Synthesis and evaluation of enantiomeric quinoline-2-carboxamides: positron emission tomography imaging agents for the translocator protein [0.03%]
喹啉-2-甲酰胺类对映体的合成与评价：一种针对转运蛋白的正电子发射断层显影剂
Lachlan J N Waddell,Mark G MacAskill,Holly McErlain et al.
Lachlan J N Waddell et al.
The translocator protein (TSPO) is a key biomarker for inflammation. Positron emission tomography (PET) imaging of TSPO has emerged as a valuable tool for investigating multiple disorders throughout the body. We previously reported the deve...
R Rama Suresh,Tuniyazi Abuduani,Mahesh Kasthuri et al.
R Rama Suresh et al.
Prodrug strategies are used to enhance the physicochemical and pharmaceutical properties of drug candidates that may not be suitable for specific delivery or are limited by formulation options. A prodrug derivative is converted into its act...
Stereoselective design of amino acid bioconjugates: targeting strategies and physicochemical optimization [0.03%]
手性氨基酸生物缀合物的结构设计、靶向策略及理化性质优化研究进展
Soma Mandal,Rajat Choudhary,V Badireenath Konkimalla
Soma Mandal
Amino acid conjugates are progressively becoming popular as a potent tactic to enhance the pharmacological efficacy of drugs, especially in the areas of cancer and antimicrobial therapy. By taking advantage of the intrinsic biological attri...
Synthesis, antibacterial activity, and mechanistic characterization of novel 9-substituted berberine derivatives [0.03%]
9-取代小檗碱衍生物的合成、抗菌活性及机制研究
Jiaying Tong,Huamao Yang,Yeying He et al.
Jiaying Tong et al.
Natural products serve as valuable sources for developing antibacterial agents. In this study, 35 berberine derivatives were synthesized, and preliminary screening revealed that most compounds effectively inhibited the growth of Methicillin...
Design and synthesis of sorafenib-inspired benzofuran hybrids as VEGFR-2 inhibitors: antiproliferative evaluation, mechanistic insights, and docking studies in hepatocellular carcinoma [0.03%]
设计并合成索拉非尼衍生物苯并呋喃杂化物作为VEGFR-2抑制剂：肝细胞癌中的抗增殖评价，机理分析和对接研究
Mohamed S Shehda,Aya M Almatary,Mohamed S H Salem et al.
Mohamed S Shehda et al.
Hepatocellular carcinoma (HCC) is a leading cause of cancer-related mortality worldwide owing to its high metastatic potential. Vascular endothelial growth factor receptor-2 (VEGFR-2), a key regulator of angiogenesis and cell proliferation,...
Screening apelin analogues and a small molecule agonist as effective cardiovascular therapeutics against reperfusion injury [0.03%]
筛选出有效的血管内皮生长因子拮抗剂及小分子激动剂以对抗再灌注损伤
Anjalee Wijewardane,Kleinberg X Fernandez,Anran Zhang et al.
Anjalee Wijewardane et al.
Ischemic reperfusion injury is a major global health threat, with the development of effective therapeutics still urgently needed. While both peptide therapeutics and small-molecule agonists have been extensively investigated to treat this ...
Discovery of novel progesterone-heterocyclic conjugates and their encapsulated polymeric nanoparticles as potential CDK8 inhibitors: lung cytotoxicity evaluation, gene expression, and molecular docking [0.03%]
新型孕酮-杂环共轭物及其包封的聚合物纳米粒子作为潜在的CDK8抑制剂的发现：肺细胞毒性评价、基因表达和分子对接研究
Yasmin Y Omar,Ghada F Elmasry,Dina S El-Kady et al.
Yasmin Y Omar et al.
CDK8 is overexpressed in many cancers and represents a potential target for developing new anticancer agents. To identify promising antineoplastic compounds as CDK8 inhibitors, progesterone-heterocyclic conjugates were synthesized through m...
Harnessing biological insights to accelerate drug discovery against ESKAPE pathogens [0.03%]
利用生物学见解加速对抗ESKAPE病原体的药物发现
Tashi Palmo,Vishwani Jamwal,Diksha Kumari et al.
Tashi Palmo et al.
The escalating global health crisis of antimicrobial resistance (AMR) is driven by the increasing prevalence of drug-resistant bacterial infections, particularly among ESKAPE pathogens. These multidrug-resistant bacteria pose a significant ...
Integrin-specific binding macrocyclic RGD peptides functionalized with dinitrophenol as multivalent antibody-recruiting molecules to enhance cytotoxicity in cancer immunotherapy [0.03%]
一种整合素特异性结合的环状RGD肽，以二硝基苯酚为臂架实现多价招募抗体的作用，增强癌症免疫治疗中的细胞毒性作用
Xiaozhong Cheng,Chenrui Hu,Wanru Gao et al.
Xiaozhong Cheng et al.
The diverse expression of antigenic subtypes on tumor cells can substantially influence the specific binding and tumor cytotoxicity of antibody-recruiting molecules (ARMs). Therefore, the development of multivalent ARMs with high selectivit...
LLDT-8 attenuates brain metastasis in non-small cell lung cancer via selective p53 activation [0.03%]
LLDT-8通过选择性激活p53抑制非小细胞肺癌脑转移
Junjie Liu,Lun Liang,Zhenning Wang et al.
Junjie Liu et al.
Brain metastasis (BM) remains a leading cause of mortality in non-small cell lung cancer (NSCLC) owing to inadequate blood-brain barrier (BBB) penetration and therapy resistance. Here, we developed a brain-tropic A549-BrM2 subline that reca...