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Bioorganic & Medicinal Chemistry Letters
IF
2.45
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27641
Papers 27666
1 page of 2,767 pages (27.7k results)
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#1Guoqing Sui (NWAFU: Northwest A&F University)H-Index: 2
#2Dan Xu (SCUT: South China University of Technology)
Last.Wenming Zhou (NWAFU: Northwest A&F University)H-Index: 2
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Abstract In continuation of our program to discover new potential antifungal agents, a series of amide and imine derivatives containing a kakuol moiety were synthesized and characterized by the spectroscopic analysis. By using the mycelium growth rate method, the target compounds were evaluated systematically for antifungal activities in vitro against four plant pathogenic fungi, and structure−activity relationships (SAR) were derived. Compounds 7d, 7e, 7h, 7i and 7r showed obvious inhibitory ac...
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#1Noritaka Furuya (OPU: Osaka Prefecture University)H-Index: 3
#2Takaki MomoseH-Index: 2
Last.Takayoshi Kinoshita (OPU: Osaka Prefecture University)H-Index: 26
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Abstract The production of TrkA-selective inhibitors is considerably difficult because the kinase domains of TrkA and its isoforms TrkB/C have highly homologous amino acid sequences. Here we describe the structural basis for the acquisition of selectivity for a isoform-selective TrkA inhibitor, namely compound V1. The X-ray structure revealed that V1 acts as a molecular glue to stabilize the symmetrical dimer of the TrkA kinase domains. V1 binds to the ATP-binding site and simultaneously engages...
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#1Sarita Singh (Central Institute of Medicinal and Aromatic Plants)H-Index: 3
#2Karishma Agarwal (Central Institute of Medicinal and Aromatic Plants)H-Index: 2
Last.Atul Gupta (Central Institute of Medicinal and Aromatic Plants)H-Index: 9
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Abstract A series of substituted 8,8-dimethyl-8H-pyrano[2,3-f]chromen-2-ones (chromeno-coumarin hybrids) was synthesized from scopoletin (11) as vasorelaxing agents. The synthesized compounds 21a-f, 22, 23a-e and scopoletin (11) were evaluated for vasorelaxation in endothelium intact rat main mesenteric artery (MMA). Compounds 11, 21a, 21c-f and 22 showed significant vasorelaxation in precontracted MMA within the range of EC50 value 1.58-5.02 µM. These derivatives presented 29.40-70.89 fold incr...
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#1Haiyan Zhao (Henan University)H-Index: 2
#2Jie Li (Henan University)H-Index: 8
Last.Xianfeng Zhu (Henan University)
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Abstract In this article, a new compound H2[{Cu(HL)(H2O)}2(P2Mo5O23)]·5H2O (1) (HL = 2-acetylpyrazine thiosemicarbazone) has been synthesized and structurally characterized by single-crystal X-ray diffraction of and other detection techniques. Interestingly, the structure of 1 is different from many reported copper-based complexes, in which the [P2Mo5O23]6–, two Cu2+ ions and two HL were directly connected by covalent bands. Biological studies demonstrated that 1 indicated moderate antibacterial...
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Abstract Uncialamycin is one of the structurally simpler and newer members of enediyne family of natural products. It exhibits highly potent activity against several types of bacteria and cancer cells. Described herein is a strategy for the targeted delivery of this cytotoxic agent to tumors using an antibody-drug conjugate (ADC) approach. Central to the design of ADC were the generation of potent and chemically stable uncialamycin analogues and attachment of protease cleavable linkers to newly ...
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#1Satapanawat Sittihan (Chulabhorn Graduate Institute)H-Index: 1
#2Watthanachai Jumpathong (Chulabhorn Graduate Institute)H-Index: 1
Last.Somsak Ruchirawat (Chulabhorn Research Institute)H-Index: 34
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Abstract A series of novel bis(arylsulfonyl)dihydroimidazolinones with different aryl substitution patterns were readily synthesized and evaluated for their antitumor activities. Some of the newly synthesized compounds exhibited cytotoxicity at micromolar range against multiple cancer cell lines, including A549, HepG2, HuCCA-1, and MOLT-3. The most potent analogue contained pentafluorobenzenesulfonyl groups, which could be chemically elaborated to serve as a potential pharmacophore.
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#1Lei Wang (FJUTCM: Fujian University of Traditional Chinese Medicine)
#2Zixuan Yang ('SMMU': Second Military Medical University)
Last.Chunquan Sheng (FJUTCM: Fujian University of Traditional Chinese Medicine)H-Index: 28
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Abstract Starting from easy accessible pyrazoletetrahydropyran acetals, a series of new pyrazolone spirocyclohexadienone derivatives were synthesized and assayed for antitumor activity. Compound 10s was identified to possess good antitumor activity. It could induce MDA-MB-231 cancer cell apoptosis in a concentration dependent manner and arrest the cell cycle progression mainly at the G1 phase.
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Abstract SHP2, a non-receptor protein tyrosine phosphatase encoded by PTPN11 gene, plays an important role in the cell growth and proliferation. Activating mutations of SHP2 have been reported as a cause of various human diseases such as solid tumors, leukemia, and Noonan syndrome. The discovery of SHP2 inhibitor can be a potent candidate for the treatment of cancers and SHP2 related human diseases. Several reports on a small molecule targeting SHP2 have published, however, there are limitations...
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#1Xiaofang Wang (UNMC: University of Nebraska Medical Center)H-Index: 14
#2Monica Cal (University of Basel)H-Index: 4
Last.Jonathan L. Vennerstrom (UNMC: University of Nebraska Medical Center)H-Index: 40
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Abstract Pyridyl benzamide 2 is a potent inhibitor of Trypanosoma cruzi, but not other protozoan parasites, and had a selectivity-index of ≥10. The initial structure-activity relationship (SAR) indicates that benzamide and sulfonamide functional groups, and N-methylpiperazine and sterically unhindered 3-pyridyl substructures are required for high activity against T. cruzi. Compound 2 and its active analogs had low to moderate metabolic stabilities in human and mouse liver microsomes.
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#1Le TaoH-Index: 2
#2Yujiang LiH-Index: 2
Last.Junbiao Chang (Henan Normal University)
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Abstract Seven novel 4-amino acid derivative substituted pyrimidine nucleoside analogues were designed, synthesized, and tested for their anti-CVB3 activity. Initial biological studies indicated that among these 4-amino acid derivative substituted pyrimidine nucleoside analogues, 4-N-(2'-amino-glutaric acid-1'-methylester)-1-(2'- deoxy-2'-β-fluoro-4'-azido)-furanosyl-cytosine 2 exhibited the most potent anti-CVB activity (IC50 = 9.3 μM). The cytotoxicity of these compounds has also been assessed...
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