95605-38-2Relevant academic research and scientific papers
New pyridin-3-ylmethyl carbamodithioic esters activate pyruvate kinase M2 and potential anticancer lead compounds
Zhang, Yu,Liu, Bin,Wu, Xingyu,Lei, Ridong,Ning, Xianling,Liu, Yu,Liu, Zhenming,Ge, Zemei,Li, Runtao,Yin, Yuxin
, p. 4815 - 4823 (2015/08/03)
Pyruvate kinase M2 (PKM2) is a key protein responsible for cancer's Warburg effect. Activation of PKM2 may alter aberrant metabolism in cancer cells, which suggests PKM2 as a tumor selective therapeutic target. In this paper, the lead compound 8 was first discovered as a new kind of PKM2 activator from a random screening of an in-house compound library. Then, a series of lead compound 8 analogs were designed, synthesized and evaluated for their activation of PKM2 and anticancer activities. 7-Azaindole analog 32 was identified as the most potent PKM2 activator. Compounds with potent enzyme activity also exhibited selective anti-proliferation activity on cancer cell lines HCT116, Hela and H1299 compared with non-tumor cell line BEAS-2B. The structure-activity relationships of these compounds were supported by molecular docking results. Preliminary pharmacological studies also showed that compound 32 arrests the cell cycle at the G2/M phase in HCT116 cell line.
Synthesis and evaluation of a novel hydrophobically associating polymer based on acrylamide for enhanced oil recovery
Sun, Jin-Sheng,Du, Wei-Chao,Pu, Xiao-Lin,Zou, Zhuan-Zheng,Zhu, Bo-Bo
, p. 1598 - 1607 (2015/10/20)
A novel polymerizable hydrophobic monomer 1-(4-dodecyloxy-phenyl)-propenone (DPP) was synthesized by esterification, Frise rearrangement and Williamson etherification; then, the obtained DPP was copolymerized with 2-(acrylamido)-dodecanesulfonic acid (AMC12S) and acrylamide (AM) initiated by a redox initiation system in an aqueous medium to enhance oil recovery (EOR). AM/AMC12S/DPP (PADP) was characterized by FT-IR, 1H NMR spectroscopy, environmental scanning electron microscopy (ESEM), DSC-TG, fluorescent probe, core flood test, etc. Results of ESEM and fluorescent probe indicate that hydrophobic microdomains and associating threedimensional networks were formed in the aqueous solution of PADP. Results of DSC-TG demonstrated that long carbon chains, aromatic groups and sulfonic groups were incorporated into the PADP polymer, which can lead to a significant increase of the rigidity of molecular chains. Performance evaluation of experiments showed superior properties in regard to temperature-tolerance, shear-tolerance and salt-tolerance. In the Sandpack Flooding Test, PADP brine solution showed a significant increase in EOR at 65°C because of its high thickening capability. All these features indicate that PADP has a potential application in EOR at harsh conditions.
Synthesis and micellar behaviors of an anionic polymerizable surfactant
Ma, Lihua,Guo, Yongjun,Feng, Rusheng,Xiang, Panpan,Li, Chunhui
, p. 583 - 588 (2014/05/20)
A novel anionic polymerizable surfactant sodium (5-acryloyl-2-(dodecyloxy) phenyl) methane sulfonate has been synthesized from phenol, acrylic acid and bromododecane by esterification, Frise rearrangement, sulfomethylation reaction and Williamson etherification. The parameters of the micellar behaviors are as follows: The CMC was 150 ppm at 40 °C; The surface absorption amounts Γm was 3.208 × 10-6 mol m-2; The molecular areas Am was 0.550 × 10-18m2 at the interface of air-water respectively; The aggregation number (N agg) at C = CMC of this surfactant was 12. A novel anionic polymerizable surfactant sodium (5-acryloyl-2-(dodecyloxy)phenyl) methane sulfonate has been synthesized from phenol, acrylic acid and bromododecane by esterification, Frise rearrangement, sulfomethylation reaction and Williamson etherification. The surfactantsynthesized was phenyl ether, and wasn't hydrolyzed in acidicor alkalic condition.
PHOSPHONATED RIFAMYCINS AND USES THEREOF FOR THE PREVENTION AND TREATMENT OF BONE AND JOINT INFECTIONS
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Page/Page column 80, (2011/11/06)
The present invention relates to phosphonated Rifamycins, and methods of making and using such compounds. These compounds are useful as antibiotics for prophylaxis and/or the treatment of bone and joint infections, especially for the prophylaxis and/or treatment of osteomyelitis.
Inactivation of GABA transaminase by 3-chloro-1-(4-hydroxyphenyl)propan-1-one
Tao, Yun-Hai,Xu, Hui-Bi,Yang, Xiang-Liang
body text, p. 731 - 734 (2009/10/02)
Previously it was found that 4-hydroxybenzaldehyde is a competitive inhibitor of GABA transaminase. Here 3-chloro-1-(4-hydroxyphenyl)propan-1-one (9), a 4-hydroxybenzaldehyde analogue, was found to inactivate potently the enzyme in a time-dependent manner. α-Ketoglutarate prevented the enzyme from inactivation, suggesting that the inactivation occurs in its active site. Several experiments indicated that the inactivation is irreversible. This study provides a novel strategy for the design of more effective inhibitors.
Phosphonated Fluoroquinolones, Antibacterial Analogs Thereof, and Methods for the Prevention and Treatment of Bone and Joint Infections
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Page/Page column 88-89, (2008/12/09)
The present invention relates to phosphonated fluoroquinolones, antibacterial analogs thereof, and methods of using such compounds. These compounds are useful as antibiotics for prevention and/or the treatment of bone and joint infections, especially for the prevention and/or treatment of osteomyelitis.
Linking bisphosphonates to the free amino groups in fluoroquinolones: Preparation of osteotropic prodrugs for the prevention of osteomyelitis
Houghton, Tom J.,Tanaka, Kelly S. E.,Kang, Ting,Dietrich, Evelyne,Lafontaine, Yanick,Delorme, Daniel,Ferreira, Sandra S.,Viens, Frederic,Arhin, Francis F.,Sarmiento, Ingrid,Lehoux, Dario,Fadhil, Ibtihal,Laquerre, Karine,Liu, Jing,Ostiguy, Valérie,Poirier, Hugo,Moeck, Gregory,Parr Jr., Thomas R.,Far, Adel Rafai
experimental part, p. 6955 - 6969 (2009/11/30)
Osteomyelitis is an infection located in bone and a notoriously difficult disease to manage, requiring frequent and heavy doses of systemically administered antibiotics. Targeting antibiotics to the bone after systemic administration may provide both grea
