Design, characterization and evaluation of a new 99mTc-labeled folate derivative with affinity towards folate receptor [0.03%]
一种新型放射性核素99mTc标记的叶酸衍生物的设计、表征及评价：一种亲和力结合叶酸受体的新方法
Soumen Das,Navin Sakhare,Dheeraj Kumar et al.
Soumen Das et al.
Folate receptors (FRs) are known to be over-expressed in several human malignancies and therefore serve as an important target for small radiolabeled folate derivatives for non-invasive imaging of tumor, which is an important tool for futur...
Synthesis, in vitro cytotoxicity evaluation and mechanism of 5' monosubstituted chalcone derivatives as antitumor agents [0.03%]
5'-单取代查尔康衍生物的合成、体外抗肿瘤活性评价及机制探讨
Xueping Xu,Jinjin Wang,Baozhang Yan et al.
Xueping Xu et al.
A series of 5' monosubstituted chalcone derivatives were synthesized to explore their antitumor activity and mechanism of action in vitro. The structures of 5' monosubstituted chalcone derivatives synthesized by reactions such as Suzuki cou...
Discovery of 3-phenyl-1,2,4-oxadiazole derivatives as a new class of SARS-CoV-2 main protease inhibitors [0.03%]
作为一类新的SARS-CoV-2主要蛋白酶抑制剂的3-苯基-1,2,4-噁二唑衍生物的发现
Nihong Guo,Chong Huang,Jingxin Qiao et al.
Nihong Guo et al.
The ongoing COVID-19 pandemic has led to massive infections and deaths and caused tremendous grief among the people. Although vaccines have played an important role in fighting COVID-19, the situation that the protective effect of current v...
Discovery of a brain-sparing GIRK1/4 inhibitor for pharmacological cardioversion of atrial fibrillation [0.03%]
发现脑安全的GIRK1/4抑制剂用于房颤的药物复律
Stefan Peukert,Hatice Belgin Gulgeze Efthymiou,Ruowei Mo et al.
Stefan Peukert et al.
Atrial fibrillation (AF) is the most common cardiac arrhythmia, and a significant risk factor for ischemic stroke and heart failure. Marketed anti-arrhythmic drugs can restore sinus rhythm, but with limited efficacy and significant toxiciti...
Design, synthesis and biological evaluation of novel N-(methyl-d3) pyridazine-3-carboxamide derivatives as TYK2 inhibitors [0.03%]
新型N-(甲基-d3)吡啶酰胺TYK2抑制剂的设计、合成及生物活性评价
Fei Liu,Bin Wang,Yanlong Liu et al.
Fei Liu et al.
As a mediator of pro-inflammatory cytokines, TYK2 is an attractive target to treat autoimmunity diseases. Herein, we reported the design, synthesis, and structure-activity relationships (SARs) of N-(methyl-d3) pyridazine-3-carboxamide deriv...
20S proteasome hydrolysis of LLVY substrates to determine preferences for moieties in its primed substrate channel [0.03%]
20S蛋白酶体底物LLVY的水解产物决定了其识别底物通道中残基偏好的机制
Christine S Muli,Darci J Trader
Christine S Muli
The proteasome is an essential multi-catalytic enzyme in cells that is responsible for degrading proteins with a ubiquitin-dependent or -independent mechanism. Many activity-based probes, inhibitors, and stimulators have been developed to s...
Dioncophyllidine E: The first configurationally semi-stable, 7,3'-coupled naphthyldihydroisoquinoline alkaloid, from Ancistrocladus abbreviatus, with antiausterity activity against PANC-1 human pancreatic cancer cells [0.03%]
来自缩果乌素藤的Dioncophyllidine E：首例构型半稳定的7，3'-偶联萘啶二氢异喹啉生物碱及其对PANC-1人胰腺癌细胞的抗奢侈化学生长活性
Shaimaa Fayez,Alessia Cacciatore,Juthamart Maneenet et al.
Shaimaa Fayez et al.
The discovery of a new naphthylisoquinoline alkaloid, dioncophyllidine E (4), from the tropical liana Ancistrocladus abbreviatus (Ancistrocladaceae) is described. Due to its rare 7,3'-coupling type, combined with the lack of an oxygen funct...
Discovery and anti-tumor activity of 4-(benzylamino)-6-(3,5-dimethylisoxazol-4-yl)quinolin-2(1H)-one (CG13250), a potent, selective and orally bioavailable BET bromodomain inhibitor [0.03%]
一种有效的、选择性的、可口服的BET溴结构域抑制剂CG13250（4-[苯基氨基]-6-[3,5-二甲基异噁唑-4-基]喹啉-2(1H)-酮）的发现及其抗肿瘤活性
Jay Chauhan,Makoto Yoshioka,Sarah Pogash et al.
Jay Chauhan et al.
The bromodomain and extra-terminal domain (BET) proteins are epigenetic readers involved in the regulation of gene transcription. Inhibitors of the BET proteins, in particular BRD4, have demonstrated anti-tumour activities and efficacies in...
2- and 3-Fluoro-3-deaza-1',6'-isoneplanocin: Synthesis and antiviral properties (including Ebola and Marburg) [0.03%]
2-和3-氟-3-脱氮-1',6'-异neplanocin：合成及其抗病毒性质（包括埃博拉和马堡病毒）
Chong Liu,Qi Chen,Stewart W Schneller
Chong Liu
To extend the antiviral properties of 2- and 3-fluoro-3-deazaneplanocins into the evolving 3-deaza-1',6'-isoneplanocin library, 2- (11) and 3-fluoro-1',6'-iso-3-deazaneplanocin A (12) have been explored. The requisite synthesis began with a...
Design, synthesis, and antitumor evaluation of morpholine substituted bisnaphthalimides as DNA targeting agents [0.03%]
设计、合成及生物评估新的DNA靶向抗肿瘤药物双萘胺类化合物及其构效关系研究
Xiao-Man Chen,Jian-Yu Zhou,Shuang-Qiang Liu et al.
Xiao-Man Chen et al.
A series of mono- and bisnaphthalimides derivatives containing 3-nitro and 4-morpholine moieties were designed, synthesized, and evaluated for their in vitro anticancer activities against four cancer cell lines. Some compounds exhibited rel...