5840-03-9Relevant academic research and scientific papers
Growing the molecular architecture of imidazole-like ligands in HO-1 complexes
Floresta, Giuseppe,Fallica, Antonino N.,Salerno, Loredana,Sorrenti, Valeria,Pittalà, Valeria,Rescifina, Antonio
, (2021/10/29)
Up-regulation of HO-1 had been frequently reported in different cases and types of human malignancies. Since poor clinical outcomes are reported in these cases, this enzyme's inhibition is considered a valuable and proven anticancer approach. To identify
HETEROCYCLIC COMPOUNDS FOR MODULATING NR2F6
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Paragraph 00503-00504; 00527, (2021/09/04)
The present disclosure relates to compounds capable of modulating the activity of NR2F6. The compounds of the disclosure may be used in methods for the prevention and/or the treatment of diseases and disorders associated with modulating NR2F6 activity.
PSNCBAM-1 analogs: Structural evolutions and allosteric properties at cannabinoid CB1 receptor
Meini, Serena,Gado, Francesca,Stevenson, Lesley A.,Digiacomo, Maria,Saba, Alessandro,Codini, Simone,Macchia, Marco,Pertwee, Roger G.,Bertini, Simone,Manera, Clementina
, (2020/07/20)
Allosteric modulation of the CB1Rs could represent an alternative strategy for the treatment of diseases in which these receptors are involved, without the undesirable effects associated with their orthosteric stimulation. PSNCBAM-1 is a reference diaryl urea derivative that positively affects the binding affinity of orthosteric ligands (PAM) and negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs. In this work we reported the design, synthesis and biological evaluation of three different series of compounds, derived from structural modifications of PSNCBAM-1 and its analogs reported in the recent literature. Almost all the new compounds increased the percentage of binding affinity of CP55940 at CB1Rs, showing a PAM profile. When tested alone in the [35S]GTPγS functional assay, only a few derivatives lacked detectable activity, so were tested in the same functional assay in the presence of CP55940. Among these, compounds 11 and 18 proved to be functional NAMs at CB1Rs, dampening the orthosteric agonist-induced receptor functionality by approximately 30percent. The structural features presented in this work provide new CB1R-allosteric modulators (with a profile similar to the reference compound PSNCBAM-1) and an extension of the structure-activity relationships for this type of molecule at CB1Rs.
One-pot propagation of (Hetero)Arylamines: Modular synthesis of diverse Amino-di(hetero)arylamines
Liang, Xueting,Xu, Liang,Li, Cuihua,Jia, Xin,Wei, Yu
, p. 721 - 731 (2019/01/08)
Formal propagation of (hetero)arylamine is achieved via a one-pot Buchwald–Hartwig C–N cross-coupling and nitro reduction sequence, enabling a rapid modular synthesis of diverse amino-di(hetero)arylamines from (hetero)arylamines and halogenated nitrobenzenes. Various functionalized aromatic amines with different electronic and steric environments can be efficiently prolongated to formally incorporate another arylamino fragments. This approach has been successfully applied in the synthesis of more than forty amino-di(hetero)arylamines. The applicability of this method has also been demonstrated in the synthesis of oligoanilines and the tyrosine-kinase inhibitor Imatinib.
Discovery of 2-((4,6-dimethylpyrimidin-2-yl)thio)-N-phenylacetamide derivatives as new potent and selective human sirtuin 2 inhibitors
Yang, Lingling,Ma, Xiaobo,Yuan, Chen,He, Yanying,Li, Ling,Fang, Sha,Xia, Wei,He, Tao,Qian, Shan,Xu, Zhihong,Li, Guobo,Wang, Zhouyu
supporting information, p. 230 - 241 (2017/04/19)
Human sirtuin 2 (SIRT2) plays pivotal roles in multiple biological processes such as cell cycle regulation, autophagy, immune and inflammatory responses. Dysregulation of SIRT2 was considered as a main aspect contributing to several human diseases, including cancer. Development of new potent and selective SIRT2 inhibitors is currently desirable, which may provide a new strategy for treatment of related diseases. Herein, a structure-based optimization approach led to new 2-((4,6-dimethylpyrimidin-2-yl)thio)-N-phenylacetamide derivatives as SIRT2 inhibitors. SAR analyses with new synthesized derivatives revealed a number of new potent SIRT2 inhibitors, among which 28e is the most potent inhibitor with an IC50 value of 42?nM. The selectivity analyses found that 28e has a very good selectivity to SIRT2 over SIRT1 and SIRT3. In cellular assays, 28e showed a potent ability to inhibit human breast cancer cell line MCF-7 and increase the acetylation of α-tubulin in a dose-dependent manner. This study will aid further efforts to develop highly potent and selective SIRT2 inhibitors for the treatment of cancer and other related diseases.
Novel SIRT2 protein inhibitor and usage thereof in pharmacy
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Paragraph 0091; 0093, (2017/08/28)
The invention discloses a compound or salt, crystallographic form and solvate compounds of the compound acceptable in pharmacy, and the compound and the salt, crystallographic form, solvate compounds of the compound are shown as formula I, wherein X is selected from the formulas (please see the specifications for the formula); R1 is selected from aryl or ceteroary or substituted aryl or substituted ceteroary or from the formula (please see the specifications for the formula); R2 is selected from the formulas (please see the specifications for the formula); and R3 is selected from halogen or C1-C4 alkyl or C1-C4 alkoxy. The novel compound shown in formula I has the advantages that not only is good inhibitory activity achieved to SIRT2, but also the inhibiting effect is achieved to the tumor, and the novel compound has good pharmaceutical potentiality and provides a novel potential choice for the clinical medicament.
Nickel(0)/N-heterocyclic carbene complexes catalysed arylation of aromatic diamines
Kuhl, Sébastien,Fort, Yves,Schneider, Rapha?l
, p. 6169 - 6177 (2007/10/03)
Nickel complexes of N-heterocyclic carbenes were examined for effecting C-N coupling reactions between aromatic diamines and aryl chlorides of varying electron density. The Ni(0) ? 2IPr (IPr = N,N′-bis(2,6- diisopropylphenyl)imidazol-2-ylidene) complex associated to t-BuONa allowed N,N′-diarylation at 100 °C in 1,4-dioxane with excellent yields. Selective monoarylation of diamines could be performed in THF at 65 °C.
On attempted oxidative cyclisation of isomeric N,N'-diphenylphenylenediamines and their N,N'-dimethyl derivatives by palladium(II) acetate and UV light
Chakrabarty,Batabyal,Khasnobis
, p. 3651 - 3668 (2007/10/03)
The cyclisation of N,N'-diphenyl-o-, m- and p-phenylenediamines and their N,N'-dimethyl derivatives by palladium(II) acetate and UV light separately led to both bis-cyclisation, furnishing indolocarbazoles, and mono-cyclisations with cleavage as well as retention of one substituent, producing substituted carbazoles.
Preparation and pharmacological activities of 10-homolupinanoyl-2-R- phenothiazines
Sparatore,Sparatore
, p. 5 - 17 (2007/10/02)
Pursuing our researches on quinolizidinyl derivatives of phenothiazine and on the ground of antidepressive, diuretic, antianginal and antiarrhythmic activities of several 10-(3-dialkylamino) propionylphenothiazines (as chloracizine, moricizine, etc.), six
