Design, synthesis and biological evaluation of novel CDK8/BRD4 dual inhibitors [0.03%]
新型CDK8/BRD4双靶点抑制剂的设计、合成及生物活性评价
Guoao Liang,Xiaochu Zhang,Jiayi Zhu et al.
Guoao Liang et al.
CDK8 is recognized as an important therapeutic target in colorectal cancer. Recently, a study has demonstrated that inhibition of CDK8 alone can activate a compensatory BRD4 signaling pathway, which may account for the modest in vivo effica...
Identification of a novel aβ-overlapping binding site on the TREM2 Ectodomain engaged by the small-molecule agonist VG-3927 [0.03%]
鉴定出一个新颖的Aβ重叠结合位点位于TREM2细胞外区并被小分子激动剂VG-3927占据
Sungwoo Cho,Moustafa T Gabr
Sungwoo Cho
Triggering receptor expressed on myeloid cells 2 (TREM2) is a microglial immune receptor genetically and functionally linked to Alzheimer's disease (AD). VG-3927, the first small-molecule TREM2 agonist to enter clinical development, has bee...
Synthesis of two indole cyanine scaffolds and evaluation of their nucleic acid-associated near-infrared imaging performance [0.03%]
两种吲哚氰系支架的合成及其核酸相关近红外成像性能评估
Wanting Su,Die Sun,Yongquan Wei et al.
Wanting Su et al.
To compare the performance of asymmetric pentamethine cyanines and squaraine-based indole cyanines in nucleic acid imaging, six indole cyanine derivatives were designed, synthesized, and evaluated. T3 which possesses a benz[e]indole termina...
NO-donating Bergenin derivatives with enhanced anti-inflammatory activity [0.03%]
具有增强的抗炎活性的NO供体 Bergenin 衍生物
Enshang Yuan,Qi Deng,Na Li et al.
Enshang Yuan et al.
Ten new nitric oxide (NO)-donating Bergenin derivatives were designed, synthesized, and evaluated for their anti-inflammatory activity. Distinguished by its superior safety profile, a single furoxan moiety conjugated hybrid I8 was selected ...
A facile one-pot synthesis to access unique benzopyranonyl cyanopyrimidinols with multitargeting potential against resistant bacteria [0.03%]
一种简便的一锅法合成独特的苯并吡喃酮氰基嘧啶醇类化合物以对抗耐药细菌多功能靶向的潜在方法研究
Ping-Ping Duan,Li Wang,Zhen-Zhen Li et al.
Ping-Ping Duan et al.
To combat rising antimicrobial resistance, a class of novel cyanopyrimidinols (CPOs) were designed and synthesized via a three-component one-pot reaction strategy. Several prepared CPOs exhibited strong antibacterial activity against the te...
Design, synthesis, and biological evaluation of BODIPY-based photoactivatable Crizotinib prodrugs for precision cancer therapy [0.03%]
基于BODIPY的Crizotinib光激活前药的设计、合成及生物活性评价用于精准癌症治疗
Chuang Xu,Peiying Lu,Mingze Qin et al.
Chuang Xu et al.
Crizotinib is an established first-line therapy for patients with anaplastic lymphoma kinase (ALK)-positive advanced non-small cell lung cancer (NSCLC). However, long-term treatment is often associated with systemic toxicity, leading to var...
A rapid and scalable microwave-assisted strategy for the synthesis of neocryptolepine and its analogues: Comprehensive bioactivity profiling [0.03%]
一种用于合成neo-隐绿碱及其类似物的快速且可扩展的微波辅助策略：综合生物活性谱分析
Siddhi Salgaonkar,Melita Rebello,Delicia Avilla Barretto et al.
Siddhi Salgaonkar et al.
A rapid synthesis of neocryptolepine and its analogues have been developed using 2-Bromo-1H-indole-3-carbaldehydes and N-methylanilines as starting materials under microwave irradiation. A total of 14 different 5-methyl-5H-indolo[2,3-b]quin...
Cannabidiol-thiosemicarbazone exhibits dual tyrosinase inhibition and antioxidant activity in human skin-derived cells [0.03%]
大麻二酚半卡巴腙对人类皮肤细胞系中酪氨酸酶的双重抑制及抗氧化作用
Maytal Shabat-Simon,Oriyan Cohen,Larisa Yaval et al.
Maytal Shabat-Simon et al.
The search for modulators of melanogenesis with improved biological compatibility remains an active area of investigation, as existing tyrosinase (TYR) inhibitors are often limited by low potency, instability, or cytotoxicity. Here, we inve...
Small molecule inhibition of CPSF3 may impact R-loop distribution and abundance [0.03%]
小分子抑制CPSF3可能会影响R环的分布和丰度
Cristina R Hofman,Victor Tse,Jiaxin Hu et al.
Cristina R Hofman et al.
R-loops are three-stranded nucleic acid structures consisting of an RNA/DNA hybrid and a displaced strand of DNA. These structures have been implicated in a variety of regulatory cellular processes. Their untimed or excess accumulation, how...
Disulfide bond formation between Cys22 and Cys44 in SARS-CoV-2 main protease [0.03%]
SARS-CoV-2主要蛋白酶中半胱氨酸22和半胱氨酸44之间二硫键的形成
Lauren R Blankenship,Kai Yang,Chia-Chuan Dean Cho et al.
Lauren R Blankenship et al.
SARS-CoV-2 main protease (MPro) is a cysteine enzyme essential for viral replication and pathogenesis. It contains multiple cysteines that are susceptible to covalent modifications. Reported modifications include inhibitor-derived modificat...