Design, synthesis, and biological evaluation of novel substituted thiourea derivatives as potential anticancer agents for NSCLC by blocking K-Ras protein-effectors interactions [0.03%]
设计、合成及生物评估新的取代硫脲衍生物作为潜在的抗癌症药物以阻断K-Ras蛋白-效应者互作来治疗非小细胞肺癌
Yuan Zhang,Xin Meng,Haikang Tang et al.
Yuan Zhang et al.
Mutation of the proto-oncogene K-Ras is one of the most common molecular mechanisms in non-small cell lung cancer. Many drugs for treating lung cancer have been developed, however, due to clinical observed K-Ras mutations, corresponding che...
Synthesis, antibacterial and anticancer activity, and docking study of aminoguanidines containing an alkynyl moiety [0.03%]
含乙炔基氨基胍的合成、抗菌和抗肿瘤活性及分子对接研究
Xianqing Deng,Mingxia Song
Xianqing Deng
Two series of aminoguanidines containing an alkynyl moiety were designed, synthesised, and screened for antibacterial and anticancer activities. Generally, the series 3a-3j with a 1,2-diphenylethyne exhibited better antibacterial activity t...
1-(Piperidin-3-yl)thymine amides as inhibitors of M. tuberculosis thymidylate kinase [0.03%]
作为M. tuberculosis胸苷酸激酶抑制剂的噻密啶胺类化合物
Yanlin Jian,Martijn D P Risseeuw,Mathy Froeyen et al.
Yanlin Jian et al.
A series of readily accessible 1-(piperidin-3-yl)thymine amides was designed, synthesised and evaluated as Mycobacterium tuberculosis TMPK (MtbTMPK) inhibitors. In line with the modelling results, most inhibitors showed reasonable MtbTMPK i...
Novel sulphonamides incorporating triazene moieties show powerful carbonic anhydrase I and II inhibitory properties [0.03%]
一类新的三氮烯类磺酰胺化合物具有较强的碳酸酐酶I和II抑制活性
Sinan Bilginer,Baris Gonder,Halise Inci Gul et al.
Sinan Bilginer et al.
A series of compounds incorporating 3-(3-(2/3/4-substituted phenyl)triaz-1-en-1-yl) benzenesulfonamide moieties were synthesised and their chemical structure was confirmed by physico-chemical methods. Carbonic anhydrase (CA, EC 4.2.1.1) inh...
Reprofiling of pyrimidine-based DAPK1/CSF1R dual inhibitors: identification of 2,5-diamino-4-pyrimidinol derivatives as novel potential anticancer lead compounds [0.03%]
嘧啶衍生物重新定位得到针对DAPK1和CSF1R的双重抑制剂：新型抗癌先导化合物2，5-二氨基-4-嘧啶醇类衍生物的发现
Ahmed K Farag,Ahmed H E Hassan,Byung Sun Ahn et al.
Ahmed K Farag et al.
Hybridization of reported weakly active antiproliferative hit 5-amino-4-pyrimidinol derivative with 2-anilino-4-phenoxypyrimidines suggests a series of 2,5-diamino-4-pyrimidinol derivatives as potential antiproliferative agents. Few compoun...
Novel benzofuran-based sulphonamides as selective carbonic anhydrases IX and XII inhibitors: synthesis and in vitro biological evaluation [0.03%]
新型苯并呋喃类磺酰胺类化合物作为选择性碳酸酐酶IX和XII抑制剂：合成及体外生物活性评价
Mohamed A Abdelrahman,Wagdy M Eldehna,Alessio Nocentini et al.
Mohamed A Abdelrahman et al.
Pursuing on our efforts toward searching for efficient hCA IX and hCA XII inhibitors, herein we report the design and synthesis of new sets of benzofuran-based sulphonamides (4a,b, 5a,b, 9a-c, and 10a-d), featuring the zinc anchoring benzen...
Screening of benzenesulfonamide in combination with chemically diverse fragments against carbonic anhydrase by differential scanning fluorimetry [0.03%]
用于筛选苯磺酰胺与化学多样性片段对碳酸酐酶组合抑制作用的差示扫描量热法
Mikhail Krasavin,Stanislav Kalinin,Sergey Zozulya et al.
Mikhail Krasavin et al.
The differential scanning fluorimetry (DSF) screening of 5.692 fragments in combination with benzenesulfonamide (BSA) against bovine carbonic anhydrase (bCA) delivered >100 hits that either caused, on their own, a significant thermal shift ...
Design, synthesis and molecular modelling studies of some pyrazole derivatives as carbonic anhydrase inhibitors [0.03%]
设计、合成并用分子模拟手段研究一些新型吡唑化合物作为碳酸酐酶抑制剂的作用机制
Yazgı Dizdaroglu,Canan Albay,Tayfun Arslan et al.
Yazgı Dizdaroglu et al.
In this study, newly synthesised compounds 6, 8, 10 and other compounds (1-5, 7 and 9) and their inhibitory properties against the human isoforms hCA I and hCA II were reported for the first time. Compounds 1-10 showed effective inhibition ...
Plasmatic exosomes from prostate cancer patients show increased carbonic anhydrase IX expression and activity and low pH [0.03%]
前列腺癌患者血浆来源的外泌体中碳酸酐酶IX表达、活性升高以及pH值降低
Mariantonia Logozzi,Davide Mizzoni,Clemente Capasso et al.
Mariantonia Logozzi et al.
Acidity, hypoxia and increased release of exosomes are severe phenotypes of tumours. The regulation of pH in tumours involves the interaction of several proteins, including the carbonic anhydrases which catalyze the formation of bicarbonate...
Evaluation of the paraoxonase-1 kinetic parameters of the lactonase activity by nonlinear fit of progress curves [0.03%]
非线性拟合进度曲线评价PARAOxonase-1的酯酶活性动力学参数
Marko Goličnik,Aljoša Bavec
Marko Goličnik
Although paraoxonase-1 (PON1) activity has been demonstrated to be a reliable biomarker of various diseases, clinical studies have been based only on relative comparison of specific enzyme activities, which capture differences mainly due to...