38077-75-7Relevant articles and documents
Triphenyl ether amide as a probe for electrochemical and optical sensing of copper, cyanide and arginine
Chhibber, Manmohan,Gupta, Shivali,Mittal, Susheel K
, (2020/12/17)
A novel triphenyl ether amide (TPEAM) derivative has been synthesises and developed as a probe for electrochemical and optical sensing of copper, cyanide ions and arginine in the presence of other amino acids. The ionophore is selective for the copper and cyanide ions among various cations and anions, with detection limits as 40 nM and 0.4 μM, respectively. Sharp anodic and cathodic peaks in the differential pulse voltammograms of the TPEAM-Cu(II) complex indicated a good complexing tendency of the ligand molecule and it was confirmed by spectrofluorimetry and 1H NMR titrations. TPEAM-Cu2+ complex further detected arginine, a semi-essential amino acid, in aqueous medium with a lower detection limit of 4 μM. Host-guest interactions between TPEAM and Cu2+ ions and intramolecular charge transfer interactions (ICT) for CN- ions are proposed as possible mechanisms for the sensing of respective ions. Cyanide detection followed a non-sequential mechanism. The application of TPEAM as a probe for Cu2+ ions has also been validated on food samples and the results are compared with atomic absorption spectroscopy.
SAR optimization studies on modified salicylamides as a potential treatment for acute myeloid leukemia through inhibition of the CREB pathway
Chae, Hee-Don,Cox, Nick,Capolicchio, Samanta,Lee, Jae Wook,Horikoshi,Kam, Sharon,Ng, Andrew A.,Edwards, Jeffrey,Butler, Tae-León,Chan, Justin,Lee, Yvonne,Potter, Garrett,Capece, Mark C.,Liu, Corey W.,Wakatsuki, Soichi,Smith, Mark,Sakamoto, Kathleen M.
supporting information, p. 2307 - 2315 (2019/06/27)
Disruption of cyclic adenosine monophosphate response element binding protein (CREB) provides a potential new strategy to address acute leukemia, a disease associated with poor prognosis, and for which conventional treatment options often carry a significant risk of morbidity and mortality. We describe the structure-activity relationships (SAR) for a series of XX-650-23 derived from naphthol AS-E phosphate that disrupts binding and activation of CREB by the CREB-binding protein (CBP). Through the development of this series, we identified several salicylamides that are potent inhibitors of acute leukemia cell viability through inhibition of CREB-CBP interaction. Among them, a biphenyl salicylamide, compound 71, was identified as a potent inhibitor of CREB-CBP interaction with improved physicochemical properties relative to previously described derivatives of naphthol AS-E phosphate.
Scaffold Diversity Inspired by the Natural Product Evodiamine: Discovery of Highly Potent and Multitargeting Antitumor Agents
Wang, Shengzheng,Fang, Kun,Dong, Guoqiang,Chen, Shuqiang,Liu, Na,Miao, Zhenyuan,Yao, Jianzhong,Li, Jian,Zhang, Wannian,Sheng, Chunquan
, p. 6678 - 6696 (2015/09/07)
A critical question in natural product-based drug discovery is how to translate the product into drug-like molecules with optimal pharmacological properties. The generation of natural product-inspired scaffold diversity is an effective but challenging strategy to investigate the broader chemical space and identify promising drug leads. Extending our efforts to the natural product evodiamine, a diverse library containing 11 evodiamine-inspired novel scaffolds and their derivatives were designed and synthesized. Most of them showed good to excellent antitumor activity against various human cancer cell lines. In particular, 3-chloro-10-hydroxyl thio-evodiamine (66c) showed excellent in vitro and in vivo antitumor efficacy with good tolerability and low toxicity. Antitumor mechanism and target profiling studies indicate that compound 66c is the first-in-class triple topoisomerase I/topoisomerase II/tubulin inhibitor. Overall, this study provided an effective strategy for natural product-based drug discovery. (Figure Presented).
