In vitro and in vivo studies of dehydroxylated-isoquines and -isotebuquines against trypanosomatids: a preclinical drug candidate for treatment of cutaneous leishmaniasis [0.03%]
脱羟基-异喹啉和-异泰布喹啉的体内外研究对抗利什曼原虫：治疗皮肤利什曼病的临床前药物候选物
Angel H Romero,Elva Serna,Elena Aguilera et al.
Angel H Romero et al.
The 4-aminoquinoline scaffold represents a promising platform for designing anti-trypanosomatid agents targeting essential survival pathways in Leishmania and T. cruzi. Herein we demonstrated the potential of the dehydroxylated isoquines (d...
PROTAC approaches against drug-resistant EGFRC797S/L858R/T790M mutants: biological evaluation and SAR studies (2020-2025) [0.03%]
针对药物耐药的EGFR C797S/L858R/T790M突变体的PROTAC方法：生物评估及构效关系研究（2020-2025）
Ankush Kumar,Vishakha Sharma,Pallvi Kumari et al.
Ankush Kumar et al.
The development of epidermal growth factor receptor (EGFR) C797S/L858R/T790M mutation has become a major barrier to tyrosine kinase inhibitors (TKIs). These mutations reduce the drug binding and increase the adenosine triphosphate (ATP) com...
Design, synthesis, and biological evaluation of X19: a matrine pyrazole derivatives therapeutic candidate [0.03%]
X19的设计、合成及生物活性评价：一种苦参碱吡唑类衍生物候选药物
Tingguo Xu,Suyi Dai,Zhouxing Hu et al.
Tingguo Xu et al.
A series of novel matrine-pyrazole derivatives were designed and synthesized through structural modification of the natural alkaloid matrine to enhance its antitumor efficacy. Among these derivatives, compound X19 was identified as the most...
Emerging strategies for Alzheimer's disease: leveraging flavonoid derivatives for early diagnosis and neuroprotection [0.03%]
阿尔茨海默病新兴策略——利用黄酮衍生物进行早期诊断和神经保护
Zhe Han,Wenling Fu,Mingjuan Dai et al.
Zhe Han et al.
Alzheimer's disease (AD) is a prevalent chronic and progressive neurodegenerative disorder predominantly affecting the elderly population. The etiology of AD is multifaceted, and despite extensive research, effective therapeutic options rem...
Antibacterial peptidomimetics via fragment display on small-molecule scaffolds [0.03%]
基于小分子支架的抗菌肽模拟物片段展示技术
Emma Dyhr,Lucía Cañete de Pinedo,Nicki Frederiksen et al.
Emma Dyhr et al.
In response to the growing threat of antimicrobial resistance, scaffold-based peptidomimetics were explored as potential antibacterial agents. This innovative design approach involved fragment display on small-molecule scaffolds of ultrasho...
Design, synthesis and exploration of cyclic imides as PDE4 inhibitors in psoriasis [0.03%]
环状酰亚胺类PDE4抑制剂的抗银屑病活性研究与发展
Veena K S,Pallabi Panja,Tirtha Nath et al.
Veena K S et al.
Psoriasis is a chronic inflammatory skin disorder for which effective oral therapies remain inadequate. Selectively targeting PDE4B has attracted interest as a promising therapeutic target because it modulates inflammatory pathways and offe...
Discovery of novel coumarin amphiphiles: dual-action antimicrobials with bacteria-mediated biofilm disruption and host-directed immunomodulation [0.03%]
新型香豆素两亲化合物的发现：具有细菌介导生物膜破坏和宿主定向免疫调节的双重作用抗菌剂
Haiyang Zhang,Qun Tang,Qian Zhu et al.
Haiyang Zhang et al.
Bacterial infections pose a threat to the health of animals and humans, and biofilm formation exacerbates the microbial threat. Therefore, new antimicrobial agents to address this challenge are much needed. In this study, some new amphipath...
Synthesis and evaluation of 14β-acyl substituted 17-cyclopropylmethyl-7,8-dihydromorphinone derivatives: mixed partial agonists at mu opioid and nociception/orphanin FQ peptide receptors [0.03%]
14β-酰基取代的17-环丙甲基-7,8-二氢吗喃酮衍生物的设计、合成及药理学评价：μ阿片受体和伤害性/孤儿肽受体的部分激动剂混合物
Mehrnoosh Ostovar,Keith Olsen,Gerta Cami-Kobeci et al.
Mehrnoosh Ostovar et al.
Opioids remain the standard of care for management of severe pain, but adverse effects limit their use, particularly for the treatment of chronic pain. Compounds that have dual partial agonist activity at mu opioid (MOP) and nociceptin opio...
Harnessing oligonucleotide architecture for potent multivalent inhibition of human carbonic anhydrases [0.03%]
用于有效抑制人源碳酸酐酶的寡核苷酸多价抑制剂的设计与合成
Eslam M Abbass,Federico Ladu,Justine Mansot et al.
Eslam M Abbass et al.
This study presents the design and synthesis of a novel class of carbonic anhydrase inhibitors (CAIs) using oligonucleotides as an original multivalent platform. Single-stranded oligonucleotides bearing one to four terminal alkyne moieties ...
A halogenated pregnenolone analogue suppresses HepG2 proliferation and induces apoptosis via PPARγ regulation [0.03%]
卤代孕烯醇酮类似物通过PPARγ调节抑制HepG2增殖并诱导凋亡
Shi-Ying Xu,Quan-Xing Liu,Yan Luo et al.
Shi-Ying Xu et al.
The broad biological activity of synthetic halogenated steroid derivatives has spurred considerable recent research. In this study, we synthesized and evaluated cytotoxicity against HepG2 cells for twenty-eight halogen-containing pregnenolo...