Decoding Structural Fingerprints to Design and Elucidate the Mechanism of Action of Prospective Cholesteryl Ester Transfer Protein Drugs [0.03%]
解码结构指纹设计并阐明预期卵磷脂胆固醇酰基转移酶药物的作用机制
Sudipta Nandi,Sanjib Senapati
Sudipta Nandi
Cardiovascular diseases (CVDs) have become a leading cause of deaths globally. Recent studies have shown that increasing the level of high-density lipoproteins (HDL) is one of the potential avenues to halt CVD progression. This could be ach...
pH-Responsive Nanoscale Mixed Ligand Metal Organic Framework as a Carrier for Photosensitizer in Targeted Antibacterial Photodynamic Therapy [0.03%]
一种用于靶向抗菌光动力治疗的pH响应型纳米混合配体金属有机框架载敏剂体系
Fathima Fasna P H,Sreesha Sasi,Hareesh N Ramanathan et al.
Fathima Fasna P H et al.
The escalating multidrug-resistant bacterial infections underscore the urgent need for alternatives to conventional antibiotics. Antimicrobial photodynamic therapy emerges as a promising strategy, leveraging light-activated photosensitizers...
Benzoxazole-Acrylonitriles: Dual Bioactivity and DNA Binding from a Sustainable Synthetic Approach [0.03%]
苯并恶唑-丙烯腈的合成：可持续合成策略与双重生物活性及DNA结合性质研究
Marina Galić,Tamara Rohtek,Leentje Persoons et al.
Marina Galić et al.
Efficient synthesis in aqueous media is employed to prepare targeted compounds to evaluate antiproliferative, antibacterial, and antiviral activity in vitro. The biological activity is influenced by the type and number of substituents place...
New Structure Activity Relationship Insight into the Role of the C-3 Extension on Rifamycin Antimycobacterial Activity [0.03%]
里法霉素C-3延长结构与抗结核活性的关系研究
Clinton G L Veale,Ewelina Smolarz,Aleksandra Leśniewska et al.
Clinton G L Veale et al.
Herein, the antimycobacterial screening of a series of rifamycin analogues, modified at their C-3 extension, is reported. Overall, these compounds display potent activity against a wild-type Mtb strain assayed in three different growth medi...
Synthesis of Caerulomycins E and A Analogs for Studying Cytotoxic Activity [0.03%]
卡瑞olutein素E和A类似物的合成及其细胞毒活性研究
Pansachon Intamalee,Jesada Maneewong,Natthiya Saehlim et al.
Pansachon Intamalee et al.
Caerulomycin A, a marine-derived natural product featuring a bipyridinic core and a substituted oxime functional group, was originally isolated from Streptomyces caeruleus and is known for its antibiotic, antifungal, and cytotoxic propertie...
AgamOBP1-Directed Discovery of Repellents to Control the Spread of Mosquito-Borne Diseases [0.03%]
新型驱蚊剂的发现及其对防控蚊媒传染病的潜在应用
Evanthia Chazapi,Eftichia Kritsi,Constantinos Potamitis et al.
Evanthia Chazapi et al.
Toward the discovery of novel efficient repellents, protein-directed dynamic combinatorial chemistry (pdDCC) coupled to saturation-transfer difference (STD) NMR spectroscopy was initially employed to identify modulators of the malaria vecto...
5-Amino-7-Oxo-4,7-Dihydroazolo[1,5-a]pyrimidine-6-Carbonitriles: Synthesis and Study of Antitumor Effect In Vitro and In Silico [0.03%]
5-氨基-7-氧代-4,7-二氢-1,5-苯并二氮杂卓-6-腈：合成及体内外抗肿瘤效果研究
Veronika V Dolgova,Konstantin V Savateev,Grigoriy V Urakov et al.
Veronika V Dolgova et al.
A novel chemotype of nitrile-containing azolopyrimidines with potential antitumor activity has been proposed, and a method for the synthesis of the corresponding 5-amino-7-oxoazolo[1,5-a]pyrimidine-6-carbonitriles by cyclocondensation of va...
Christina L L Chai
Christina L L Chai
Drug discovery and development is a complex, arduous and uncertain activity that is more likely to fail than succeed. To improve the odds of success, numerous dogmas have become entrenched in medicinal chemistry. This has unwittingly led to...
Next-Generation Bcl-2 Inhibitors: Design and Evaluation of Indolyl-Triazole Derivatives with Anticancer Potential [0.03%]
下一代Bcl-2抑制剂的设计与评价：具有抗癌潜力的吲哚三唑衍生物
Ahmed M Almehdi,Samar Damiati,Ihsan A Shehadi et al.
Ahmed M Almehdi et al.
The Bcl-2 protein family plays a critical role in regulating apoptosis, making it a key target for cancer therapy. In this study, a series of novel Bcl-2 inhibitors have been designed, synthesized, and evaluated. To disrupt the interactions...
Development of a Partial Proteolysis Targeting Chimera Library Based on Achiral Cereblon E3 Ligase Ligands and its Application for Bruton's Tyrosine Kinase Degraders [0.03%]
基于无手性 cereblon e3 激酶底物的蛋白质酶体靶向嵌合体库的开发及其在布鲁顿酪氨酸激酶降解中的应用
Chelsi M Almodóvar-Rivera,Ira Tandon,Ramesh Mudududdla et al.
Chelsi M Almodóvar-Rivera et al.
Proteolysis targeting chimeras (PROTACs) offer a promising therapeutic approach by leveraging the ubiquitin-proteasome system (UPS) to degrade target proteins. These heterobifunctional molecules consist of a target protein ligand, an E3 lig...