Synthesis and biological evaluation of novel nitrogen-containing heterocyclic derivatives as potential anticancer agents [0.03%]
新型含氮杂环衍生物的合成及其抗肿瘤活性研究
Qiu Li,Minghui Li,Yafang Xiao et al.
Qiu Li et al.
Based on screening results, a series of nitrogen-containing five-membered heterocyclic compounds were designed and synthesized for anticancer evaluation. Among them, 7 s, featuring a 1,2,3-triazole scaffold, exhibited the most potent antipr...
Biochemical investigations into the incorporation of 8-oxo-2'-deoxyguanosine-5'-triphosphate with two A-family polymerases [0.03%]
两种A家族聚合酶掺入8-氧代-2'-脱氧鸟苷三磷酸的生化研究
Michelle L Hamm,Katherine Alexander,Mary W N Burns et al.
Michelle L Hamm et al.
8-Oxo-2'-deoxyguanosine-5'-triphosphate (OdGTP) is a promutagenic oxidatively damaged nucleotide that can base pair to both 2'-deoxycytidine (dC) and 2'-deoxyadenosine (dA) and may play a role in antibiotic initiated bacterial cell death. W...
Design, synthesis and docking study of 1,2,3-triazole incorporated benzoxazole-oxazole derivatives and evaluation as potential anticancer agents [0.03%]
含1,2,3-三氮唑并苯并噁唑-噁唑衍生物的设计、合成与对接研究及其潜在抗肿瘤活性评估
Adurthi Suryakumari,Chithaluri Sudhakar,Bijaya Ketan Sahoo
Adurthi Suryakumari
The study reports the design and synthesis of a new library of triazole in-corporated benzoxazole oxazole compounds (11a-j) and their in vitro cytotoxic activity evaluation. The structural reliability of the synthesized compounds was confir...
Solid-phase synthesis of a pyrrole library and identification of bioactive compounds [0.03%]
固相合成吡咯化合物文库及筛选活性化合物
Sukhyun Lee,Lisa M Eubanks,Kim D Janda
Sukhyun Lee
Pyrrole derivatives represent a privileged scaffold in medicinal chemistry due to their frequent presence in biologically active compounds. Herein, we report the solid-phase synthesis of a combinatorial library consisting of 211 pyrrole der...
Discovery of GLPG4471, a potent and selective IRAK4 inhibitor for the treatment of inflammatory and autoimmune diseases [0.03%]
GLPG4471的发现：一种用于治疗炎症和自身免疫疾病的高效选择性IRAK4抑制剂
Oscar Mammoliti,Florence Bonnaterre,Gregory Newsome et al.
Oscar Mammoliti et al.
Interleukin-1 receptor associated kinase 4 (IRAK4) is a key mediator of the secretion of cytokines and interferons via Toll-like receptor and interleukin-1 receptor signaling pathways. Modulation of IRAK4 activity has been investigated for ...
Study of the reversal of metallo-β-lactamase-mediated resistance in Gram-negative bacteria by EDTMP [0.03%]
乙二醇四甲基磷酸酯逆转革兰阴性菌金属β-内酰胺酶介导耐药性的研究
Chen Wu,Yuzhou Hu,Zouyi Sun et al.
Chen Wu et al.
Metallo-β-lactamases (MBLs) are major causes of carbapenem resistance in Gram-negative bacteria. In this study, a simple and practical method was developed to synthesize the fluorescent probe CE-HF, which was proven effective for detecting...
Novel azabicyclic series of potent SHP2 allosteric inhibitors [0.03%]
一类新型氮杂 bicyclic 口服活性的SHP2别构抑制剂
Alessio Sferrazza,Ilaria Rossetti,Danilo Fabbrini et al.
Alessio Sferrazza et al.
The non-receptor protein tyrosine phosphatase SHP2, encoded by PTPN11, is a critical component of the RAS/RAF/MEK/ERK signaling pathway, functioning upstream of RAS to promote oncogenic signaling and tumor growth. As part of a drug discover...
Design, synthesis and anti-pneumonic activity evaluation of shikonin ester derivatives [0.03%]
设计、合成与肺部作用评价肖今素酯类化合物
Xuelian Shen,Aga Er-Bu,Xiaoxia Liang
Xuelian Shen
Acute lung injury (ALI) is a serious and prevalent clinical condition with limited treatments. Recent research has highlighted the potential of targeting inflammatory pathways as a therapeutic strategy for ALI. In this study, a series of sh...
Discovery of small-molecule modulators of ppGalNAc-T2 targeting the metastable states during its loop-closing process [0.03%]
发现小分子化合物调节物ppGalNAc-T2的作用机制及其在环闭合过程中的亚稳态作用
Danfeng Shi,Xialin Luo,Lu Wang et al.
Danfeng Shi et al.
The polypeptide N-acetyl-galactosaminyltransferase 2 (ppGalNAc-T2) is a promising therapeutic target for metabolic and neurodevelopmental disorders in humans. The atomic-scale insights into metastable states of ppGalNAc-T2 during the loop-c...
Identification of potent and orally bioavailable GSPT1 molecular glue degraders [0.03%]
高效且口服生物利用的GSPT1分子胶降解剂的鉴定
Run-Duo Gao,Wenzhong Liu,Yuanyuan Liu et al.
Run-Duo Gao et al.
G1 to S phase transition 1 (GSPT1) is involved in multiple biological processes and is significantly overexpressed in various cancer tissues and cells. Degradation of GSPT1 protein proves to be a potential therapeutic option through the tec...