Discovery of the thieno[2,3-b][1,4]thiazin-2(3H)-one STING inhibitors [0.03%]
一类噻唑并[2,3-b][1,4]噻嗪酮类STING抑制剂的发现
Lu Han,Shumin Zang,Wenxin Li et al.
Lu Han et al.
The adaptor molecule STING is embedded in the endoplasmic reticulum (ER) membrane. In innate immunity, STING is a critical cascade in regulating the cytoplasmic DNA-recognizing signaling. Aberrant STING signaling facilitates the host body t...
Feifei Wang,Hongxue Dai,Kuanxin Wan et al.
Feifei Wang et al.
CDK12 (Cyclin-dependent kinase 12) is a cyclin-dependent kinase that regulates gene transcription by phosphorylating the C-terminal domain of RNA polymerase II, playing a crucial role in maintaining genomic stability. Mutations or alteratio...
Discovery of monoterpenoid-based benzamides bearing bicyclo[2.2.1]heptane motif as influenza H1N1 virus inhibitors [0.03%]
一类双环[2.2.1]庚烷苯甲酰胺类单萜衍生物抗流感H1N1病毒活性研究
Anastasiya S Sokolova,Valeria V Samsonova,Sergey O Kuranov et al.
Anastasiya S Sokolova et al.
The persistent threat of influenza pandemics and the limitations of existing therapies necessitate the discovery of novel antiviral agents. This study investigates a series of monoterpenoid-based benzamides, derived from natural products (+...
Harnessing N-substituted benzotriazole scaffolds as potent methionine aminopeptidase inhibitors: from chemical design to cellular efficacy [0.03%]
利用苯并三唑衍生物作为强有力的蛋氨酸氨肽酶抑制剂：从化学设计到细胞活性研究
Vivekananda Saha,Ajinur Hossain,Khairud Zaman Miraj et al.
Vivekananda Saha et al.
Herein, we present the synthesis, characterization, and biological evaluation of twenty-five N-substituted benzotriazole derivatives as potential anticancer agents targeting methionine aminopeptidase (MAP) enzymes. The compounds were synthe...
Discovery and characterization of a high-affinity G-quadruplex binding peptide via mRNA display [0.03%]
基于mRNA展示技术的高亲和力G-四链体结合肽的发现与表征
Naka Kudo Ida,Yoshimasa Kawaguchi,Shiroh Futaki et al.
Naka Kudo Ida et al.
G-quadruplexes (G4s) are non-canonical secondary structures of nucleic acids that play crucial roles in gene expression, and their dysregulation has been implicated in various diseases. Therefore, development of G4-binding molecules, includ...
Regio- and Diastereoselective Arylation of rosin acids: A practical strategy for bioactive compounds discovery [0.03%]
松香酸的区域及非对映异构选择性芳基化反应：用于生物活性化合物发现的一种实用策略
Farked S Wahoodi,Antonio Fernández,Juan Sainz et al.
Farked S Wahoodi et al.
A mild, sustainable, and cost-effective arylation of rosin-acids is reported. This new approach, based on a regio- and diastereoselective Friedel-crafts alkylation, enabled the synthesis of fourteen new resin acid derivatives. Selected comp...
Design, synthesis and anti-tumor activities of pyridine-benzamide containing dithiocarbamate moiety as EZH2 inhibitors [0.03%]
含二硫代氨基甲酸盐的吡啶-苯胺类EZH2抑制剂的设计、合成及抗肿瘤活性研究
Hui Lu,Yuling Xiang,Ping Gong
Hui Lu
Based on the reported Enhancer of zeste homolog 2 (EZH2) inhibitors characterized by pyridone-benzamide components, a series of derivatives were designed and synthesized through structural optimization based on rational drug design principl...
Structure-activity relationship study of a new class of 2-amino-3,4-dihydroquinazolines as antitubercular agents [0.03%]
一类新的2-氨基-3，4-二氢喹唑啉类抗结核药物的构效关系研究
Lena Trifonov,Helena I Boshoff,Jose Santinni O Roma et al.
Lena Trifonov et al.
The discovery of novel chemical matter with antitubercular activity that could feed into the tuberculosis (TB) drug discovery pipeline addresses the need to develop novel drugs that inhibit growth of both drug sensitive and drug resistant s...
Novel 7-Substituted-1,2,4-Triazolopyrimidines targeting Nav1.2 channels as low-neurotoxicity antiepileptic agents [0.03%]
一种新型的针对Nav1.2通道的抗癫痫药物：具有低神经毒性的7取代的1,2,4-三唑并嘧啶类化合物
Yuxi Zhou,Weina Wang,Cui Lv et al.
Yuxi Zhou et al.
In pursuit of novel antiepileptic agents with improved safety profiles, a series of novel 7-substituted-[1,2,4]triazolo[1,5-a]pyrimidine derivatives were synthesized and evaluated for antiepileptic activity using the subcutaneous pentylenet...
Computationally guided design of N4-(2-methyl-2H-indazol-6-yl)-N2-phenylpyrimidine-2,4-diamine inhibitors of EGFR kinase targeting Cys797 [0.03%]
计算指导设计EGFR激酶Cys797定点的N4-(2-甲基-2H-吲达唑-6-基)-N2-苯基嘧啶-2,4-二胺抑制剂
Adchata Konsue,Duangkamol Gleeson,Kiattawee Choowongkomon et al.
Adchata Konsue et al.
The epidermal growth factor receptor kinase (EGFR) is a tyrosine kinase (TK) implicated in the uncontrolled growth of non-small cell lung cancer. EGFR-TK inhibitors have been used extensively, however inhibitor resistance often develops lea...