Synthesis and antimicrobial activity mechanism of N-substituted methyl Matrinecarboxylate derivatives [0.03%]
Yaoli Fan,Meiyan Jiang,Jing Hu et al.
Yaoli Fan et al.
To address the crisis of multidrug-resistant microbial infections, this study used matrine, a natural product, as the lead compound to design and synthesize a series of novel N-substituted methyl matrinecarboxylate derivatives. Antimicrobia...
Design, synthesis and antitumor activity of celastrol thiazole derivatives with enhanced covalent binding capacity [0.03%]
Siqi Zhang,Maoshan Zhang,Bing Zhang et al.
Siqi Zhang et al.
Celastrol (CEL), a natural product, has attracted great attention because of its remarkable antitumor potential. Its unique quinone methide (QM) moiety covalently binds to the thiol groups of cysteine residues, thereby exerting antitumor ac...
Design, synthesis, and anti-tumor evaluation of indolin-2-one derivatives based on 3D-QSAR [0.03%]
基于三维定量结构活性关系的吲哚啉-2-酮衍生物的设计、合成及抗肿瘤评价
Xingdan Wang,Liying Zhang,Ziqi He et al.
Xingdan Wang et al.
Tropomyosin receptor kinase (TRK) plays a critical role in tumorigenesis, and its aberrant activation is strongly implicated in cancer progression and metastasis. In this study, a series of novel indoline-2-one derivatives were designed and...
Optimization of pyridopyrimidinedione derivatives as non-covalent SARS-CoV-2 3CL protease inhibitors [0.03%]
用于非共价抑制SARS-CoV-2 3CL蛋白酶的吡啶并[1,2-a]嘧啶二酮衍生物优化研究
Yoshiyuki Taoda,Keiichiro Hirai,Shuichi Sugiyama et al.
Yoshiyuki Taoda et al.
COVID-19, an infectious disease caused by SARS-CoV-2, first identified in Wuhan, China, in 2019 and rapidly spread around the world. In response to this worldwide crisis, the research and development of antiviral drugs advanced together wit...
Design, synthesis, and biological evaluation of pyridine-triazole derivatives as URAT1 inhibitors with potential application in hyperuricemia and gout [0.03%]
设计、合成及生物活性评估新的尿酸转运蛋白1抑制剂用于高尿酸血症和痛风治疗
Yujiao Hu,Wei Liu,Ruikang Sun et al.
Yujiao Hu et al.
Hyperuricemia is a major risk factor for gout and is closely associated with metabolic and cardiovascular disorders. Urate-lowering drugs targeting the urate transporter 1 (URAT1) represent an effective therapeutic strategy; however, the cl...
Fluorescent-labeled anti-inflammatory α-galactosylceramide derivative and its intracellular behavior associated with selective immune function [0.03%]
荧光标记的抗炎α-半乳糖基 ceramide 衍生物及其与选择性免疫功能相关的细胞内行为研究
Shunya Kikuchi,Takanori Matsumaru,Yukari Fujimoto
Shunya Kikuchi
The immune activity is markedly modulated by glycolipid antigens through CD1d-dependent recognition, with the glycolipid antigen-CD1d complex recognition and selective cytokine induction of NKT cells. In this study, we developed a novel and...
Aryl-functionalized mono- and diketone curcumin derivatives inhibit SARS-CoV-2 Spike:ACE2 interactions [0.03%]
芳基功能化单二酮姜黄素衍生物可抑制SARS-CoV-2刺突蛋白与ACE2的相互作用
Jeremiah Gabriel G Africa,Kyra Danielle C Magdato,Monissa C Paderes
Jeremiah Gabriel G Africa
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) initiates viral entry through binding of its spike (S) protein receptor-binding domain (RBD) with the human angiotensin-converting enzyme 2 (ACE2). Curcumin, a turmeric-derived cu...
Ferrocenyl substitution turns valproate into a glutamate decarboxylase inhibitor [0.03%]
铁ocene取代将丙戊酸转变为谷氨酸脱羧酶抑制剂
Danijela N Nikolić,Marija S Genčić,Biljana Arsić et al.
Danijela N Nikolić et al.
2-(Ferrocenylmethyl)pentanoic acid (Fc-VPA), a ferrocenyl analog of valproic acid (VPA), was synthesized, fully characterized and its effect on glutamate decarboxylase (GAD) evaluated in mouse brain homogenates using an HPLC assay. Fc-VPA p...
Optimization of 68Ga-DOTA radiolabeling conditions for disulfide-directed multicyclic peptides and amphiphilic antimicrobial peptides [0.03%]
用于二硫键导向的多环肽和两亲性抗菌肽的68Ga-DOTA标记条件优化
Xueyao Chen,Siqi Zhang,Shuo Jiang et al.
Xueyao Chen et al.
Gallium-68 labeled peptide radiotracers have attracted significant attention in positron emission tomography (PET) imaging of various diseases. While 68Ga-DOTA radiolabeling protocols are well-established, two classes of peptides, disulfide...
Design, synthesis, and Lead optimization of novel Quinazoline-based FLT3 inhibitors with potent anti-acute myelogenous leukemia activity [0.03%]
具有抗急性髓系白血病活性的新型喹唑啉FLT3抑制剂的设计、合成及成药性优化研究
Wei Liu,Shuaibo Du,Miaomiao Wang et al.
Wei Liu et al.
FLT3 mutations, including internal tandem duplications (ITD) and tyrosine kinase domain (TKD) variants, are key drivers of acute myeloid leukemia (AML) and represent attractive therapeutic targets. Guided by a scaffold-hopping strategy base...