21900-25-4Relevant academic research and scientific papers
Macrofilaricidal Benzimidazole-Benzoxaborole Hybrids as an Approach to the Treatment of River Blindness: Part 2. Ketone Linked Analogs
Carter, David S.,Jacobs, Robert T.,Freund, Yvonne R.,Berry, Pamela W.,Akama, Tsutomu,Easom, Eric E.,Lunde, Christopher S.,Rock, Fernando,Stefanakis, Rianna,Mckerrow, James,Fischer, Chelsea,Bulman, Christina A.,Lim, Kee Chong,Suzuki, Brian M.,Tricoche, Nancy,Sakanari, Judy A.,Lustigman, Sara,Plattner, Jacob J.
, p. 180 - 185 (2020/02/13)
The optimization of a series of benzimidazole-benzoxaborole hybrid molecules linked via a ketone that exhibit good activity against Onchocerca volvulus, a filarial nematode responsible for the disease onchocerciasis, also known as river blindness, is desc
Palladium-Catalyzed C-H Trifluoroethoxylation of N-Sulfonylbenzamides
Yang, Long,Li, Shangda,Cai, Lei,Ding, Yongzheng,Fu, Lei,Cai, Zhihua,Ji, Huafang,Li, Gang
supporting information, p. 2746 - 2749 (2017/05/24)
The trifluoroethyl aryl ethers are important motifs in drug molecules. However, a report devoted specifically to the study of transition-metal-catalyzed C-H trifluoroethoxylation has not been reported to date. A protocol of Pd(II)-catalyzed o-C-H trifluor
Studies on phenothiazines: New microtubule-interacting compounds with phenothiazine A-ring as potent antineoplastic agents
Ghinet, Alina,Moise, Iuliana-Monica,Rigo, Beno?t,Homerin, Germain,Farce, Amaury,Dubois, Jo?lle,B?cu, Elena
, p. 2307 - 2317 (2016/04/26)
New phenothiazine derivatives 6-20 have been designed, synthesized and evaluated in vitro for their ability to inhibit tubulin polymerization and antiproliferative activity against 60 cancer cell lines, including several multi-drug resistant (MDR) tumor cell lines. The phenothiazine unit may successfully replace the classical 3,4,5-trimethoxyphenyle A ring of parent combretastatin A-4 or phenstatin, confirming previous studies. The most promising structural modulations have been realized on the B ring, the 2′-fluoro-4′-methoxy substitution in compound 6 and the 2′-trifluoromethyl-4′-methoxy substitution in compound 7 providing the best antitubulin and antitumor activity in the current study. Compounds 6-8 and 16 exhibited more important cell growth inhibition than parent phenstatin 2 on human colon Duke's type D, colorectal adenocarcinoma COLO 205 and on human kidney adenocarcinoma A498 cell lines. 10-Methylphenothiazine derivatives 19 and 20 did not show biological activity but exerted bright fluorescence and solvatochromism effects. These molecules deserve further chemical efforts in order to provide valuable tools for biophysical studies.
Silicon and germanium dyes for use in genetic identity
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, (2015/11/16)
Si- and Ge-based dyes and methods of using same.
SUBSTITUTED TRIAZOLES AND THEIR USE FOR TREATMENT AND/OR PREVENTION NEUROLOGICAL AND PSYCHIATRIC DISORDERS
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Page/Page column 61, (2013/07/31)
This invention relates to compounds of formula (I), their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.
NOVEL COMPOUNDS
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Paragraph 0323; 0324, (2013/07/25)
This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.
Compounds for use as therapeutic agents affecting p53 expression and/or activity
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Page/Page column 48, (2012/10/18)
The present invention relates to compound (I) wherein R1 and R2 independently represent a hydrogen atom, a (C1-C4)alkoxy group, a fluoro(C1-C4)alkoxy group, a hydroxyl group, a benzyloxy group, a di(C1-C4)alkylamino group, a pyridyl-vinyl group, a pyrimidinyl-vinyl group, a styryl group, or a -NHCOphenyl group; R3, R4 and R5 independently represent a hydrogen atom, a (C1-C4)alkyl group, a CONHR6 group, a -CONR7R8 group, a -SO2NHR6 group, or a heteroaryl group optionally substituted by a halogen atom, a -(CH2)nNR7R8 group or a hydroxy(C1-C4)alkyl group; R6 represents a hydrogen atom, a -(CHR9)m(CH2)nNR7R8 group or a (C1-C6)alkyl group optionally substituted by a hydroxyl group; or anyone of its pharmaceutically acceptable salt, for use as an agent for preventing, inhibiting or treating a disease in a patient suffering thereof, said disease involving a deregulated p53. Some of said compounds are new and also form part of the invention.
The Synthesis and evaluation of a novel class of (E)-3-(1-cyclohexyl-1H- pyrazol-3-yl)-2-methylacrylic acid Hepatitis C virus polymerase NS5B inhibitors
Martin, Scott W.,Glunz, Peter,Beno, Brett R.,Bergstrom, Carl,Romine, Jeffrey L.,Scott Priestley,Newman, Makenzie,Gao, Min,Roberts, Susan,Rigat, Karen,Fridell, Robert,Qiu, Dike,Knobloh, Galina,Wang, Ying-Kai
supporting information; experimental part, p. 2869 - 2872 (2011/06/26)
Herein we report the identification and evaluation of a novel series of (E)-3-(1-cyclohexyl-1H-pyrazol-3-yl)-2-methylacrylic acid derivatives identified from a deannulation study performed on the reported benzimidazole NS5B inhibitor, 1. This resulted in
End group-functionalization and synthesis of block-copolythiophenes by modified nickel initiators
Smeets, Alfons,Willot, Pieter,De Winter, Julien,Gerbaux, Pascal,Verbiest, Thierry,Koeckelberghs, Guy
scheme or table, p. 6017 - 6025 (2012/03/08)
Polythiophenes with alcohol, tosylate, azide, ethynylene, carboxylic acid, and amine end groups were prepared by a combination of functionalized nickel initiators and postpolymerization reactions. The azide and ethynylene polymers were subsequently used in a click reaction to produce a conjugated block copolymer. Finally, a conjugated triblock-copolymer was synthesized by means of a chain growth polymerization initiated by a binuclear nickel initiator.
ANTAGONISTS OF LYSOPHOSPHATIDIC ACID RECEPTORS
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Page/Page column 22, (2010/06/22)
Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
