125872-97-1Relevant academic research and scientific papers
NOVEL PROCESS FOR THE PREPARATION OF BELINOSTAT
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Page/Page column 23, (2017/12/16)
The present invention provides a novel and commercially viable process with high yield for the preparation of (E)-N-hydroxy-3-(3-phenylsulfamoyl-phenyl)-acrylamide, also known as Belinostat (I). The invention also provides process for purification and nov
5,6-dihydropyrrolo[2,1-a]isoquinolines as alternative of new drugs with cytotoxic activity
Chávez-Santos, Rosa María,Torres-Ochoa, Rubén Omar,Ramírez-Apan, María Teresa,Martínez, Roberto,Reyes-Gutiérrez, Paul Eduardo
, p. 973 - 981 (2018/11/02)
In this study, the pyrrolo[2,1-a]isoquinolines 4a–n were synthesized in good yields in a three steps synthesis from the corresponding α,β-unsaturated esters starting materials. These compounds were tested on six human cancer cells lines to measure the cyt
Synthesis of fluorescent molecular probes based on cis-cinnamic acid and molecular imaging of lettuce roots
Fukuda, Hiroshi,Nishikawa, Keisuke,Fukunaga, Yukihiro,Okuda, Katsuhiro,Kodama, Kozue,Matsumoto, Kenji,Kano, Arihiro,Shindo, Mitsuru
supporting information, p. 6492 - 6498 (2016/09/23)
We synthesized azo dye- and fluorescence-labeled cis-cinnamic acid analogues possessing inhibitory activity against lettuce root growth and a trans-isomer without bioactivity as a control probe. The radicles incubated with the azo dye-labeled analogue were stained red, with their tips especially deeply dyed. The fluorescent images of the radicles incubated with each of these molecular probes depicted that the root cap was fluorescence-stained. However, images of the control radicles prepared by staining with the trans-isomer fluorescent probe did not show emission at the root cap. These contrasts suggest specific localization of the cis-cinnamate analogue at the columella cells.
N, N-disubstituted benzo-nitrogen heterocycles-2-amine compound and use thereof
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, (2016/10/09)
The invention mainly relates to an N,N-double substituted benzoazacyclo-2-amide compound and an application thereof. The N,N-double substituted benzoazacyclo-2-amide compound is a compound shown as formula I or a salt formed by a medical acid or alkali. The compound provided by the invention has strong inhibition activity on RhoA protease which is tightly related with cardiovascular and cerebrovascular diseases. The compound provided by the invention is hopeful to be developed into a RhoA protease small-molecule inhibitor type cardiovascular and cerebrovascular disease treatment medicine.
Development of second-generation small-molecule RhoA inhibitors with enhanced water solubility, tissue potency, and significant in vivo efficacy
Ma, Sheng,Deng, Jing,Li, Baoli,Li, Xiujiang,Yan, Zhaowei,Zhu, Jin,Chen, Gang,Wang, Zhong,Jiang, Hualiang,Miao, Liyan,Li, Jian
, p. 193 - 206 (2015/03/13)
RhoA, a member of the Rho GTPases, is involved in a variety of cellular functions and could be a suitable therapeutic target for the treatment of cardiovascular diseases. However, few small-molecule RhoA inhibitors have been reported. Based on our previously reported lead compounds, 32 new 2-substituted quinoline (or quinoxaline) derivatives were synthesized and tested in biological assays. Six compounds showed high RhoA inhibitory activities, with IC50 values of 1.17-1.84 μM. Among these, (E)-3-(3-(ethyl(quinolin-2-yl)amino)phenyl)acrylic acid (26b) and (E)-3-(3-(butyl(quinolin-2-yl)amino)phenyl)acrylic acid (26d) demonstrated noticeable vasorelaxation effects against phenylephrine-induced contraction in thoracic aorta artery rings, and compound 26b had good water solubility and showed significant in vivo efficacy, which was similar to that of 5-(1,4-diazepane-1-sulfonyl)isoquinoline (fasudil) in a subarachnoid hemorrhage-cardiovascular model. To the best of our knowledge, compound 26b is the first example of a small-molecule RhoA inhibitor with potent in vivo efficacy, which could serve as a good lead for designing cardiovascular agents.
Identification of novel phenyl butenonyl C-glycosides with ureidyl and sulfonamidyl moieties as antimalarial agents
Ramakrishna, K. Kumar G.,Gunjan, Sarika,Shukla, Akhilesh Kumar,Pasam, Venkata Reddy,Balaramnavar, Vishal M.,Sharma, Abhisheak,Jaiswal, Swati,Lal, Jawahar,Tripathi, Renu,Anubhooti,Ramachandran, Ravishankar,Tripathi, Rama Pati
supporting information, p. 878 - 883 (2014/09/17)
A new series of C-linked phenyl butenonyl glycosides bearing ureidyl(thioureidyl) and sulfonamidyl moieties in the phenyl rings were designed, synthesized, and evaluated for their in vitro antimalarial activities against Plasmodium falciparum 3D7 (CQ sensitive) and K1 (CQ resistant) strains. Among all the compounds screened the C-linked phenyl butenonyl glycosides bearing sulfonamidyl moiety (5a) and ureidyl moiety in the phenyl ring (7d and 8c) showed promising antimalarial activities against both 3D7 and K1 strains with IC50 values in micromolar range and low cytotoxicity offering new HITS for further exploration.
Novel symmetrical ureas as modulators of protein arginine methyl transferases
Fontán, Noelia,García-Domínguez, Patricia,álvarez, Rosana,De Lera, ángel R.
, p. 2056 - 2067 (2013/05/09)
Methylation of histone arginine residues is an epigenetic mark related to gene expression that is implicated in a variety of biological processes and can be reversed by small-molecule modulators of protein arginine methyltransferases (PRMTs). A series of symmetrical ureas, designed as analogues of the known PRMT1 inhibitor AMI-1 have been synthesized using Pd-catalyzed Ar-N amide bond formation processes or carbonylation reactions as key steps. Their inhibitory profile has been characterized. The enzymatic assays showed a weak effect on PRMT1 and PRMT5 activity for most of the compounds. The acyclic urea that exhibited the strongest effect on the inhibition of the PRMT1 activity also showed the greatest effect on the expression of some androgen receptor target genes (TMPRSS2 and FKBP5), which may be related with its enzymatic activity. Surprisingly, AMI-1 behaved as an activator of PRMT5 activity, a result not reported so far.
Compositions Including 6-Aminohexanoic Acid Derivatives As HDAC Inhibitors
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Page/Page column 45, (2012/04/23)
This invention relates to compounds of Formula (I) wherein Cy1, L1, Y, R1, L2, and Ar2 are defined herein, for the treatment of cancers, inflammatory disorders, and neurological conditions.
EP2 RECEPTOR AGONISTS
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Page/Page column 68; 115, (2008/06/13)
A compound of Formula (I) or a salt, solvate and chemically protected form thereof, wherein: R5 is an optionally substituted C5-20 aryl or C4-20 alkyl group; A is selected from the group consisting of Formulae (Ai), (Aii), (Aiii) D is selected from Formulae (Di), (Dii), (Diii), (Div), (Dv) B is selected from the group consisting of Formulae (Bi), (Bii), (Biii), (Biv) (Bv).
3-Ureidobenzodiazepinones useful as antagonists of CCK or of gastrin
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, (2008/06/13)
This invention relates to compounds having formula (I), STR1 wherein R1 is a hydrogen or halogen atom or an alkyl, alkoxy, alkylthio, nitro, hydroxy or cyano radical; R2 is an alkyl radical or a chain --CH(R5)--CO--R6
