Discovery of new 5-substituted-indole-2-carboxamides as dual epidermal growth factor receptor (EGFR)/cyclin dependent kinase-2 (CDK2) inhibitors with potent antiproliferative action [0.03%]
一类新的5位取代的吲哚-2-羧酸胺类化合物作为表皮生长因子受体（EGFR）和周期蛋白依赖性激酶2（CDK2）抑制剂的研究及其抗增殖活性研究
Fatma A M Mohamed,Saleha Y M Alakilli,Eman Fawzy El Azab et al.
Fatma A M Mohamed et al.
A new series of 5-substituted-3-ethylindole-2-carboxamides 5a-k and 6a-c was designed and synthesised in an attempt to develop a dual targeted antiproliferative agent. Various spectroscopic methods of analysis were used to confirm the struc...
Multi-target antibacterial mechanism of ruthenium polypyridine complexes with anthraquinone groups against Staphylococcus aureus [0.03%]
含蒽醌基钌聚吡啶复合物的多靶点抗菌机制研究——以金黄色葡萄球菌为模型菌种
Li Jiang,Yuanyuan Ma,Yiman Chen et al.
Li Jiang et al.
Three new Ru(ii) complexes, [Ru(dtb)2PPAD](PF6)2 (Ru-1), [Ru(dmob)2PPAD](PF6)2 (Ru-2) and [Ru(bpy)2PPAD](PF6)2 (Ru-3) (dtb = 4,4'-di-tert-butyl-2,2'-bipyridine, dmob = 4,4'-dimethyl-2,2'-bipyridine, bpy = 2,2'-bipyridine and PPAD = 2-(pyrid...
Reactive fragments targeting carboxylate residues employing direct to biology, high-throughput chemistry [0.03%]
用于直接生物化学的高通量化学的靶向羧基残基的反应片段
Ross P Thomas,Emma K Grant,Eleanor R Dickinson et al.
Ross P Thomas et al.
The screening of covalent or 'reactive' fragment libraries against proteins is becoming an integral approach in hit identification, enabling the development of targeted covalent inhibitors and tools. To date, reactive fragment screening has...
Synthesis and anti-proliferative activity of dehydroabietinol derivatives bearing a triazole moiety [0.03%]
含三氮唑结构的松香烷醇衍生物的合成及抗肿瘤活性研究
Mingjun Zhu,Jinchuan Sun,Yaju Wu et al.
Mingjun Zhu et al.
In search of more efficacious antitumor agents, a series of novel dehydroabietinol derivatives containing a triazole moiety was synthesized, and evaluated for cytotoxicity against four human cancer cell lines. Many exhibited superior cytoto...
Peptide-based positron emission tomography probes: current strategies for synthesis and radiolabelling [0.03%]
基于肽的正电子发射断层显像探针：合成及放射性标记的最新策略
Mariacristina Failla,Giuseppe Floresta,Vincenzo Abbate
Mariacristina Failla
In medical imaging, techniques such as magnetic resonance imaging, contrast-enhanced computerized tomography, and positron emission tomography (PET) are extensively available and routinely used for disease diagnosis and treatment. Peptide-b...
Development of thiazole-appended novel hydrazones as a new class of α-amylase inhibitors with anticancer assets: an in silico and in vitro approach [0.03%]
新型噻唑并杂芳酰腙类α-淀粉酶抑制剂的开发及其体内外抗肿瘤活性研究
Sandhya Chahal,Jyoti Punia,Payal Rani et al.
Sandhya Chahal et al.
Hyperamylasemia is reported to be associated with numerous chronic diseases, including diabetes and cancer. Considering this fact, we developed a series of thiazole-clubbed hydrazones. The derivatives were explored for their in vitro α-amy...
Inhibition of mitochondrial metabolism by (-)-jerantinine A: synthesis and biological studies in triple-negative breast cancer cells [0.03%]
(-)-jerantinine A通过抑制代谢过程来抑制三阴性乳腺癌细胞中的线粒体呼吸：合成及生物研究
Timothy L Gialelis,Zifei Wang,Joshua A Homer et al.
Timothy L Gialelis et al.
A concise semi-synthesis of the Aspidosperma alkaloids, (-)-jerantinine A and (-)-melodinine P, and derivatives thereof, is reported. The novel compounds were shown to have potent activity against MDA-MB-231 triple-negative breast cancer ce...
Design, synthesis and evaluation of the anti-breast cancer activity of 1,3-oxazolo[4,5- d]pyrimidine and 1,3-oxazolo[5,4- d]pyrimidine derivatives [0.03%]
1,3-氧杂螺[4,5-d]嘧啶和1,3-氧杂螺[5,4-d]嘧啶衍生物的设计、合成及抗乳腺癌活性评价
Yevheniia Velihina,Raey Gesese,Victor Zhirnov et al.
Yevheniia Velihina et al.
A series of 1,3-oxazolo[4,5-d]pyrimidine and 1,3-oxazolo[5,4-d]pyrimidine derivatives were synthesized and functionalized in this study. The obtained compounds were tested against breast cancer cell lines of the NCI subpanel, followed by fu...
Ribosome-targeting antibiotics and resistance via ribosomal RNA methylation [0.03%]
核糖体靶向抗生素及通过核糖体RNA甲基化介导的抗性机制
Learnmore Jeremia,Benjamin E Deprez,Debayan Dey et al.
Learnmore Jeremia et al.
The rise of multidrug-resistant bacterial infections is a cause of global concern. There is an urgent need to both revitalize antibacterial agents that are ineffective due to resistance while concurrently developing new antibiotics with nov...
Computational design of a cyclic peptide that inhibits the CTLA4 immune checkpoint [0.03%]
计算设计一种可抑制CTLA4免疫检查点的环形肽类药物
Ravindra Thakkar,Deepa Upreti,Susumu Ishiguro et al.
Ravindra Thakkar et al.
Proteins involved in immune checkpoint pathways, such as CTLA4, PD1, and PD-L1, have become important targets for cancer immunotherapy; however, development of small molecule drugs targeting these pathways has proven difficult due to the na...