20443-03-2Relevant articles and documents
Synthetic Approaches to the Bifunctional Chelators for Radio nuclides Based on Pyridine-Containing Azacrown Compounds
Fedorova, Olga A.,Shchukina, Anna A.,Zubenko, Anastasia D.
, p. 1087 - 1095 (2020)
Synthetic ways to introduce functional groups (CO 2 Me, CO 2 H, OCH 2 CO 2 H, OCH 2 C≡CH, CH 2 OH, CH 2 Cl, CH 2 N 3) into the pyridine ring of pyridine-containing azacrown compounds are described. These groups were introduced at position-4 of the pyridine ring, while keeping the macrocyclic carboxylate groups available for metal chelation. The derivatives were obtained by macrocyclization reaction of 4-substituted, trimethyl pyridine-2,4,6-tricarboxylate or by modification of methyl ester group in pyridine fragment of macrocycles. Obtained derivatives can be applied for preparing radiotherapeutic agents by conjugation to different vector biomolecules for targeted drug delivery to cancer cells without damaging healthy tissue.
Monitoring and Modulating mtDNA G-Quadruplex Dynamics Reveal Its Close Relationship to Cell Glycolysis
Chen, Shuo-Bin,Chen, Xiu-Cai,Dai, Jing,Huang, Zhi-Shu,Luo, Wen-Hua,Shao, Wen,Tan, Jia-Heng,Tang, Gui-Xue,Zeng, Shu-Tang
supporting information, p. 20779 - 20791 (2021/12/14)
The mitochondrial DNA G-quadruplex (mtDNA G4) is a potential regulatory element for the regulation of mitochondrial functions; however, its relevance and specific roles in diseases remain largely unknown. Here, we engineered a set of chemical probes, incl
Picolinamide oligomers, preparation method and applications thereof
-
Paragraph 0024; 0047; 0050, (2018/08/28)
The invention belongs to the technical field of membrane separation, and more specifically relates to picolinamide oligomers, a preparation method and applications thereof. The picolinamide oligomerscomprise the following characteristics: 1. the oligomers
The assembly of "s3N"-ligands decorated with an azo-dye as potential sensors for heavy metal ions
Rasheed,McDouall,Muryn,Raftery,Vitorica-Yrezabal,Quayle
, p. 5229 - 5239 (2017/04/27)
An "S3N-ligand azo-dye" conjugate has been synthesised with a view to the development of a sensor for heavy metal ions. Complexation of this system with Ag(i), Hg(ii) and Cu(ii) salts has been investigated and an X-ray structure has been obtained for a Hg(ii) complex. Complexation of the conjugated dye to these metals results in a bathochromic shift in the absorption maximum of the azo dye, an effect which is most pronounced for Cu(ii).
The Synthesis of Group 10 and 11 Metal Complexes of 3,6,9-Trithia-1-(2,6)-pyridinacyclodecaphane and Their Use in A3-Coupling Reactions
Rasheed, Omer K.,Bawn, Carlo,Davies, David,Raftery, James,Vitorica-Yrzebal, I?igo,Pritchard, Robin,Zhou, Huimin,Quayle, Peter
supporting information, p. 5252 - 5261 (2017/09/29)
The reaction between 3,6,9-trithia-1(2,6)-pyridinacyclodecaphane and representative group 10 and 11 metal salts [Cu(NO3)2, NiCl2 or Ag(CF3CO2)] afforded 1:1 complexes, which in the case of CuII and AgI were characterised by single-crystal X-ray crystallography. The catalytic activity of these complexes in A3-coupling reactions between aldehydes, terminal alkynes and amines was assessed in both protic (water) and aprotic (toluene) media. These A3-reactions prove to be more efficient, proceed with lower catalyst loadings and with faster reaction rates, when conducted in a focused microwave reactor as compared to the same reactions promoted by standard, thermal, modes of activation.
Pyridostatin compound and its preparation method and application
-
Paragraph 0037-0040, (2016/10/09)
The invention provides Pyridostatin compounds, and a preparation method and application thereof. The structural formula of the Pyridostatin compounds is disclosed as Formula I. The compounds and pharmaceutically acceptable salts thereof have favorable antitumor activity for human lung cancer and human colon cancer.
Stabilization of G-quadruplex DNA and inhibition of Bcl-2 expression by a pyridostatin analog
Feng, Yun,Yang, Dazhang,Chen, Hongbo,Cheng, Wenli,Wang, Lixia,Sun, Hongxia,Tang, Yalin
supporting information, p. 1660 - 1663 (2016/07/27)
The G-quadruplexes located in the P1 promoter of B-cell lymphoma-2 (Bcl-2) gene are implicated to regulate Bcl-2 expression. Here, we designed a new pyridostatin analog named PDF, which exhibited high specificity and stabilizing effect toward G-quadruplexes. The luciferase assay demonstrated that PDF could significantly suppress Bcl-2 transcriptional activation in human laryngeal squamous carcinoma cells (Hep-2) cells. Besides, PDF also induced cell apoptosis in vitro assays. These results provide an excellent G-quadruplex specific ligand as an efficient Bcl-2 inhibitor. These results also implicate that PDF may be a potential anticancer drug to head neck cancer.
Pyridostatins selectively recognize two different forms of the human telomeric G-quadruplex structures and their anti-tumor activities in vitro
Wang, Li-Xia,Shang, Qian,Li, Qian,Xiang, Jun-Feng,Liu, Yan,Guan, Ai-Jiao,Sun, Hong-Xia,Yu, Li-Jia,Tang, Ya-Lin
supporting information, p. 4982 - 4986 (2015/06/23)
G-quadruplex as a therapeutic target to develop novel anti-cancer agents has attracted a growing interest. Among all the ligands of G-quadruplexes, pyridostatin derivatives play a very important role. Here, we first reported the recognition of the fundamental skeleton pyridostatin I, which was simply synthesized. Compared to pyridostatin II comprising terminal amino groups, pyridostatin I selectively stabilized intramolecular anti-parallel telomeric G-quadruplex by raising the melting temperature about 20 °C at 295 nm of H22, while pyridostatin II preferred to stabilize intermolecular parallel telomeric G-quadruplex by raising the melting temperature about 25 °C at 265 nm of H7, maybe due to the suited size measurements between G-quadruplex hosts and pyridostatin guests. MTT assays indicated that pyridostatin II had better cytotoxic effects against HCT-8 and A549 cell lines obviously, indicating positively charged side chains may be required for improving the water solubility and cellular uptake of the apolar central skeleton.
Structure-activity relationship study of BACE1 inhibitors possessing a chelidonic or 2,6-pyridinedicarboxylic scaffold at the P2 position
Hamada, Yoshio,Suzuki, Kenji,Nakanishi, Tomoya,Sarma, Diganta,Ohta, Hiroko,Yamaguchi, Ryoji,Yamasaki, Moe,Hidaka, Koushi,Ishiura, Shoichi,Kiso, Yoshiaki
, p. 618 - 623 (2014/01/23)
We have previously reported potent substrate-based pentapeptidic BACE1 inhibitors possessing a hydroxymethylcarbonyl isostere as a substrate transition-state mimic. While these inhibitors exhibited potent activities in enzymatic and cellular assays (KMI-4
A novel small molecule that alters shelterin integrity and triggers a DNA-damage response at telomeres
Rodriguez, Raphael,Mueller, Sebastian,Yeoman, Justin A.,Trentesaux, Chantal,Riou, Jean-Francois,Balasubramanian, Shankar
supporting information; experimental part, p. 15758 - 15759 (2009/05/15)
We describe a novel synthetic small molecule which shows an unprecedented stabilization of the human telomeric G-quadruplex with high selectivity relative to double-stranded DNA. We report that this compound can be used in vitro to inhibit telomerase activity and to uncap human POT1 (protection of telomeres 1) from the telomeric G-overhang. We also show that the small molecule G-quadruplex binder induces a partial alteration of shelterin through POT1 uncapping from telomeres in human HT1080 cancer cells and the presence of γH2AX foci colocalized at telomeres. Copyright