Design, synthesis, and biological evaluation of selective cytotoxicity-derived Miliusol derivatives inducing profound TNBC regression in vivo [0.03%]
具有选择性细胞毒性的米利索衍生物的设计、合成及生物学评价诱导活体乳腺癌 regressions
Xiaoling Cheng,Weiji Chen,Wenli Hao et al.
Xiaoling Cheng et al.
Triple-negative breast cancer (TNBC) remains a challenging malignancy due to its aggressive nature and lack of targeted therapies. Miliusol, a natural product isolated from Miliusa tenuistipitata, exhibits potent anti-proliferative activity...
Novel Piperine derivatives containing substituted Benzamide fragments: Design, synthesis, anti-breast cancer activity, and mechanistic study on the PI3K/AKT/mTOR pathway [0.03%]
新型含有取代苯胺片段的胡椒碱衍生物：设计、合成、抗乳腺癌活性及PI3K/AKT/mTOR途径作用机制研究
Mengwei Song,Ying Zhou,Sen Wang et al.
Mengwei Song et al.
Breast cancer is the most prevalent malignant tumor among women worldwide, and recurrence, metastasis, and drug resistance remain major challenges that compromise treatment efficacy and patient prognosis. Piperine has been reported to posse...
3-Deoxy-4-sulfonamido-butein derivatives promote cell cycle arrest and apoptosis by inhibiting EGFR/JAK2/STAT3 signaling in A549 lung cancer cells [0.03%]
3-脱氧-4-磺胺基-白杨茋衍生物通过抑制EGFR/JAK2/STAT3信号通路促进A549肺癌细胞周期阻滞和凋亡
Jung Hwan Choi,Hyun-Ha Hwang,Jinwon Hong et al.
Jung Hwan Choi et al.
Butein, a naturally occurring chalcone, exhibits diverse pharmacological potential but suffers from limited anticancer efficacy. To address this limitation and improve drug-likeness, we designed and synthesized a novel series of 3-deoxy-4-s...
Peptide-drug conjugates bearing an antimitotic Ahx-DA1 payload achieve potent antitumor activity in Her2-amplified and EGFR-positive KRAS-mutant cancers in vivo [0.03%]
含抗微管Ahx-DA1载荷的多肽偶联药物在体内HER2扩增和EGFR阳性KRAS突变癌症中表现出有效的抗肿瘤活性
Akash Panja,Pousali Mitra,Iryna Tkachenko et al.
Akash Panja et al.
Peptide-drug conjugates (PDCs) represent a targeted cancer therapy strategy that combines tumor-homing peptides with potent cytotoxic payloads, offering a promising alternative to antibody-drug conjugates (ADCs) through improved tissue pene...
Emerging chemical strategies for CD38 inhibition: restoring NAD+ metabolism and disease control [0.03%]
新兴的CD38抑制化学策略：恢复NAD+代谢和疾病控制
Zeyu Zhang,Arshad J Ansari,Ethan R Fayne et al.
Zeyu Zhang et al.
Cluster of differentiation 38 (CD38) is a multifunctional ectoenzyme regulating immune functions, calcium signaling, and nicotinamide adenine dinucleotide (NAD+) metabolism. Through rapid hydrolytic degradation of NAD+, CD38 drives cellular...
Development and preclinical evaluation of [111In]In-DTPA-EphA2-57-1: a single-photon emission computed tomography probe targeting EphA2-expressing tumors [0.03%]
111In标记的DTPA-EphA2-57-1：一种针对表达EphA2肿瘤的单光子发射计算机断层成像技术探针的研究及临床前评估
Minon Sasaki,Hiroyuki Kimura,Takumi Iwasawa et al.
Minon Sasaki et al.
Erythropoietin-producing hepatocellular receptor A2 (EphA2) is overexpressed in various malignant tumors and represents a promising target for cancer-specific imaging and therapy. However, many therapeutics (as well as imaging probes) targe...
Chemoselective and quantitative detection of acrolein based on pyrene excimer fluorescence via cycloaddition reaction of conjugated imine [0.03%]
基于共轭亚胺的环加成反应定量检测丙烯醛的化学选择性检测新方法
Masayuki Takamatsu,Hiroya Tsuchida,Hinako Nabetani et al.
Masayuki Takamatsu et al.
Acrolein is a highly reactive and toxic aldehyde generated in various biological and environmental contexts, including tobacco combustion and cellular oxidative stress. Herein, we present a novel quantitative method for acrolein detection u...
Design, synthesis, and biological evaluation of Chromene-Phenylpiperazine-Chalcone hybrids as multi-target-directed ligands for the treatment of Alzheimer's disease [0.03%]
基于色烯-苯哌嗪-查尔酮杂环衍生物的多靶点配体设计、合成及其对阿尔茨海默病的作用研究
Yuanxiu Liu,Zhenze Jiang,Die Chen et al.
Yuanxiu Liu et al.
A novel series of chromene-phenylpiperazine-chalcone hybrids was rationally designed, synthesized and evaluated as multi-target-directed ligands (MTDLs) for Alzheimer's disease (AD). Among them, compound 9 s exhibited selective equine serum...
Discovery of 1H-pyrazolo[3,4-d]pyrimidin-4-ylamine derivatives as potent PI3Kδ/BTK dual-target inhibitors for the treatment of B-cell lymphoma [0.03%]
作为B细胞淋巴瘤治疗药物的PI3Kδ/BTK双靶点抑制剂1H-吡唑并[3,4-d]嘧啶-4-胺衍生物的研究与发现
Zunyuan Wang,Yingqiao Ye,Youkun Kang et al.
Zunyuan Wang et al.
B-cell lymphoma (BCL) is a hematological system malignant tumor with a relatively high incidence, and PI3Kδ and BTK play an important role in the development of BCL. In the preliminary investigation, we found that when the PI3K inhibitor a...
Identification of daurioxoisoporphine D and moringamine I as blood-brain barrier-permeable natural inhibitors of amyloid-β aggregation and neuronal toxicity [0.03%]
鉴定可穿透血脑屏障的天然抑制淀粉样蛋白聚集和神经毒性的大牻吲哚异卟啉D和幕尼甘胺I
Hayato Yoshikawa,Emi Yoshida,Takahiro Matsumoto et al.
Hayato Yoshikawa et al.
Early Alzheimer's disease (AD) is characterized by extracellular accumulation of amyloid-β (Aβ) peptides and degeneration of basal forebrain cholinergic neurons. Currently, acetylcholinesterase inhibitors and costly anti-Aβ antibodies ar...