Exploration of Fluorinated Pyrazolidine-3,5-Diones for Positron Emission Tomography Imaging of the P2Y12 Receptor in the Central Nervous System [0.03%]
中枢神经系统P2Y12受体正电子发射断层成像的含氟吡唑啶-3,5-二酮的研究
E Johanna L Stéen,Anne van der Schatte Olivier,Berend van der Wildt et al.
E Johanna L Stéen et al.
The purinergic receptor P2Y12 (P2Y12R) has emerged as a promising biomarker for selectively imaging the anti-inflammatory phenotype of microglia. Developing positron emission tomography (PET) tracers for this target is an active area of res...
Cytotoxic, Antibacterial, and in Silico Pks13 Inhibitory Properties of Indole-Coupled Dihydrobenzo[c]phenanthridines [0.03%]
吲哚偶联二氢苯并菲啶类生物碱的细胞毒、抗菌及基于分子对接的抗PKS13抑制活性研究
Reyna Martha Gallegos-Alvarado,Adriana Romo-Pérez,Luis Demetrio Miranda et al.
Reyna Martha Gallegos-Alvarado et al.
The indoles and benzo[c]phenanthridines have attracted much interest as potential anticancer and antibacterial agents. Herein, the synthesis and bioactivity of new and known indole-coupled dihydrobenzo[c]phenanthridines are reported. Among ...
Development of Dual Aurora-A and Aurora-B Degrading PROTACs for MCYN-Amplified Neuroblastoma [0.03%]
开发用于MCYN扩增的神经母细胞瘤的双重Aurora-A和Aurora-B降解PROTACs
Sydney E Nelson,James R Tucker,Madelen G Prado et al.
Sydney E Nelson et al.
In neuroblastoma, MCYN amplification is associated with survival rates of
Structure-Based Drug Design of Novel Heterocyclic Scaffolds as TgCDPK1 Inhibitors [0.03%]
基于结构的药物设计新型杂环支架作为TgCDPK1抑制剂
Anoopjit Singh Kooner,Mariah Norman,Igi Vilza et al.
Anoopjit Singh Kooner et al.
Toxoplasmosis is caused by the protozoan parasite Toxoplasma gondii and poses grave health concern for immunocompromised patients. T. gondii has a family of calcium dependent protein kinases (CDPKs) that control a variety of critical proces...
Kunal Madaan,Ram Singh
Kunal Madaan
Isoindolin-1-one scaffolds have emerged as privileged structures in medicinal and synthetic chemistry due to their diverse biological activities and synthetic accessibility. This review comprehensively highlights the recent advancements in ...
Design, Synthesis, and Antiproliferative and Apoptotic Assessment of Triazole-Tethered Bisnaphthalimide-Isatin Hybrids on Triple-Negative Breast and Prostate Cancers [0.03%]
三氮唑连接的双萘胺-异丁酰 hybrids 的设计、合成及三阴性乳腺癌和前列腺癌的抗增殖和凋亡作用评估
Preeti,Asif Raza,Garima Arora et al.
Preeti et al.
This study reports the design, synthesis, and biological evaluation of 1H-1,2,3-triazole-tethered bisnaphthalimide-isatin hybrids as potential antiproliferative agents. The compounds are efficiently synthesized via copper-promoted azide-alk...
A Short Peptide Inhibitor of Measles Virus Fusion Protein that Exhibits Passive Membrane Permeability [0.03%]
一种具有被动膜通透性的短肽类融合蛋白抑制剂：对麻疹病毒的作用
Ziwei Gao,Jiei Sasaki,Tateki Suzuki et al.
Ziwei Gao et al.
In this study, a passively membrane-permeable short peptide inhibitor targeting the measles virus fusion protein (MeV-F) is reported. Measles virus (MeV) is highly contagious, yet no approved antiviral drugs are currently available. MeV-F p...
Unveiling Benzoxazole-Substituted Thiazolyl-Pyrazole Derivatives Inducing Apoptosis by Targeting β-Tubulin and Caspase-3 [0.03%]
一种通过靶向β-微管和Caspase-3诱导凋亡的苯并恶唑取代的噻唑基吡唑衍生物
Burak Kuzu,Mustafa Cakir,Eda Acikgoz et al.
Burak Kuzu et al.
In the present study, the biological activities of novel compounds (BP-1 to BP-6), designed as antitubulin agents, were systematically evaluated, with a particular focus on their effects on the triple-negative breast cancer cell line MDA-MB...
Xuanming Teng,Jingyi Yang,Zhiyi Ren et al.
Xuanming Teng et al.
Proteolysis targeting chimera (PROTAC) technology holds great promise as a protein degradation modality in therapeutic development. However, there remain challenges, including complex chemical synthesis and linker screening. To address this...