N-Substituted-4-phenylphthalazin-1-amine-derived VEGFR-2 inhibitors: Design, synthesis, molecular docking, and anticancer evaluation studies [0.03%]
N-取代-4-苯基酞嗪-1-胺衍生物的VEGFR-2抑制剂：设计、合成、分子对接及抗肿瘤评价研究
Khaled El-Adl,Mohamed-Kamal Ibrahim,Fathalla Khedr et al.
Khaled El-Adl et al.
In accordance with the significant impetus of the discovery of potent vascular endothelial growth factor receptor 2 (VEGFR-2) inhibitors, herein, we report the design, synthesis, and anticancer evaluation of 12 new N-substituted-4-phenylpht...
Identification of new IDH2R140Q inhibitors by discriminatory analysis-based molecular docking and biological evaluation [0.03%]
基于区分分析的分子对接鉴定出新的IDH2R140Q抑制剂及其生物评价研究
Xiaoyun Chen,Xianmin Wu,Jian Gao et al.
Xiaoyun Chen et al.
Isocitrate dehydrogenase 2 (IDH2) is a key enzyme in the regulation of cell metabolism. Its mutated type can lead to the accumulation of 2-hydroxyglutarate, which is often related to malignancies such as acute myeloid leukemia. Therefore, i...
Ahmed A Fadda,Eman H Tawfik,Marwa Abdel-Motaal et al.
Ahmed A Fadda et al.
In this study, some novel cyanine dyes, 1, 3, and 5-15, were synthesized by a one-pot step reaction of pyridinium salts 2 and/or 4 with benzenaminium salt 1. N-{[1-Chloro-3,4-dihydronaphthalen-2-yl)methylene]benzenaminium} chloride 1 was ob...
Novel benzoic acid derivatives: Synthesis and biological evaluation as multitarget acetylcholinesterase and carbonic anhydrase inhibitors [0.03%]
新型苯甲酸衍生物：多靶点乙酰胆碱酯酶和碳酸酐酶抑制剂的合成与生物学评价
Muharrem Kalaycı,Cüneyt Türkeş,Mustafa Arslan et al.
Muharrem Kalaycı et al.
Alzheimer's disease (AD) is a neurodegenerative disorder characterized by dementia, memory impairment, cognitive dysfunction, and speech impairment. The utility of cholinergic replacement by acetylcholinesterase (AChE) inhibitors in AD trea...
Synthesis and anticancer activities of some new coumarin derivatives including the triazole ring and their in silico molecular docking studies [0.03%]
三唑环取代香豆素衍生物的合成及其抗肿瘤活性和分子对接研究
Emre Menteşe,Adem Güner,Elifsu Polatlı et al.
Emre Menteşe et al.
The synthesis, docking study, and investigation of the anticancer activities of some coumarin derivatives containing the triazole ring are reported in this study. The newly synthesized compounds were screened for their in vitro anticancer a...
Protective effect of corynoline in a murine allergic rhinitis model via inhibition of caspase-1/NF-κB [0.03%]
小分子化合物Corynoline通过抑制Caspase-1/NF-κB信号通路保护变应性鼻炎模型小鼠
Li Wei,Dan Ren,Guna Zhao et al.
Li Wei et al.
Allergic rhinitis (AR) is a serious public health concern worldwide. Therefore, the present study was conducted to scrutinize the protective effect of corynoline (COR) against ovalbumin (OVA)-induced AR in BALB/c mice. The effect of COR was...
Synthesis, antiproliferative activities, and DNA binding of coumarin-3-formamido derivatives [0.03%]
香豆素-3-甲酰氨基衍生物的合成、抗增殖活性以及DNA结合性质研究
Jiuzhou Shi,Wen Lu,Jichao Chen et al.
Jiuzhou Shi et al.
Ten coumarin-3-formamido derivatives, N-benzyl-coumarin-3-carboxamide (2), N-fluorobenzyl-coumarin-3-carboxamide (3-5), N-methoxybenzyl-coumarin-3-carboxamide (6-8), N-((1-methyl-1H-imidazol-5-yl)methyl)-coumarin-3-carboxamide (9), N-(thiop...
Synthesis, antimicrobial evaluation, DNA gyrase inhibition, and in silico pharmacokinetic studies of novel quinoline derivatives [0.03%]
新型喹啉衍生物的合成，抗菌活性评价，DNA促旋酶抑制和计算机辅助药代动力学研究
Mohamed H El-Shershaby,Kamal M El-Gamal,Ashraf H Bayoumi et al.
Mohamed H El-Shershaby et al.
Herein, we report the synthesis and in vitro antimicrobial evaluation of novel quinoline derivatives as DNA gyrase inhibitors. The preliminary antimicrobial activity was assessed against a panel of pathogenic microbes including Gram-positiv...
Synthesis, biological evaluation, and in silico study of pyrazoline-conjugated 2,4-dimethyl-1H-pyrrole-3-carboxylic acid derivatives [0.03%]
吡唑啉连接的2,4-二甲基-1H-吡咯-3-羧酸衍生物的合成，生物活性评价和模拟研究
Nishant K Rasal,Rahul B Sonawane,Sangeeta V Jagtap
Nishant K Rasal
A potential molecular hybridization strategy was used to develop 24 novel pyrazoline-conjugated 2,4-dimethyl-1H-pyrrole-3-carboxylic acid and amide derivatives. The preliminary in vitro antimicrobial assay delivered four potential derivativ...
Design, synthesis, molecular docking, anticancer evaluations, and in silico pharmacokinetic studies of novel 5-[(4-chloro/2,4-dichloro)benzylidene]thiazolidine-2,4-dione derivatives as VEGFR-2 inhibitors [0.03%]
新型5-[(4-氯/2,4-二氯)苯亚甲基]噻唑烷-2,4-二酮衍生物的设计、合成、分子对接、抗肿瘤评价和计算机辅助药代动力学研究作为VEGFR-2抑制剂
Khaled El-Adl,Abdel-Ghany A El-Helby,Helmy Sakr et al.
Khaled El-Adl et al.
The anticancer activity of novel thiazolidine-2,4-diones was evaluated against HepG2, HCT-116, and MCF-7 cells. MCF-7 was the most sensitive cell line to the cytotoxicity of the new derivatives. In particular, compounds 18, 12, 17, and 16 w...