73870-24-3Relevant articles and documents
Novel quinolone-based potent and selective HDAC6 inhibitors: Synthesis, molecular modeling studies and biological investigation
Relitti, Nicola,Saraswati, A. Prasanth,Chemi, Giulia,Brindisi, Margherita,Brogi, Simone,Herp, Daniel,Schmidtkunz, Karin,Saccoccia, Fulvio,Ruberti, Giovina,Ulivieri, Cristina,Vanni, Francesca,Sarno, Federica,Altucci, Lucia,Lamponi, Stefania,Jung, Manfred,Gemma, Sandra,Butini, Stefania,Campiani, Giuseppe
, (2020/11/24)
In this work we describe the synthesis of potent and selective quinolone-based histone deacetylase 6 (HDAC6) inhibitors. The quinolone moiety has been exploited as an innovative bioactive cap-group for HDAC6 inhibition; its synthesis was achieved by applying a multicomponent reaction. The optimization of potency and selectivity of these products was performed by employing computational studies which led to the discovery of the diethylaminomethyl derivatives 7g and 7k as the most promising hit molecules. These compounds were investigated in cellular studies to evaluate their anticancer effect against colon (HCT-116) and histiocytic lymphoma (U9347) cancer cells, showing good to excellent potency, leading to tumor cell death by apoptosis induction. The small molecules 7a, 7g and 7k were able to strongly inhibit the cytoplasmic and slightly the nuclear HDAC enzymes, increasing the acetylation of tubulin and of the lysine 9 and 14 of histone 3, respectively. Compound 7g was also able to increase Hsp90 acetylation levels in HCT-116 cells, thus further supporting its HDAC6 inhibitory profile. Cytotoxicity and mutagenicity assays of these molecules showed a safe profile; moreover, the HPLC analysis of compound 7k revealed good solubility and stability profile.
Copper-Induced Topology Switching and Thrombin Inhibition with Telomeric DNA G-Quadruplexes
Engelhard, David M.,Nowack, Julia,Clever, Guido H.
supporting information, p. 11640 - 11644 (2017/09/11)
The topological diversity of DNA G-quadruplexes may play a crucial role in its biological function. Reversible control over a specific folding topology was achieved by the synthesis of a chiral, glycol-based pyridine ligand and its fourfold incorporation into human telomeric DNA by solid-phase synthesis. Square-planar coordination to a CuII ion led to the formation of a highly stabilizing intramolecular metal–base tetrad, substituting one G-tetrad in the parent unimolecular G-quadruplex. For the Tetrahymena telomeric repeat, CuII-triggered switching from a hybrid-dominated conformer mixture to an antiparallel topology was observed. CuII-dependent control over a protein–G-quadruplex interaction was shown for the thrombin–tba pair (tba=thrombin-binding aptamer).
Semiconductor quantum dots photosensitizing release of anticancer drug
Liu, Zhenzhen,Lin, Qiuning,Huang, Qi,Liu, Hui,Bao, Chunyan,Zhang, Wenjin,Zhong, Xinhua,Zhu, Linyong
supporting information; experimental part, p. 1482 - 1484 (2011/03/20)
A new photo-controlled anticancer drug release system is reported based on the photo-induced electron transfer (PET) between semiconductor quantum dots (QDs) and N-methyl-4-picolinium (NAP) ester 1 under the excitation of visible light.
NOVEL BENZODIOXANE AND BENZOXAZINE DERIVATIVES USEFUL AS CC CHEMOKINE RECEPTOR LIGANDS
-
Page/Page column 81, (2010/06/22)
The present invention relates to benzodioxane and benzoxazine derivatives that act as ligands for CC chemokine receptors, such as CCR1. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
PIPERIDINONES USEFUL IN THE TREATMENT OF INFLAMMATION
-
Page/Page column 113, (2008/12/07)
There is provided compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, m and n have meanings given in the description, and pharmaceutically acceptable derivatives thereof, which compounds are useful in the treatment of diseases and conditions associated with inflammation.
Remote controlled nucleophilicity, 2: Lithiated C(α)-substituted 4-methylpyridines
Anders,Opitz,Bauer
, p. 1221 - 1227 (2007/10/02)
C(α)-substituted 4-methylpyridines have been N-lithiated and reacted with chlorotrimethylsilane and other electrophiles. The lithiated C(α)-NMe2 substituted intermediate shows an interesting dichotomy of behavior towards electrophiles: It represents the borderline between compounds for which an extreme N or C(α) regionucleophilicity is observed.
