Results 31 to 40 of about 24,681 (243)

Computational modeling of distribution coefficients and their correlations with pharmacokinetic properties of 17α-picolyl and 17(E)-picolinylidene androstane derivatives [PDF]

Acta Periodica Technologica, 2019
The present study describes the computational modeling of distribution coefficient (logD) of 17α-picolyl and 17(E)-picolinylidene androstane derivatives, as a group of compounds with significant anticancer activities.
Kovačević Strahinja Z., Karadžić-Banjac Milica Ž., Podunavac-Kuzmanović Sanja O., Ajduković Jovana J.   +3 more
doaj   +1 more source

A Modular Synthesis of C5‐Sulfenyl Thiazoles via an Intermolecular Pummerer Rearrangement: An Underexplored Scaffold for Medicinal Chemistry

Angewandte Chemie, EarlyView.
Modular access to underexplored C5‐sulfenyl thiazoles via an intermolecular Pummerer rearrangement is reported. The methodology exhibits a broad functional group tolerance enabling the seamless design of trisubstituted thiazole cores bearing a sulfur handle for further elaboration.
Joe L. Smy, Theo C. Webb, Barnaby W. Greenland, S. Mark Roe, John Spencer, Storm Hassell‐Hart   +5 more
wiley   +2 more sources

Preclinical in vitro screening of newly synthesised amidino substituted benzimidazoles and benzothiazoles

Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Newly synthesised benzimidazole/benzotiazole derivatives bearing amidino, namely 3,4,5,6-tetrahydropyrimidin-1-ium chloride, substituents have been evaluated for their potential antitumor activity in vitro.
Livio Racané, Maja Cindrić, Ivo Zlatar, Tatjana Kezele, Astrid Milić, Karmen Brajša, Marijana Hranjec   +6 more
doaj   +1 more source

G2-manifolds and the ADM formalism [PDF]

Differential Geometry and its Applications, 2019
In this paper we study a Hamiltonian function on the cotangent bundle of the space of Riemannian metrics on a 3-manifold $M$ and prove the orbits of the constrained Hamiltonian dynamical system correspond to $G_2$-manifolds foliated by hypersurfaces diffeomorphic to $M\times \mathrm{SO}(3)$.
openaire   +3 more sources

Chemically Regulated STING‐Activating Prodrugs of Deoxyribose Cyclic Dinucleotides Elicit Robust Immune Activation and Durable Antitumor Immunity

Angewandte Chemie, EarlyView.
All three diastereoisomers of an esterase‐sensitive phosphotriester dCDN prodrug demonstrate improved activity. The (Rp,Rp) diastereoisomer shows the highest activity with an EC50 of 1.7 nM in STING activation and displays the most pronounced antitumor activity via intravenous administration, significantly suppressing tumor proliferation, extending the
Zhiqiang Xie, Huimin Liu, Yuchen Yang, Xiaohan Sun, Jingwen Wang, Tianxiang Liu, Baifan Wang, Wenrui Qiu, Yiwen Sun, Yuting Bai, Yao Zhang, Dejun Ma, Rong Xiang, Shibo Li, Zhen Xi   +14 more
wiley   +2 more sources

adm kurikulum

, 2019
Abstrak— the term curriculum administration emphasizes efforts to direct the curriculum so that the curriculum can be implemented appropriately in various educational activities. As is known, the curriculum contains planned activities that will be carried out during the teaching and learning process.
openaire   +5 more sources

Biological evaluation of selected metronidazole derivatives as anti-nitroreductase via in silico approach

Eclética Química, 2022
The 1-(2-hydroxyethyl)-2-methyl-5-nitroimidazole (2HMN) is a powerful antibacterial and antiparasitic drug used alongside other drugs against Helicobacter pylori infection and was investigated the effects of substituents: –OH (A), H (B), –SPh (C), –COOH (
Moriam Dasola Adeoye, Abel Kolawole Oyebamiji, Mojeed Ayoola Ashiru, Rasheed Adewale Adigun, Olabisi Hadijat Olalere, Banjo Semire   +5 more
doaj   +1 more source

An Enzymatic Platform for Late‐Stage (Radio)isotope Labelling of Oligonucleotides With Methyltransferases

Angewandte Chemie, EarlyView.
State‐of‐the‐art synthesis of radiolabelled oligonucleotides involves multi‐step synthesis with high costs, extended timelines and significant radioactive waste generation. Herein, a dual‐methyltransferase platform enables late‐stage, site‐specific labelling, overcoming these limitations through reduced costs, faster turnaround and minimal radioactive ...
Christopher R. B. Swanson, Ulrich Kauhl, Martin R. Edelmann, Florian P. Seebeck   +3 more
wiley   +2 more sources

Application of drug-induced growth rate inhibition and intracellular drug exposures for comprehensive evaluation of cellular drug sensitivity

Scientific Reports
In vitro cellular assays are indispensable tools for preclinical understanding of therapeutic candidates. Herein, we have outlined methods for robust determination of cellular sensitivities by adapting drug-induced growth-rate inhibition analysis ...
Dolonchampa Maji, Malerie Wolke, Shamim Khaja, John P. Savaryn, John C. Kalvass, Gary J. Jenkins   +5 more
doaj   +1 more source

Targeting WDR12 Unleashes T‐Cell‐Mediated Antitumor Activity in Melanoma by Destabilizing CD276

Advanced Science, EarlyView.
WDR12 cooperates with the chaperonin subunit CCT7 to maintain CD276 stability on tumor cells, suppressing T‐cell activity and promoting immune escape. SU14813, a small‐molecule WDR12 inhibitor, reduces CD276 stability and relieves CD276‐mediated T‐cell suppression.
Jie Pan, Ruimin Chang, Meng Zhang, Qian Dong, Guanxiong Zhang, Xiang Chen, Mingliang Chen, Lixia Lu, Xiaowei Liang, Yeye Guo, Juan Su   +10 more
wiley   +1 more source