Search results for "Deriva"

Cytotoxic activity of several ent-kaurane derivatives of atractyligenin. Synthesis of unreported diterpenic skeleton by chemical rearrangement

2022

Atractyloside, carboxyatractyloside, their aglycon atractyligenin, and several synthetic derivatives were tested and found to be active against a panel of human tumor cell lines. Atractyligenin was subjected to oxidation, bromination, and elimination reactions, obtaining several compounds. A singular skeleton was synthesized by chemical rearrangement starting from 3 beta-bromo-2,15-diketoatractyligenin methyl ester. The synthesized compounds resulted active against all cell lines tested. In particular, 15-ketoatractyligenin methyl ester and 3 beta bromo-2,15-diketoatractyligenin methyl ester resulted the most active with IC50 values of 0.427 and 0.723 mu M against A375 melanoma cell line. E…

Different muscarinic receptor subtypes modulate proliferation of primary human detrusor smooth muscle cells via Akt/PI3K and map kinases.

2013

While acetylcholine (ACh) and muscarinic receptors in the bladder are mainly known for their role in the regulation of smooth muscle contractility, in other tissues they are involved in tissue remodelling and promote cell growth and proliferation. In the present study we have used primary cultures of human detrusor smooth muscle cells (HDSMCs), in order to investigate the role of muscarinic receptors in HDSMC proliferation. Samples were obtained as discarded tissue from men >65 years undergoing radical cystectomy for bladder cancer and cut in pieces that were either immediately frozen or placed in culture medium for the cell culture establishment. HDSMCs were isolated from samples, propagat…

Efficient Capture of Organic Dyes and Crystallographic Snapshots by a Highly Crystalline Amino-Acid-Derived Metal-Organic Framework

2018

The presence of residual organic dyes in water resources or wastewater treatment systems, derived mainly from effluents of different industries, is a major environmental problem with no easy solution. Herein, an ecofriendly, water-stable metal-organic framework was prepared from a derivative of the natural amino acid l-serine. Its functional channels are densely decorated with highly flexible l-serine residues bearing hydroxyl groups. The presence of such a flexible and functional environment within the confined environment of the MOF leads to efficient removal of different organic dyes from water: Pyronin Y, Auramine O, Methylene Blue and Brilliant Green, as unveiled by unprecedented snaps…

DESIGN, SYNTHESIS, AND BIOLOGICAL EVALUATION OF NOVEL HETEROCYCLIC DERIVATIVES AS MODULATORS OF B-DNA AND G-QUADRUPLEXES DNA FUNCTIONS

Biogēno amīnu noteikšana Latvijas vīnos, izmantojot augsti efektīvo šķidrumu hromatogrāfiju

2018

Biogēno amīnu noteikšana, izmantojot augsti efektīvo šķidrumu hromatogrāfiju. Rimoviča K., zinātniskais vadītājs Dr. ķīm., pētnieks Antons Podjava. Bakalaura darbs. 40 lappuses, 9 attēli, 13 tabulas, 42 literatūras avoti, 2 pielikumi. Latviešu valodā. Literatūras apskatā apkopota informācija par biogēno amīnu veidošanos un funkcijām, kā arī derivatizāciju un fluorescences detektora lietošanu to analīzei. Eksperimentālajā daļā analizēti sešu biogēno amīnu standarti, mobilās fāzes vides pH ietekme, kā arī astoņu kolonnu ietekme uz joslu izšķiršanu, izmantojot augsti efektīvo šķidruma hromatogrāfiju ar fluorescences detektēšanu.

Computational Studies on BaCeO3 and BaZrO3 Derivatives.

2011

Asymmetric Michael Addition in Synthesis of β-Substituted GABA Derivatives

2022

γ-Aminobutyric acid (GABA) represents one of the most prolific structural units widely used in the design of modern pharmaceuticals. For example, β-substituted GABA derivatives are found in numerous neurological drugs, such as baclofen, phenibut, tolibut, pregabalin, phenylpiracetam, brivaracetam, and rolipram, to mention just a few. In this review, we critically discuss the literature data reported on the preparation of substituted GABA derivatives using the Michael addition reaction as a key synthetic transformation. Special attention is paid to asymmetric methods featuring synthetically useful stereochemical outcomes and operational simplicity. This research was funded by the National Na…

Effect of linker distribution in the photocatalytic activity of multivariate mesoporous crystals

2021

The use of Metal-Organic Frameworks as crystalline matrices for the synthesis of multiple component or multivariate solids by the combination of different linkers into a single material has emerged as a versatile route to tailor the properties of single-component phases or even access new functions. This approach is particularly relevant for Zr6-MOFs due to the synthetic flexibility of this inorganic node. However, the majority of materials are isolated as polycrystalline solids, which are not ideal to decipher the spatial arrangement of parent and exchanged linkers for the formation of homogeneous structures or heterogeneous domains across the solid. Here we use high-throughput methodologi…

Essays on Risk Disclosure: Evidence from the Banking Industry

2021

Influence of side chain characteristics on the aggregation-induced emission (AIE) properties of tetrasubstituted tetraphenylethylene (TPE)

2017

[EN] Five new tetraphenylethylene (TPE) derivatives were synthesised and their aggregation-induced emission (AIE) was evaluated in mixtures of THF/water and MeOH/water. The influence of regiochemistry and length of the chains in the substituents on emissive properties was studied.