Coumarin-dihydropyrimidinone hybrids as promising agents against ovarian cancer: synthesis, SAR, and in silico evaluation [0.03%]
具有香豆素-二氢嘧啶酮结构的杂环化合物作为抗卵巢癌药物的研究：合成，结构活性关系及分子模拟研究
Jhonathan R N Dos Santos,Alice K A Martinez,Saulo H Mendes Abe et al.
Jhonathan R N Dos Santos et al.
The coumarin scaffold is widely recognized for its broad range of biological activities, including antibacterial, anti-HIV, and anticancer properties. In parallel, molecular hybridization has emerged as an effective strategy to enhance biol...
Novel benzothiazole fused iminothiazolines: Design, synthesis, anticancer and antimicrobial profiling with in silico insights [0.03%]
新型苯并噻唑融合亚胺噻唑啉的创新设计、合成及抗肿瘤和抗菌性能研究（含计算机辅助研究）
P M BharathKumar,A C Kumar,Madalambika et al.
P M BharathKumar et al.
A series of novel twenty benzothiazole-fused iminothiazoline derivatives (7aa-7df) were synthesized and evaluated for their invitro anticancer activity and their antimicrobial studies. The structures of the final compounds were confirmed th...
Nitroxoline-O-protected derivatives inhibit MetAP2 and activate ATF4 through mTORC1 to inhibit cancer cell growth [0.03%]
氮卓酮-O保护衍生物通过mTORC1抑制MetAP2和激活ATF4以抑制癌细胞生长
Michael J Williams,Conor T Ronayne,Tanner J Schumacher et al.
Michael J Williams et al.
Reprogrammed cancer cell proliferation requires high levels of protein synthesis and concomitant folding and processing. N-terminal methionine amino peptidases (MetAP) are a class of enzymes that cleave the initiator methionine amino acids ...
Computational modeling-assisted discovery of the structural effects of phenylpropanoid derivatives on intracellular anti-Trypanosoma cruzi activity [0.03%]
计算模型辅助发现苯丙素衍生物对细胞内抗查加斯病原虫活性的结构效应
Matheus L Silva,Henrique Barbosa,Mateus C Silva et al.
Matheus L Silva et al.
Previous investigations have demonstrated that n-hexacosyl p-coumarate, a natural product isolated from the Brazilian plant Baccharis sphenophylla, exhibits activity against the extracellular (trypomastigote) forms of Trypanosoma cruzi. Str...
Discovery of Pyrazolo[1,5-a]pyridine derivatives as potent RET inhibitors for the treatment of human thyroid and lung Cancer [0.03%]
作为人类甲状腺和肺癌治疗的高效RET抑制剂的吡唑并[1,5-a]吡啶衍生物的研究发现
Lin Pan,Yangxiao Hu,Fuxing Tan et al.
Lin Pan et al.
Rearranged during transfection (RET) kinase mutations are frequently observed in the context of human thyroid and lung cancer treatment. Moreover, a considerable amount of effort has been dedicated by the scientific community to the identif...
A glutathione-activated anthraquinone-based photosensitizer for selective photodynamic therapy of cancer cells overexpressing glutathione [0.03%]
一种谷胱甘肽激活的蒽醌基光敏剂选择性杀伤高表达谷胱甘肽的癌细胞
Yuzuha Miyazawa,Daisuke Takahashi,Kazunobu Toshima
Yuzuha Miyazawa
An anthraquinone derivative 2 was found to induce protein degradation under neutral conditions and without additives upon visible light irradiation. Based on this finding, a glutathione (GSH)-activatable photosensitizer 3 was designed and s...
Discovering potent EGFR inhibitors through the structural optimization of the Betti-base scaffold [0.03%]
基于贝蒂骨架的结构优化发现有效的EGFR抑制剂
Xiaotian Xu,Yongbo Wei,Huan He et al.
Xiaotian Xu et al.
EGFR is a critical oncogenic driver in non-small cell lung cancer (NSCLC). However, there are no approved inhibitors for the C797S resistance mutation. Allosteric inhibitors targeting a site near the ATP-binding pocket have emerged as a pro...
Discovery of novel thiophene amide derivatives with potent antibacterial activity [0.03%]
一类具有强抗菌活性的噻吩酰胺衍生物的研究发现
Chengyu Sun,Jiahao Zhang,Furong Yu et al.
Chengyu Sun et al.
The escalating threat of antibiotic resistance has become an urgent issue in global public health, and this study designed and synthesized 28 novel thiophene amide derivatives to address this challenge. In vitro antibacterial activity tests...
The design, synthesis and evaluation of [18F]ASK1-IN-6 as the first Fuorine-18 positron emission tomography radiotracer for ASK1 neuroimaging [0.03%]
设计、合成及评价用于ASK1神经影像学的首个氟[18F]放射性配体[18F]ASK1-IN-6
Yafei Huang,Yongle Wang,Yanli Wang et al.
Yafei Huang et al.
ASK1 is a key regulator in the molecular mechanisms underlying multiple neurological diseases, where it drives oxidative stress, inflammation, and apoptotic pathways. ASK1 has emerged as a potential therapeutic target in a range of neurodeg...
Biosynthetically natural product-conserved scaffolds: Harnessing power with molecular-medicinal strategy for new therapeutic development [0.03%]
利用分子医学策略挖掘生物合成天然产物骨架的治疗潜力
Ayan Acharya,Vaibhav Gupta,Mithilesh Nagpure et al.
Ayan Acharya et al.
This perspective demonstrates a critical analysis of natural products-conserved scaffolds, the molecular architectures that are produced in the common T-point of naturally evolved various biosynthetic pathways. It presents structure and fun...