The Carbonic Anhydrase IX inhibitor SLC-0111 as emerging agent against the mesenchymal stem cell-derived pro-survival effects on melanoma cells [0.03%]
碳酐酶IX抑制剂SLC-0111有望成为针对间充质干细胞衍生促黑色素瘤细胞存活效应的新型药物
Silvia Peppicelli,Elena Andreucci,Jessica Ruzzolini et al.
Silvia Peppicelli et al.
Mesenchymal stem cells (MSC) take part to solid tumour-associated stroma and critically influence progression of malignancy. Our study represents a striking example of melanoma progression to a more malignant and resistant phenotype promote...
Oxy-imino saccharidic derivatives as a new structural class of aldose reductase inhibitors endowed with anti-oxidant activity [0.03%]
一类具有抗氧化活性的新型糖脎类醛糖还原酶抑制剂
Felicia D&#x;Andrea,Stefania Sartini,Ilaria Piano et al.
Felicia D&#x;Andrea et al.
Aldose reductase is a key enzyme in the development of long term diabetic complications and its inhibition represents a viable therapeutic solution for people affected by these pathologies. Therefore, the search for effective aldose reducta...
Repurposing strategies on pyridazinone-based series by pharmacophore- and structure-driven screening [0.03%]
基于药效团和结构的筛选再利用吡啶并嗪酮类化合物系列的新策略研究
Giuseppe Floresta,Letizia Crocetti,Maria Paola Giovannoni et al.
Giuseppe Floresta et al.
We report here in silico repurposing studies on 52 new pyridazinone-based small-molecules through inverse virtual screening (iVS) methodologies. These analogues were originally designed as formyl peptide receptor (FPR) ligands. As it is som...
Biochemical mechanism and biological effects of the inhibition of silent information regulator 1 (SIRT1) by EX-527 (SEN0014196 or selisistat) [0.03%]
EX-527(SEN0014196或selisistat)抑制沉默信息调节因子1(SIRT1)的生化机制及其生物学效应
Sylvain Broussy,Hanna Laaroussi,Michel Vidal
Sylvain Broussy
The human sirtuin silent information regulator 1 (SIRT1) is a NAD+-dependent deacetylase enzyme. It deacetylates many protein substrates, including histones and transcription factors, thereby controlling many physiological and pathological ...
Recent progress in the development of steroid sulphatase inhibitors - examples of the novel and most promising compounds from the last decade [0.03%]
近年开发的类固醇硫酸酯酶抑制剂研究进展——过去十年中新型和最有前景化合物的例子
Mateusz Daśko,Sebastian Demkowicz,Karol Biernacki et al.
Mateusz Daśko et al.
The purpose of this review article is to provide an overview of recent achievements in the synthesis of novel steroid sulphatase (STS) inhibitors. STS is a crucial enzyme in the biosynthesis of active hormones (including oestrogens and andr...
Design, synthesis and in vitro antiproliferative activity of new thiazolidinedione-1,3,4-oxadiazole hybrids as thymidylate synthase inhibitors [0.03%]
新型噻唑烷二酮-1,3,4-氧氮杂环丁烷衍生物的设计、合成及体外抗增殖活性和胸苷酸合酶抑制作用研究
Zohor Mohammad Mahdi Alzhrani,Mohammad Mahboob Alam,Thikryat Neamatallah et al.
Zohor Mohammad Mahdi Alzhrani et al.
Thymidylate synthase (TS) has been an attention-grabbing area of research for the treatment of cancers due to their role in DNA biosynthesis. In the present study, we have synthesised a library of thiazolidinedione-1,3,4-oxadiazole hybrids ...
Discovery of 5-methyl- N-(2-arylquinazolin-7-yl)isoxazole-4-carboxamide analogues as highly selective FLT3 inhibitors [0.03%]
FLT3抑制剂5-甲基-N-（2-芳基喹唑啉-7-基）异噁唑-4-甲酰胺类似物的研究发现
Daseul Im,Hyungwoo Moon,Jinwoong Kim et al.
Daseul Im et al.
A series of 4-arylamido 5-methylisoxazole derivatives with quinazoline core was designed and synthesised based on conformational rigidification of a previous type II FMS inhibitor. Most of quinazoline analogues displayed activity against FL...
Synthesis and carbonic anhydrase activating properties of a series of 2-amino-imidazolines structurally related to clonidine1 [0.03%]
一类与克隆底因相关的2-氨基恶唑烷的合成及其碳酸酐酶活性研究
Niccolò Chiaramonte,Soumia Maach,Caterina Biliotti et al.
Niccolò Chiaramonte et al.
The Carbonic Anhydrase (CA, EC 4.2.1.1) activating properties of histamine have been known for a long time. This compound has been extensively modified but only in few instances the imidazole ring has been replaced with other heterocycles. ...
Chemical approaches for the enhancement of porphyrin skeleton-based photodynamic therapy [0.03%]
基于卟啉骨架的光动力治疗的化学增效方法研究进展
Yuyan Lin,Tao Zhou,Renren Bai et al.
Yuyan Lin et al.
With the development of photodynamic therapy (PDT), remarkable studies have been conducted to generate photosensitisers (PSs), especially porphyrin PSs. A variety of chemical modifications of the porphyrin skeleton have been introduced to i...
Synthesis and biological evaluation of new 3(2 H)-pyridazinone derivatives as non-toxic anti-proliferative compounds against human colon carcinoma HCT116 cells [0.03%]
一类新型3(2H)-哒嗪酮衍生物的合成及其体外抗肿瘤活性研究
Zeynep Özdemir,Semra Utku,Bijo Mathew et al.
Zeynep Özdemir et al.
Novel 3(2H)-pyridazinone derivatives were designed, synthesised in satisfactory yields and evaluated in different experimental assays to assess their preliminary toxicity in vivo and anti-proliferative effects against HCT116 cell lines in v...