62086-52-6Relevant academic research and scientific papers
DESIGN, SYNTHESIS, AND BIOLOGICAL ACTIVITY OF PLATINUM-BENZ[C]ACRIDINE HYBRID AGENTS AND METHODS ASSOCIATED THEREWITH
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Page/Page column 29, (2015/11/10)
The present invention relates to the compounds of formula (I), pharmaceutically acceptable salts, and solvates thereof, wherein the various substituents are as defined herein. The compounds, solvates and salts thereof of Formula (I) are effective as anti-cancer compounds.
NOVEL COMPOUNDS AS CHLORIDE CHANNEL BLOCKING AGENT
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Paragraph 0178; 0179; 0180; 0181; 0182; 0183; 0223-0225, (2015/06/03)
Disclosed is a novel compound to function as a calcium-dependent chloride channel blocking agent.
Redesigning the DNA-Targeted chromophore in platinum-acridine anticancer agents: A structure-activity relationship study
Pickard, Amanda J.,Liu, Fang,Bartenstein, Thomas F.,Haines, Laura G.,Levine, Keith E.,Kucera, Gregory L.,Bierbach, Ulrich
, p. 16174 - 16187 (2015/02/19)
Platinum-acridine hybrid agents show low-nano-molar potency in chemoresistant non-small cell lung cancer (NSCLC), but high systemic toxicity in vivo. To reduce the promiscuous genotoxicity of these agents and improve their pharmacological properties, a mo
Monna, a potent and selective blocker for transmembrane protein with unknown function 16/anoctamin-1
Oh, Soo-Jin,Hwang, Seok Jin,Jung, Jonghoon,Yu, Kuai,Kim, Jeongyeon,Choi, Jung Yoon,Hartzell, H. Criss,Roh, Eun Joo,Justin Lee
supporting information, p. 726 - 735 (2013/11/06)
Transmembrane protein with unknown function 16/anoctamin-1 (ANO1) is a protein widely expressed in mammalian tissues, and it has the properties of the classic calcium-activated chloride channel (CaCC). This protein has been implicated in numerous major physiological functions. However, the lack of effective and selective blockers has hindered a detailed study of the physiological functions of this channel. In this study, we have developed a potent and selective blocker for endogenous ANO1 in Xenopus laevis oocytes (xANO1) using a drug screening method we previously established (Oh et al., 2008). We have synthesized a number of anthranilic acid derivatives and have determined the correlation between biological activity and the nature and position of substituents in these derived compounds. A structure-activity relationship revealed novel chemical classes of xANO1 blockers. The derivatives contain a-NO2 group on position 5 of a naphthyl group-substituted anthranilic acid, and they fully blocked xANO1 chloride currents with an IC 5050 of 0.08 μM for xANO1. Selectivity tests revealed that other chloride channels such as bestrophin-1, chloride channel protein 2, and cystic fibrosis transmembrane conductance regulator were not appreciably blocked by 10~30 μM MONNA. The potent and selective blockers for ANO1 identified here should permit pharmacological dissection of ANO1/CaCC function and serve as potential candidates for drug therapy of related diseases such as hypertension, cystic fibrosis, bronchitis, asthma, and hyperalgesia.
Metal catalyst-free amination of 2-chloro-5-nitrobenzoic acid in superheated water
Lan, Cong,Xia, Zhi-Ning,Li, Zheng-Hua,Liang, Rong-Hui
, p. 726 - 728 (2013/02/23)
A series of N-arylanthranilic acid derivatives were synthesised by amination of 2-chloro-5-nitrobenzoic acid with various arylamine in superheated water with potassium carbonate as base. Good yields were achieved within 2-3 h at 150-190 °C. The results indicated that this metal catalyst-free method is a simple, environmentally-friendly and efficient synthesis of N-phenylanthranilic acid derivatives. Furthermore, it will work with an alkylamine and phenol.
