全部文献期刊会议图书|学者科研项目
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作者:Aida Iraji , Ali Nouri , Najmeh Edraki ...
来源:[J].Bioorganic & Medicinal Chemistry(IF 2.903), 2020, Vol.28 (7)
摘要:Abstract(#br)A series of N,N -diethyl phenyl thioxo-tetrahydropyrimidine carboxamide have been synthesized and investigated for their β-glucuronidase inhibitory activities. All molecules exhibited excellent inhibition with IC 50 values ranging from 0.35 to 42.05 µM and found...
作者:Jian Chen , Cheng Tao , Xiaofei Huang ...
来源:[J].Bioorganic & Medicinal Chemistry(IF 2.903), 2020, Vol.28 (6)
摘要:Abstract(#br)Magnolol, a major bioactive component found in Magnolia officinalis with anti-inflammation and anti-oxidation activities as well as minimized cytotoxic effects. Although magnolol has a wide range of clinical applications, the anti-tumor activity of magnolol is not ef...
作者:Maria A. Ortiz , Heather Michaels , Brandon Molina ...
来源:[J].Bioorganic & Medicinal Chemistry Letters(IF 2.338), 2020
摘要:Abstract(#br)Lemur tyrosine kinase 3 (LMTK3) is oncogenic in various cancers. In breast cancer, LMTK3 phosphorylates and modulates the activity of estrogen receptor-α (ERα) and is essential for the growth of ER-positive cells. LMTK3 is highly expressed in ER-negative breast ...
作者:Marco Potowski , Robin Esken , Andreas Brunschweiger
来源:[J].Bioorganic & Medicinal Chemistry(IF 2.903), 2020
摘要:Abstract(#br)The Petasis three-component reaction gives rise to diverse substituted α-aryl glycines from readily available amines, boronic acids and glyoxalic acid. Thus, this reaction is highly attractive for DNA-encoded small molecule screening library synthesis. The Petas...
作者:Christopher A. Lipinski , Andrew G. Reaume
来源:[J].Bioorganic & Medicinal Chemistry(IF 2.903), 2020
摘要:Abstract(#br)Drug discovery requires the combination of medicinal chemistry and biology. In this article Chris Lipinski, the medicinal chemist, describes the chemical origins at Pfizer of Tolimidone 1 the starting point for the repurposed MLR-1023 2 . Andrew Reaume, the biologist...
作者:Niall A. Anderson , Jenni Cryan , Adil Ahmed ...
来源:[J].Bioorganic & Medicinal Chemistry Letters(IF 2.338), 2020
摘要:Abstract(#br)Inhibitors of CDK4 and CDK6 have emerged as important FDA-approved treatment options for breast cancer patients. The properties and pharmacology of CDK4/6 inhibitor medicines have been extensively profiled, and investigations into the degradation of these target...
作者:Hongmao Sun , Yuhong Wang , Dorian M. Cheff ...
来源:[J].Bioorganic & Medicinal Chemistry(IF 2.903), 2020
摘要:Abstract(#br)Cytotoxicity is a critical property in determining the fate of a small molecule in the drug discovery pipeline. Cytotoxic compounds are identified and triaged in both target-based and cell-based phenotypic approaches due to their off-target toxicity or on-target...
作者:Hehua Xiong , Jianqing Zhang , Qian Zhang ...
来源:[J].Bioorganic & Medicinal Chemistry Letters(IF 2.338), 2020
摘要:Abstract(#br)A series of 4-(pyridin-4-yloxy)benzamide derivatives bearing a 5-methylpyridazin-3(2 H )-one fragment were designed, synthesized, and evaluated for their biological activity. Most compounds showed effective inhibitory activity against cancer cell lines of A549, ...
作者:Shanshan Lin , LingYu Zhang , Xiao Zhang ...
来源:[J].Bioorganic & Medicinal Chemistry(IF 2.903), 2020
摘要:Abstract(#br)Poly (ADP-ribose) polymerase (PARP) inhibitors have achieved great success in clinical application, especially for the prolonged survival of cisplatin-sensitive ovarian cancer patients. However, there are still many patients who do not respond to PARP inhibitors. Nov...
作者:Wafaa A. Ewes , Mohammad A. Elmorsy , Shahenda M. El-Messery ...
来源:[J].Bioorganic & Medicinal Chemistry(IF 2.903), 2020, Vol.28 (7)
摘要:Abstract(#br)New series of triazolo[4,3- c ]quinazolines were designed, synthesized and their structures were elucidated using different spectroscopic techniques. They were evaluated for their in vitro antitumor activity against HepG2, MCF-7, PC-3, HCT-116 and HeLa cancer ce...

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