Chlorophenylpyrazolone derivatives as novel PD-L1-targeted inhibitors of the PD-1/PD-L1 immune checkpoint [0.03%]
氯苯基吡唑酮衍生物作为新型PD-L1靶向抑制剂以针对PD-1/PD-L1免疫检查点反应
Frédérique Klupsch,Raphaël Le Biannic,Hassiba El Bouazzati et al.
Frédérique Klupsch et al.
Immune checkpoint inhibitors have emerged as one of the most promising approaches for cancer immunotherapy. Several injectable monoclonal antibodies targeting the programmed cell death-1/programmed cell death-ligand 1 (PD-1/PD-L1) pathway a...
A simple solid-phase approach for the synthesis of DOTA-conjugated α-ketoamide-based fibroblast activation protein-targeted ligands [0.03%]
一种简单固相合成DOTA偶联的以α-酮胺为基础的纤维活化蛋白靶向配体的方法
Shireen Jozi,Pauline Ng,Helen Merkens et al.
Shireen Jozi et al.
Several studies have shown that fibroblast activation protein (FAP)-targeted radioligands with an α-ketoamide as the warhead can lead to high affinity for FAP and prolonged tumor retention. However, the preparation of reported FAP-targeted...
Design, synthesis and antibacterial evaluation of novel unsaturated butenolide-fatty amine hybrids against multidrug-resistant pathogens [0.03%]
新型不饱和丁内酯-脂肪胺衍生物的抗菌设计、合成及评价对抗多重耐药病原体的影响
Su-Yun Tang,Yue-Ping Wang,Ding-Mei Qin et al.
Su-Yun Tang et al.
To address the growing public health challenge of multidrug-resistant bacterial infections, 26 new butenolide amides bearing fatty chains of different lengths (CnH2n+1, n = 4-16) were designed and synthesized and evaluated for their antibac...
Design and synthesis of trolline derivatives with Nrf2 pathway-associated anti-inflammatory activity [0.03%]
Nrf2通路相关抗炎活性的没食子儿茶素类似物的设计与合成
Bill Zhereng Liao,Qi-Mei Tan,Ya-Lin Li et al.
Bill Zhereng Liao et al.
Activation of nuclear factor erythroid-2-related factor 2 (NRF2) has been proven to be an effective means to prevent the development of inflammatory diseases. In this study, series of trolline derivatives (4 -25) were designed and synthesiz...
Synthesis and preliminary enzymatic evaluation of polyol-based 4-phenylbutyrate derivatives [0.03%]
基于多元醇的4-苯基丁酸衍生物的合成及初步酶解评价
Laura Suchetti,Tomas C Tempesti,Carlos Ferrayoli
Laura Suchetti
4-Phenylbutyric acid (4-PBA) is clinically used for the treatment of urea cycle disorders and has attracted increasing attention due to its ability to modulate endoplasmic reticulum stress through its dual function as a chemical chaperone a...
Chemo-enzymatic synthesis of G1-monoacrylate and derived amphiphiles with β-thiopropionate ester linker for drug delivery applications [0.03%]
用于药物输送的G1单丙烯酸及其含有β-硫代丙酸酯连接臂的衍生物两亲分子的化学生物学合成方法
Pooja Kumari,Sumit Kumar
Pooja Kumari
pH-labile linkers have garnered significant attention in biomedical applications, particularly in designing the stimuli-responsive carriers for targeted drug delivery systems. In the present work, we have synthesized G1-monoacrylate from G1...
New thiazole-biaryls as small molecule immunomodulators (SMIs) targeting PD-1/PD-L1 axis [0.03%]
新型噻唑联芳类免疫调节小分子化合物(SMIs)PD-1/PD-L1轴靶向作用研究
Swapnanjali Karamtoth,Maresha Ramakrishna,Swapnil Anil Sule et al.
Swapnanjali Karamtoth et al.
Immune Checkpoint Inhibitors (ICIs) targeting the PD-1/PD-L1 axis have improved the clinical outcomes and revolutionized oncology treatment. However, monoclonal antibody (mAb)-based ICIs are limited by high production and treatment cost, po...
Design, synthesis, and biological evaluation of 1H-1,2,4-triazole-3-carboxamides as apelin receptor agonists [0.03%]
作为阿皮林受体激动剂的1H-1,2,4-三唑-3-甲酰胺的设计、合成及生物学评价
Chong Shen,Yan Zhou,Xinlong Shen et al.
Chong Shen et al.
The apelin receptor (AplnR) is a prominent peptide-binding Class A G protein-coupled receptor (GPCR) involved in the regulation of cardiovascular, gastrointestinal, and immune functions, as well as skeletal development. Activation of the Ap...
Biological evaluation of guanidines, bisguanidines, and their derivatives as anti-Trypanosoma cruzi agents [0.03%]
胍类、双功能化的胍类及其衍生物作为抗查加斯病药物的活性评价研究
Angela Mesías-Salazar,Benjamin Nogueda-Torres,Rogelio Gómez et al.
Angela Mesías-Salazar et al.
Chagas disease remains a major public health concern, and the limited efficacy and safety of current therapies underscore the need for new antitrypanosomal agents. In this study, a series of guanidine and bisguanidine derivatives were evalu...
Multifunctional quinoline-based hydrazones as promising antidiabetic agents: experimental and computational insights [0.03%]
具有多重功能的喹啉类化合物肼腙作为有潜力的抗糖尿病药物：实验和计算分析
Aditi Kalakwade,Rohini S Kavalapure,Shankar Gharge et al.
Aditi Kalakwade et al.
A new library of quinoline-based hydrazone analogues (7a-7j) was designed and synthesized to evaluate their potential as multifunctional antidiabetic agents. In contrast to earlier quinoline derivatives primarily developed for single-enzyme...