Dipicolinic acid (DPA)-based chelators for zirconium-89 PET imaging applications [0.03%]
基于二吡咯甲烷(DPA)配体的锆-89 PET显像剂的研究进展
Siyuan Ren,Haixing Wang,Yujie Liu et al.
Siyuan Ren et al.
We report the synthesis and evaluation of pyridine-based chelators for 89Zr with applications in positron emission tomography (PET) imaging. A series of pyridine-containing small molecule ligands were screened for spectroscopic Zr(IV) compl...
Synthesis of symmetrical bis(indolyl)methanes via Sc(OTf)3 catalyzed tandem CO and CC bond breaking reaction and their anti-bacterial studies [0.03%]
斯克里奇催化剂串联断碳氧和碳碳反应合成吲哚甲烷类化合物及抗菌活性研究
Nazir Uddin,Sudipta Roy,Rwivoo Baruah et al.
Nazir Uddin et al.
Bis(indolyl)methanes (BIMs) are significant molecular scaffolds comprising nitrogen heterocycles that exhibit notable biological and pharmacological properties. This work represents an alternative and novel method for the synthesis of BIMs ...
Synthesis and biological evaluation of structurally L-shaped carbostyril derivatives with integrated side chains as cyclooxygenase inhibitors [0.03%]
一类新型L型卡伯斯蒂尔衍生物的合成及其抗环氧合酶活性研究
Toshihiko Tashima,Yoshinori Suzuma,Hiroaki Murata et al.
Toshihiko Tashima et al.
In daily life, nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly used drugs that elicit analgesic, antipyretic, anti-inflammatory, and antithrombotic activities. However, gastric ulceration is a serious side effect of these drugs, ...
New salidroside-furoxan hybrids as potential agents inhibit triple-negative breast cancer [0.03%]
新的补骨脂素-硝基苯并恶唑类衍生物作为抑制三阴性乳腺癌的潜在候选药物
Bing Zhang,Yongqing Zhang,Siqi Zhang et al.
Bing Zhang et al.
Salidroside (SAL) is a natural glycoside compound with various biological activities. Recent studies have shown that SAL exhibits certain therapeutic effects on triple-negative breast cancer (TNBC). To enhance the anti-TNBC activity, 15 SAL...
Synthesis and antimicrobial activity mechanism of N-substituted methyl Matrinecarboxylate derivatives [0.03%]
N-甲基马钱素羧酸酯衍生物的合成及抗菌活性机制研究
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%]
一类与靶点共价结合能力增强的雷公藤红素噻唑衍生物的设计、合成及抗肿瘤活性研究
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...