Disrupting melanin transfer: innovative strategy for anti-pigmentation drug discovery [0.03%]
干扰黑色素转移：抗色素沉着药物发现的创新策略
Xiaotian Niu,Jia Zhi,Meiling Feng et al.
Xiaotian Niu et al.
The excessive synthesis of melanin leads to skin hyperpigmentation. While tyrosinase activity inhibition has demonstrated efficacy in ameliorating hyperpigmentation, its effectiveness remains limited, and tyrosinase inhibitors may induce ir...
Exploring diarylheptanoid derivatives to target LIMK1 as potential agents against colorectal cancer [0.03%]
探索茋庚烷类衍生物靶向LIMK1作为潜在的结直肠癌作用剂
Liang-Chieh Chen,Tung-Cheng Chang,Hui-Ju Tseng et al.
Liang-Chieh Chen et al.
LIMK1 has been demonstrated to be highly correlated with the progression and overall survival rates of colorectal cancer (CRC) patients. In this study, a series of diarylheptanoid scaffold derivatives were intentionally designed and synthes...
Discovery of benzyl carbamate inhibitors of coronavirus Mpro enzymes from a legacy collection of cysteine protease inhibitors [0.03%]
从半胱氨酸蛋白酶抑制剂老药新用化合物库中发现苯甲基碳酰胺类冠状病毒Mpro酶抑制剂
Mateus Sá Magalhães Serafim,Thales Kronenberger,Karol R Francisco et al.
Mateus Sá Magalhães Serafim et al.
The constant emergence of SARS-CoV-2 resistance drives the search for new antivirals. We screened the SARS-CoV-2 cysteine proteases, the main protease (Mpro) and papain-like protease (PLpro), with 141 peptidyl and peptidomimetic inhibitors ...
Novel compounds with promising HuH-7 inhibitory activity as new cancer drug candidates: derivatives of N,N'-diphenylurea linked with 1,2,3-triazole [0.03%]
具有抗癌活性的新型联有1,2,3-三唑的N,N'-二苯基脲衍生物类化合物：作为新的癌症药物候选物对HuH-7的抑制作用研究
Yajie Guo,Huibao Long,Haoying Zhang et al.
Yajie Guo et al.
Targeted cancer drug therapy has emerged as a critical treatment modality for advanced hepatocellular carcinoma (HCC). The discovery and development of novel anti-HCC drug therapeutics with improved pharmacological properties remains an urg...
Synthesis of novel pyrazole derivatives and neuroprotective effect investigation [0.03%]
新型吡唑衍生物的合成及神经保护作用研究
Aihua Feng,Qing Zeng,Jun Wang et al.
Aihua Feng et al.
Spinal cord injuries (SCIs) cause irreversible damage and lasting neurological impairments. Current treatments are limited to surgical and pharmaceutical interventions, underscoring the need for novel agents. In this study, 27 novel pyrazol...
Design, synthesis, and evaluation of 1, 3-dioxo- N- phenylisoindoline-5-carboxamide derivatives as potent reversible inhibitors of human monoamine oxidase B with neuroprotective properties [0.03%]
一类新型可逆的人Monoamine氧化酶B抑制剂的设计、合成及生物活性研究
Mengxue Mu,Yu Zhang,Bo Wang et al.
Mengxue Mu et al.
A series of 1, 3-dioxo-N-phenylisoindoline-5-carboxamide derivatives were designed, synthesised and evaluated as potent human monoamine oxidase B (hMAO-B) inhibitors with neuroprotective properties. The structure-activity relationship (SAR)...
Structure-based identification of a non-covalent thioredoxin reductase inhibitor with proven ADMET suitability [0.03%]
基于结构的非共价型硫氧还蛋白还原酶抑制剂筛选及人体内药代动力学研究
Giuseppe Lamanna,Giuseppa Augello,Luisa Ronga et al.
Giuseppe Lamanna et al.
Thioredoxin reductase 1 (TrxR1), a selenoprotein enzyme crucial for redox homeostasis in mammals, has emerged as a promising target for anticancer therapy. In this study, we present a non-covalent TrxR1 inhibitor, identified through an inte...
Harnessing coumarin-thio(seleno)cyanate conjugates: potent In vivo antiproliferative agents targeting carbonic anhydrases [0.03%]
苦马豆素-噻(硒)腈酸共轭物：靶向碳酸酐酶的体内抗增殖剂
Silvia Alejandra Meza-Ireta,Laura L Romero-Hernández,Paloma Begines et al.
Silvia Alejandra Meza-Ireta et al.
We synthesised coumarin-based derivatives bearing thio- and selenocyanates to selectively inhibit tumour-associated carbonic anhydrases (CAs) IX and XII and to exert antiproliferative effects on tumour cells. Structural variations included ...
Identification of a novel and high-affinity cyclic peptide targeting Keap1 for inflammation treatment by a combined virtual screening strategy [0.03%]
结合虚拟筛选策略识别新颖高效的Keap1靶向环肽用于抗炎治疗
Shenglin Gao,Xiaokai Shi,Shudan Yang et al.
Shenglin Gao et al.
Inhibition of the Keap1-Nrf2 protein-protein interaction with cyclic peptides represents an attractive strategy to treat inflammation. However, the cyclic peptides for this inhibition are constrained by their low affinity. In this study, th...
Discovery of flavonoids as potent inhibitors of CYP1A to alleviate cellular inflammation and oxidative stress induced by benzo[a]pyrene-induced high CYP1A expression [0.03%]
黄酮类化合物作为CYP1A强效抑制剂的发现以缓解苯并[a]芘诱导的CYP1A高表达引起的细胞炎症和氧化应激
Xiao-Dong Li,Nan-Shan Ma,Ci-Ye He et al.
Xiao-Dong Li et al.
The environmental pollutant benzo[a]pyrene (BaP) can induce cytochrome P450 family 1 subfamily A (CYP1A) or generate metabolic products that disrupt the balance of oxidative stress, triggering inflammatory responses in the lungs and leading...