Results 61 to 70 of about 1,937,826 (232)

Thinking Outside the Binding Site: A Self‐Encapsulating Kinase Inhibitor Remodels Its Pocket to Achieve Selectivity

Angewandte Chemie International Edition, EarlyView.
To make exceptionally effective drugs, thinking “outside the binding site” is required. This work reveals that counterintuitive targeting of a kinase‐conserved region can lead to highly selective binding. Inhibitor discovery coupled to x‐ray crystallography shows that a network of noncanonical interactions and long‐range effects of distant unique amino
Nico J. Seidler, Monica R. MacDonald, Athina A. Moschopoulou, Sahba Cunningham, Tess M. Weber, Nader N. Nasief, Lorenz Mayer, Frederik W. Hacker, Ekaterina Hermann, Mareike B. Möllers, Yuliia Skliarenko, Tahereh Damghani, Abid N. Manzar, Kaly S. Lin, Ramona Rudalska, Marcia I. Goettert, Lars Zender, Daniel Dauch, Michael Forster, Stefan A. Laufer, David E. Heppner   +20 more
wiley   +1 more source

Synthesis and Antibacterial Activity of a Novel Series of Potent DNA Gyrase Inhibitors. Pyrazole Derivatives

, 2016
We have previously found that a pyrazole derivative 1 possesses antibacterial activity and inhibitory activity against DNA gyrase and topoisomerase IV.
Mika Fujimoto (2713765), Masaaki Wachi (352707), Keiko Ofuji (2713762), Akihiko Tanitame (2713750), Hideaki Ito (2713756), Yoshihiro Oyamada (2713759), Noritaka Iwai (664205), Motoji Kawasaki (2713768), Hideo Terauchi (1546195), Kazuo Nagai (2713753), Jun-ichi Yamagishi (2713771), Yoichi Hiyama (2713747), Kenji Suzuki (157178)   +12 more
core   +1 more source

Evaluation of 3,5-Diphenyl-2-Pyrazolines for Antimitotic Activity by Inhibition of Tubulin Polymerization

Journal of Chemistry, 2022
Chalcones have a skeleton of diphenyls connected via an α,β-unsaturated carbonyl group. Many chalcone derivatives have been shown to interact with tubulin. Based on previous reports, chalcones derived by substitution of a carbonyl group with 2-pyrazoline
Soon Young Shin, Euitaek Jung, Young Han Lee, Yoongho Lim, Seunghyun Ahn, Dongsoo Koh   +5 more
doaj   +1 more source

A Functional Link between Store-operated and TRPC Channels Revealed by the 3,5-Bis(trifluoromethyl)pyrazole Derivative, BTP2*

Journal of Biological Chemistry, 2005
The coupling between receptor-mediated Ca2+ store release and the activation of “store-operated” Ca2+ entry channels is an important but so far poorly understood mechanism.
Li-Ping He, Thamara Hewavitharana, J. Soboloff, M. Spassova, D. Gill   +4 more
semanticscholar   +1 more source

Data_Sheet_5_Development of 1,5-Diaryl-Pyrazole-3-Formate Analogs as Antifungal Pesticides and Their Application in Controlling Peanut Stem Rot Disease.PDF

, 2022
Stem rot disease caused by Sclerotium rolfsii is one of the destructive diseases in peanut and poses a big risk to peanut production. Current fungicides in the market have not provided satisfactory control efficacy and thus called for novel fungicides ...
Junhuai Zu (11897600), Guangyu Qin (11897597), Jun Yang (2084), Yihui Ma (10522205), Dangwei Yang (11897594)   +4 more
core   +1 more source

UTILITY OF 2- HYDRAZIN04,6 DIMETHYLPYRIMIDINE IN HETEROCY CLIC SYNTHESIS

Zagazig Journal of Pharmaceutical Sciences, 1997
2-Hydrazino-4,6-dimethy1pyridine (1) readily underwent ring closure with benzoy1 chloride to give 5,7 dimethy1-3-pheny1-1,2,4-triazolo[4,3,-a]pyrimidine (4a). Either N-benzoyl derivative (2) or the hydrazone (3a) can be used for the formation of compound
Mohamed AL Ashmawy , Zakaria Abd El-Samii , Said El-Feky , Nermin Osman   +3 more
doaj   +1 more source

Extending Peptide Ligation to Acidic pH and Junctions Comprising Glycosylated and Phosphorylated Amino Acids

Angewandte Chemie International Edition, EarlyView.
A pyridine‐containing ligation auxiliary eliminates a major bottleneck of peptide ligation chemistry. The extended range of applicable pH values (2.0–7.5) in the ligation reaction helps to avoid epimerization. Native chemical ligation (NCL) proceeds at virtually any junction, including reactions at β‐branched amino acids, as well as O‐glycosylated or O‐
Sebastian Trunschke, Antonia Feida, Hendrik Hanebrink, Arseniy Galashov, Alina Herfort, Oliver Seitz   +5 more
wiley   +1 more source

Image_1_PCW-1001, a Novel Pyrazole Derivative, Exerts Antitumor and Radio-Sensitizing Activities in Breast Cancer.tif

, 2022
As pyrazole and its derivatives have a wide range of biological activities, including anticancer activity, the design of novel pyrazole derivatives has emerged as an important research field.
Kwan-Young Jung (1621513), Jiyeon Ahn (624498), Ah-Young Kim (531209), Kyu Myung Lee (6185675), Sangwook Wu (8352264), Suk Joon Cho (12314645), Young-Ju Kwon (3445073), Jae-Sung Kim (605888), Navin Pandit (12314642), Jeong Su Oh (2802904), Minsung Kang (6458120)   +10 more
core   +1 more source

Antiviral activity of pyrazole derivatives bearing a hydroxyquinoline scaffold against SARS-CoV-2, HCoV-229E, MERS-CoV, and IBV propagation

RSC Advances
The ongoing global threat posed by coronaviruses necessitates the urgent development of effective antiviral agents. In this study, we investigated the potential of hydroxyquinoline-pyrazole candidates as antiviral agents against a range of coronaviruses,
Alaa R. I. Morsy, Sara H Mahmoud, Noura M Abou Shama, Walaa Arafa, Gehad A. Yousef, A. A. Khalil, S. K. Ramadan   +6 more
semanticscholar   +1 more source

Accelerating green heterocyclic synthesis: Convergence of AI, automation, and sustainable chemistry

Bulletin of the Korean Chemical Society, EarlyView.
Green heterocyclic synthesis and data‐driven tools such as AI, high‐throughput experimentation, continuous flow, and self‐driving laboratories have developed largely in parallel. This review connects them and asks how green metrics such as E‐factor and PMI might serve as explicit optimization targets rather than post‐hoc measures, toward sustainable ...
Noor Aisyah Ahmad Shah, Amirreza Mottafegh, Su‐Hyun Yoo, Jongwoon Kim, Minseon Byeon, Juhwan Noh, Yea‐Lee Lee, Jin Suk Myung, Gwang‐Noh Ahn   +8 more
wiley   +1 more source