40680-63-5Relevant academic research and scientific papers
New Size-Expanded Fluorescent Thymine Analogue: Synthesis, Characterization, and Application
Hirashima, Shingo,Han, Ji Hoon,Tsuno, Hitomi,Tanigaki, Yusuke,Park, Soyoung,Sugiyama, Hiroshi
, p. 9913 - 9919 (2019)
Here, the synthesis, photophysical characterization, and application of a new size-expanded thymine nucleoside, dioxT, is described. dioxT has desirable qualities as a T surrogate, including excellent quantum yield (0.36) and high environmental sensitivity. When incorporated into single- and double-stranded DNA, dioxT showed excellent photophysical characteristics including a high quantum yield (average 0.20), and unlike BgQ, demonstrated dependence on neighboring bases without significant destabilization of the duplex. Interestingly, the matched base pair of adenine (A) and dioxT has the unique property that it exhibits higher fluorescence than mismatched base pairs, and dioxT has self-quenching effects. As one example of the possible applications of these promising features, single nucleoside polymorphism typing is demonstrated for discrimination of A by using dioxT. The results suggest that dioxT can be used for a broad range of applications in chemical biology.
ACTIVATORS OF THE RETINOIC ACID INDUCIBLE GENE "RIG-1" PATHWAY AND METHODS OF USE THEREOF
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Paragraph 0268, (2020/03/02)
The present invention is directed to compounds of Formula (I), which are activators of the RIG-I pathway.
ACTIVATORS OF THE RETINOIC ACID INDUCIBLE GENE "RIG-I' PATHWAY AND METHODS OF USE THEREOF
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Page/Page column 87, (2020/03/05)
The present invention is directed to compounds of Formula (I), which are activators of the RIG-I pathway.
ACTIVATORS OF THE RETINOIC ACID INDUCIBLE GENE "RIG-I" PATHWAY AND METHODS OF USE THEREOF
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Paragraph 0546, (2020/03/01)
The present invention is directed to compounds of Formula (I), which are activators of the RIG-I pathway.
As the PI3K/mTOR inhibitor tricyclic compound, its preparation and use
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Paragraph 0152; 0155, (2017/08/25)
The invention discloses a tricyclic compound as a PI3K/mTOR inhibitor. The tricyclic compound is a compound with the general formula (I) in the specification, wherein Ar is selected from aryl or heteroaryl; X, Y and Z are independently selected from O, CR2R3 and NR4 respectively; Q is selected from O, CR2R3 and NR4 or does not exists; R1 represents C1-C6 alkyl; n is selected from integers from 0 to 4; when n is more than or equal to 2, two R1 and a morpholine cycle can be combined into a combined cycle, a bridge cycle or a spiral cycle; R2 and R3 are selected from hydrogen and C1-C6 alkyl; R4 is selected from hydrogen, C1-C6 alkyl, C3-C7 cycloalkyl, heterocyclic radical, acyl and sulfonyl. The invention further discloses a perpetration method of the compound with the general formula (I) as well as a pharmaceutical composition and application of the compound with the general formula (I).
Computer-aided identification, synthesis, and biological evaluation of novel inhibitors for botulinum neurotoxin serotype A
Teng, Yu-Han Gary,Berger, William T.,Nesbitt, Natasha M.,Kumar, Kunal,Balius, Trent E.,Rizzo, Robert C.,Tonge, Peter J.,Ojima, Iwao,Swaminathan, Subramanyam
, p. 5489 - 5495 (2015/11/11)
Botulinum neurotoxins (BoNTs) are among the most potent biological toxin known to humans, and are classified as Category A bioterrorism agents by the Centers for Disease Control and prevention (CDC). There are seven known BoNT serotypes (A-G) which have b
Design, synthesis, and DNA-binding of N-alkyl(anilino)quinazoline derivatives
Garofalo, Antonio,Goossens, Laurence,Baldeyrou, Brigitte,Lemoine, Amélie,Ravez, Séverine,Six, Perrine,David-Cordonnier, Marie-Hélène,Bonte, Jean-Paul,Depreux, Patrick,Lansiaux, Amélie,Goossens, Jean-Fran?ois
scheme or table, p. 8089 - 8103 (2011/03/17)
New N-alkylanilinoquinazoline derivatives 5, 12, 20, and 22 have been prepared from 4-chloro-6,7-dimethoxyquinazoline 3, 4-chloro-6,7- methylenedioxyquinazoline 19, and commercially available anilines. Differents classes of compounds substituted by an aryloxygroup (6a-c, 16a,b, and 17a,b), (aminophenyl)ureas (12a,b and 13a-f), anilines (4a-m, 20a,b), N-alkyl(aniline) (5a-m, 21a,b, 22a,d), and N-aminoalkyl(aniline) (22e-g) have been synthesized. These molecules were evaluated for their cytotoxic activities and as potential DNA intercalating agents. We studied the strength and mode of binding to DNA of these molecules by DNA melting temperature measurements, fluorescence emission, and circular dichroism. The results of various spectral and gel electrophoresis techniques obtained with the different compounds, in particular compounds 5g and 22f, revealed significant DNA interaction. These experiments confirm that the N-aminoalkyl(anilino)-6,7-dimethoxyquinazoline nucleus is an efficient pharmacophore to trigger binding to DNA, via an intercalative binding process.
Novel 6-methanesulfonamide-3,4-methylenedioxyphenyl-N-acylhydrazones: Orally effective anti-inflammatory drug candidates
Tributino, Jorge L.M.,Duarte, Carolina D.,Correa, Rodrigo S.,Doriguetto, Antonio C.,Ellena, Javier,Romeiro, Nelilma C.,Castro, Newton G.,Miranda, Ana Luisa P.,Barreiro, Eliezer J.,Fraga, Carlos A.M.
experimental part, p. 1125 - 1131 (2009/09/25)
We described herein the molecular design of novel in vivo anti-inflammatory 6-methanesulfonamide-3,4-methylenedioxyphenyl-N-acylhydrazone derivatives (1) planned by applying the molecular hybridization approach. This work also points out to the discovery
Synthesis and analgesic profile of conformationally constrained N-acylhydrazone analogues: Discovery of novel N-arylideneamino quinazolin-4(3H)-one compounds derived from natural safrole
Maia, Rodolfo C.,Silva, Leandro L.,Mazzeu, Eduardo F.,Fumian, Milla M.,de Rezende, Claudia M.,Doriguetto, Antonio C.,Correa, Rodrigo S.,Miranda, Ana Luisa P.,Barreiro, Eliezer J.,Fraga, Carlos Alberto Manssour
experimental part, p. 6517 - 6525 (2009/12/06)
In this work we reported the synthesis and evaluation of the analgesic, anti-inflammatory, and platelet anti-aggregating properties of new 3-(arylideneamino)-2-methyl-6,7-methylenedioxy-quinazolin-4(3H)-one derivatives (3a-j), designed as conformationally constrained analogues of analgesic 1,3-benzodioxolyl-N-acylhydrazones (1) previously developed at LASSBio. Target compounds were synthesized in very good yields exploiting abundant Brazilian natural product safrole (2) as starting material. The pharmacological assays lead us to identify compounds LASSBio-1240 (3b) and LASSBio-1272 (3d) as new analgesic prototypes, presenting an antinociceptive profile more potent and effective than dipyrone and indomethacin used, respectively, as standards in AcOH-induced abdominal constrictions assay and in the formalin test. These results confirmed the success in the exploitation of conformation restriction strategy for identification of novel cyclic N-acylhydrazone analogues with optimized analgesic profile.
N-aryl(thio)anthranilic acid amide derivatives, their preparation and their use as VEGF receptor tyrosine kinase inhibitors
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, (2008/06/13)
Described are compounds of formula (I), wherein W is O or S; X is NR8; Y is CR9R10-(CH2)n wherein R9 and R10 are independently of each other hydrogen or lower alkyl, and n is an integer of
