Targeting SIRT6: the design and therapeutic implications of activators and inhibitors [0.03%]
靶向SIRT6：活化剂和抑制剂的设计及治疗意义
Yuxin Shi,Xiaofan Han,Xinqi Li et al.
Yuxin Shi et al.
Sirtuin 6 (SIRT6) is an NAD+-dependent deacylase that maintains genomic stability, regulates metabolism, and influences aging, making it an attractive but challenging therapeutic target. Pharmacological modulation of SIRT6 holds promise for...
PSMA binding of carbamate-containing peptidomimetics influenced by side chain length and stereocenter configuration in preclinical prostate cancer model [0.03%]
碳水化合物肽模拟物的侧链长度和立体中心构型对PSMA结合在前列腺癌前期模型中的影响
Áron Roxin,Helen Merkens,Chengcheng Zhang et al.
Áron Roxin et al.
To explore how core backbone modifications influence prostate-specific membrane antigen (PSMA) targeting, we synthesized a series of novel peptidomimetics replacing the classic urea linkage of established radiotracers with a carbamate funct...
Phenotypic discovery of a pyrimidine derivative with dual anti-prostate cancer and cardioprotective potential via ROS modulation [0.03%]
一种兼具抗前列腺癌和心肌保护活性的嘧啶衍生物的表型发现及其调节ROS潜能的研究
Yaquan Cao,Yaxi Wu,Yunfei Li et al.
Yaquan Cao et al.
Cardiotoxicity remains a major limitation of current anticancer therapies, highlighting the need for agents that combine antitumor efficacy with intrinsic cardiac safety. Phenotypic screening of a pyrimidine-based compound library identifie...
Cationic amino acid-engineered radiopeptides for breast cancer targeting [0.03%]
用于乳腺癌靶向的阳离子氨基酸工程标记肽
Akanksha Jain,Manoj Kumar,R Vasumathy et al.
Akanksha Jain et al.
G-protein coupled estrogen receptors (GPER) represent clinically important target for detection and treatment of breast cancer owing to their high expression. Present study aimed to incorporate and determine the influence of cationic amino ...
Design, synthesis and biological evaluation of triazolo[1,5-a]pyrimidinone derivatives as potent and orally efficacious WRN helicase inhibitors for MSI cancer therapy [0.03%]
一类高效口服活性WRN解旋酶抑制剂的三唑并吡啶酮衍生物的设计、合成及生物评价研究用于MSI阳性肿瘤治疗
Yi Xiong,Hao Jiang,Jiayin Zhang et al.
Yi Xiong et al.
Microsatellite instability-high (MSI-H) cancers represent an unmet clinical need due to treatment resistance, and WRN helicase is a validated synthetic lethal target for this indication. Herein, we rationally designed, synthesized, and biol...
Design, synthesis and antiviral activity of ciclopirox (CPX) analogs against orthopoxvirus [0.03%]
环吡酮（CPX）类似物的设计、合成及正痘病毒抗病毒活性研究
D M Nirosh Udayanga,Ziyue Wang,Anil Pant et al.
D M Nirosh Udayanga et al.
In search for structurally novel antiviral leads against orthopoxvirus, we have previously identified and characterized ciclopirox (CPX) as a strong antiviral hit inhibiting vaccinia virus (VACV) replication. We report herein the antiviral ...
Novel benzofuran-1,3,4-thiadiazole aryl urea hybrids as dual VEGFR-2/BRAF inhibitors: anticancer activity, apoptosis induction, and molecular modeling studies [0.03%]
新型苯并呋喃-1,3,4-噻二唑芳基脲杂化物作为VEGFR-2 / BRAF双重抑制剂：抗肿瘤活性，诱导细胞凋亡和分子建模研究
Marwa I Serag,Mohamed R Elnagar,Wafaa A Ewes et al.
Marwa I Serag et al.
The development of dual-directed anticancer agents has emerged as an effective strategy to simultaneously modulate tumor proliferation and angiogenesis while overcoming resistance associated with single-target therapies. In the present stud...
Design, synthesis and antitubercular evaluation of 2,5-disubstituted 1,3,4-oxadiazoles bearing a 3,5-dinitrophenyl pharmacophore [0.03%]
含3,5-二硝基苯药效团单环三氮唑并[4,3-b]吡啶的合成及抗结核活性研究
Václav Pflégr,Jiřina Stolaříková,Enikő Šikorová et al.
Václav Pflégr et al.
Tuberculosis (TB) continues to demand new chemotypes able to overcome acquired drug-resistance. Here, we designed and synthesized two related series of twenty 3,5-dinitrophenyl-based 1,2-diacylhydrazines and their cyclic analogues, 2,5-disu...
Rational design, synthesis, and evaluation of acridone-peptide based antimicrobial and Antifolate agents against methicilin-resistant Staphylococcus aureus, Bacillus subtilis and dihydrofolate reductase [0.03%]
合理设计、合成及评估抗甲氧西林金黄色葡萄球菌、枯草芽孢杆菌和二氢叶酸还原酶的吖啶酮-肽类抗菌与抗二氢叶酸化合物
Sombir Jaglan,Palwinder Singh,Varinder Kaur et al.
Sombir Jaglan et al.
To conquer the antimicrobial resistance, here, we developed acridone-peptide based DHFR inhibitors. Small peptides or amino acids are coupled with acid acridone either through amide linkage or via an azole-based linker. These hybrids exerte...
Structure-based identification of novel indole-fused polycyclic derivatives as potent acetylcholinesterase inhibitors [0.03%]
基于结构的新型并吲哚多环衍生物作为乙酰胆碱酯酶抑制剂的研究
Wenbin Chen,Keyu Zhan,Chenrui Xu et al.
Wenbin Chen et al.
The pathogenesis of Alzheimer's disease (AD) is closely associated with cholinergic neuronal impairment, which is induced by excessive degradation of acetylcholine (ACh) mediated by acetylcholinesterase (AChE). In this study, a series of no...