TPE-peptide@CaCO₃ targeting mitochondrial calcium overload and PDT synergistic tumor therapy [0.03%]
用于靶向线粒体钙超载和光动力治疗的TPE-肽@碳酸钙肿瘤协同疗法
Jinrong Chen,Peixuan Zhao,Jiaqi Li et al.
Jinrong Chen et al.
The high mortality rate of cancer necessitates the development of efficient treatments. Here, we developed acid-sensitive CaCO₃ (calcium carbonate) particles loaded with TPE (tetraphenylethylene)-peptide conjugates for mitochondrial target...
Compounds mimicking the Michaelis-Menten transition state of the phosphatidylinositol 4-kinase [0.03%]
模仿磷脂酰肌醇-4-激酶的迈克耳孙-mented过渡态的化合物
Hubert Hřebabecký,Martin Klima,Milan Dejmek et al.
Hubert Hřebabecký et al.
Phosphatidylinositol 4-kinases (PI4Ks) are crucial enzymes in lipid signaling responsible for generating phosphatidylinositol-4-phosphate (PI4P). Although the ATP-binding site of PI4Ks has been extensively studied, the structural characteri...
5,6,7,8-Tetrahydroimidazo[1,2-a]pyrazine-based thiosemicarbazones as anti-Trypanosoma cruzi agents [0.03%]
基于5,6,7,8-四氢咪唑并[1,2-α]吡嗪的噻二唑啉亚胺𬭩化合物作为抗克氏锥虫剂的研究
Marlene Saraiva de Araújo Neta,Maísa Cavalcanti Coelho,Felipe Neves Coutinho et al.
Marlene Saraiva de Araújo Neta et al.
Chagas disease, caused by Trypanosoma cruzi, remains a major neglected tropical disease for which current chemotherapies are limited by toxicity and variable efficacy. In the present work, a new series of 5,6,7,8-tetrahydroimidazo[1,2-a]pyr...
Recent developments in Haspin kinase inhibitors: Structure, synthesis and activities [0.03%]
Haspin激酶抑制剂的研究进展：结构、合成及活性
Killian Malosse,Elisabeth Pereira,Francis Giraud et al.
Killian Malosse et al.
Haspin is an atypical serine/threonine protein kinase involved in the regulation of mitosis progression. In the recent years, significant progress, especially in terms of selectivity, has been achieved in the discovery of Haspin inhibitors....
Design, synthesis and biological evaluation of 2,4,5-trisubstituted 7H-Pyrrolo[2,3-d]pyrimidine derivatives as potent EGFR tyrosine kinase inhibitors against the C797S acquired resistance mutation [0.03%]
设计、合成及生物活性评价2,4,5-三取代的7H-吡咯并[2,3-d]嘧啶类化合物作为有效抑制EGFR C797S继发突变的酪氨酸激酶抑制剂
Hao Zhang,Tianlong Lan,Rui Li et al.
Hao Zhang et al.
The C797S mutation in the epidermal growth factor receptor (EGFR) presents a significant challenge in treating non-small cell lung cancer (NSCLC), as it confers resistance to osimertinib. To tackle this issue, we designed and synthesized no...
Discovery of Hsp70 inhibitors for allosteric dissociation of the Hsp70/BAG3 complex via structure-based de novo design [0.03%]
基于结构的从头设计发现Hsp70异位分解Hsp70 / BAG3复合物的抑制剂
Hang Wang,Tong Ji,Jingjing Liu et al.
Hang Wang et al.
Protein-protein interaction (PPI) with cochaperones could induce conformational changes of Hsp70. The Hsp70/BAG3 PPI shows tumor specificity and could be regarded as potential targets for cancer therapy. In this paper, a de novo structure-b...
Synthesis of new 2-styryl-3-nitroimidazo[1,2-a]pyridine derivatives via base-induced elimination of 2-N-tosyl intermediates and in vitro antileishmanial evaluation [0.03%]
通过碱诱导的N-甲苯磺酰基中间体消除合成新的2-茋-3-硝基咪唑并[1,2-a]吡啶衍生物及其体外抗利什曼原虫活性评价
Inès Jacquet,Caroline Castera-Ducros,Romain Paoli-Lombardo et al.
Inès Jacquet et al.
To explore the antileishmanial structure-activity relationships in a 3-nitroimidazo[1,2-a]pyridine series, we developed a previously undescribed olefination strategy at position 2 via elimination of intermediates bearing an N-tosyl group, g...
Design, synthesis, and evaluation of novel tricyclononene carboxamide derivatives as dual anti-orthopoxvirus and anti-inflammatory agents [0.03%]
新型三环壬烯羧酰胺衍生物的设计、合成与评价作为抗正痘病毒和抗炎剂Dual Anti-Orthopoxvirus And Anti-InflammatoryAgents)
Tengxiao Sun,Wei Zheng,Haiguo Sun et al.
Tengxiao Sun et al.
Orthopoxviruses, particularly the monkeypox virus, can cause acute systemic disease accompanied by excessive inflammatory immune responses, while therapeutic options remain limited. In this study, a series of tricyclononene derivatives were...
Synthesis and anti-tumor activity evaluation of novel chalcone derivatives as potential HDAC6 inhibitors [0.03%]
新型查尔康茋衍生物的合成及其作为HDAC6抑制剂的抗肿瘤活性研究
Xin Ma,Siqi Li,Xinyue Huang et al.
Xin Ma et al.
Histone deacetylase inhibitors (HDACis) are a class of epigenetic drugs that, as the name suggests, inhibit histone deacetylases (HDACs), which are anticancer therapeutic targets. Several studies have investigated hydroxamic acid HDACi. How...
Exploration of a novel series of isoindolinone-based hydroxamate derivatives: Design, synthesis, and evaluation of anticancer activity [0.03%]
基于异靛哚啉𬭩类羟胺酸衍生物抗肿瘤活性研究：设计、合成及评价
Xizheng Quan,Yumei Chen,Fangli Ma et al.
Xizheng Quan et al.
Histone deacetylases (HDACs) have been identified as a class of crucial epigenetic enzymes that are responsible for the removal of acetyl groups from the lysine residues in the amino-terminal tails of histones. Their overexpression is close...