fulvio
experimental part, p. 9498 - 9510 (2009/04/05)
PPARs are ligand-activated transcription factors that govern lipid and glucose homeostasis and play a central role in cardiovascular disease, obesity, and diabetes. Herein, we present screening results for a series of chiral 2-(4-chloro-phenoxy)-3-phenyl-propanoic acid derivatives, some of which are potent PPARγ agonists as well as PPARα agonists. To investigate the binding modes of the most interesting derivatives into the PPARα and PPARγ binding clefts and evaluate their agonist activity, docking experiments, molecular dynamics simulations, and MM-PBSA analysis were performed.
