Design, synthesis and biological evaluation of a new thieno[2,3- d]pyrimidine-based urea derivative with potential antitumor activity against tamoxifen sensitive and resistant breast cancer cell lines [0.03%]
新型噻吩并[2,3-d]嘧啶基脲衍生物的设计、合成及对他莫昔芬敏感和耐药乳腺癌细胞系的潜在抗肿瘤活性的生物学评价
Marwa Sharaky,Marwa Kamel,Marwa A Aziz et al.
Marwa Sharaky et al.
Breast cancer (BC) and endocrine resistance to chemotherapy are challenging problems where angiogenesis plays fundamental roles. Thus, targeting of VEGFR-2 signalling pathway has been an attractive approach. In this study, we synthesised a ...
Identification of probe-quality degraders for Poly(ADP-ribose) polymerase-1 (PARP-1) [0.03%]
聚（ADP-核糖）聚合酶1(PARP-1)的降解剂探针的质量识别
Zhimin Zhang,Xinyue Chang,Chixiao Zhang et al.
Zhimin Zhang et al.
Poly(ADP-ribose) polymerase-1 (PARP-1), a critical DNA repair enzyme in the base excision repair pathway, has been pursued as an attractive cancer therapeutic target. Intervention with PARP-1 has been proved to be more sensitive to cancer c...
Claudiu T Supuran
Claudiu T Supuran
Coumarins constitute a relatively new class of inhibitors of the zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1), possessing a unique inhibition mechanism, acting as "prodrug inhibitors." They undergo the hydrolysis of the lactone ring medi...
Design, synthesis and biological evaluation of edaravone derivatives bearing the N-benzyl pyridinium moiety as multifunctional anti-Alzheimer's agents [0.03%]
具有N-苄基吡啶鎓基团的依达拉奉衍生物作为多功能抗阿尔茨海默氏症剂的设计，合成和生物评价
Luke S Zondagh,Sarel F Malan,Jacques Joubert
Luke S Zondagh
A series of multi-target directed edaravone derivatives bearing N-benzyl pyridinium moieties were designed and synthesised. Edaravone is a potent antioxidant with significant neuroprotective effects and N-benzyl pyridinium has previously ex...
Cytotoxic substituted indolizines as new colchicine site tubulin polymerisation inhibitors [0.03%]
具有细胞毒性的取代吲哚嗪作为新的秋水仙碱位点微管聚合抑制剂
Monica-Cornelia Sardaru,Anda Mihaela Craciun,Cristina-Maria Al Matarneh et al.
Monica-Cornelia Sardaru et al.
A potential microtubule destabilising series of new indolizine derivatives was synthesised and tested for their anticancer activity against a panel of 60 human cancer cell lines. Compounds 11a, 11b, 15a, and 15j showed a broad spectrum of g...
Discovery of N-(1-(3-fluorobenzoyl)-1 H-indol-5-yl)pyrazine-2-carboxamide: a novel, selective, and competitive indole-based lead inhibitor for human monoamine oxidase B [0.03%]
N-(1-(3-氟苯甲酰基)-1H-吲哚-5-基）吡唑啉-2-甲酰胺的发现：一种新型的选择性和竞争性的吲哚类先导抑制剂用于人单胺氧化酶B
Ahmed Elkamhawy,Sora Paik,Hyeon Jeong Kim et al.
Ahmed Elkamhawy et al.
Herein, two new series of N-substituted indole-based analogues were rationally designed, synthesized via microwave heating technology, and evaluated as noteworthy MAO-B potential inhibitors. Compared to the reported indazole-based hits VI a...
Design, synthesis and biological evaluation of novel tetrahydrothieno [2,3-c]pyridine substitued benzoyl thiourea derivatives as PAK1 inhibitors in triple negative breast cancer [0.03%]
新型四氢噻喃并[2,3-c]吡啶取代的苯甲酰基硫脲衍生物的设计，合成及其作为三阴性乳腺癌中PAK1抑制剂的生物活性研究
Dahong Yao,Jian Huang,Jinhui Wang et al.
Dahong Yao et al.
The overexpression of P21-activated kinase 1 (PAK1) is associated with poor prognosis in several cancers, which has emerged as a promising drug targets. Based on high-throughput virtual screening strategy, tetrahydrothieno [2,3-c]pyridine s...
Escherichia coli γ-carbonic anhydrase: characterisation and effects of simple aromatic/heterocyclic sulphonamide inhibitors [0.03%]
大肠杆菌γ-碳酸酐酶：特性以及简单芳香/杂环磺胺类抑制剂的影响
Sonia Del Prete,Silvia Bua,Claudiu T Supuran et al.
Sonia Del Prete et al.
Carbonic anhydrases (CAs, EC 4.2.1.1) are ubiquitous metalloenzymes involved in biosynthetic processes, transport, supply, and balance of CO2/HCO3 - into the cell. In Bacteria, CAs avoid the depletion of the dissolved CO2/HCO3 - from the ce...
Functionality study of chalcone-hydroxypyridinone hybrids as tyrosinase inhibitors and influence on anti-tyrosinase activity [0.03%]
查耳酮-羟基吡啶嗪杂环类化合物作为酪氨酸酶抑制剂的功能性研究及其对抑酶活性的影响
L Ravithej Singh,Yu-Lin Chen,Yuan-Yuan Xie et al.
L Ravithej Singh et al.
In an attempt to synthesise new tyrosinase inhibitors, we designed and synthesised a series of chalcone-hydroxypyridinone hybrids as potential tyrosinase inhibitors adopting strategic modifications of kojic acid. All the newly synthesised c...
Inhibitory activity against carbonic anhydrase IX and XII as a candidate selection criterion in the development of new anticancer agents [0.03%]
新的抗癌药物在研发过程中,抑制碳酸酐酶IX和XII的活性作为候选标准
Mikhail Krasavin,Stanislav Kalinin,Tatiana Sharonova et al.
Mikhail Krasavin et al.
Analysis of the literature data reveals that while inhibition of cancer-related carbonic anhydrase IX and XII isoforms continues to be an important enrichment factor for designing anticancer agent development libraries, exclusive reliance o...