163233-08-7Relevant academic research and scientific papers
HIF-1α inhibitors: Synthesis and biological evaluation of novel moracin O and P analogues
Xia, Yan,Jin, Yinglan,Kaur, Navneet,Choi, Yongseok,Lee, Kyeong
, p. 2386 - 2396 (2011/06/21)
The natural products moracins O and P exhibited potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1), which is a key mediator during adaptation of cancer cells to tumour hypoxia. Systematic variations of the structures of benzofuran type moracins were made and structure-activity relationship analysis showed the importance of the 2-arylbenzofuran ring and the (R)-configuration of the core scaffold. Further evaluation of the representative compound 5 showed its inhibitory effect on HIF-1α protein accumulation and target gene expression under hypoxia.
THIAZOLIDINONE COMPOUNDS, AND METHODS OF MAKING AND USING SAME
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Page/Page column 71-72, (2009/04/25)
Provided herein are thiazolidinone compounds, and methods of making and using the same. Such compounds may be used in inflammatory or immune-mediated disorders. The disclosure provides for treating respiratory or ocular disorders, treating arthritis, or may be used to treat cancer, such as prostate or breast cancer, or multiple myeloma.
Inhibition of IKK-2 by 2-[(aminocarbonyl)amino]-5-acetylenyl-3- thiophenecarboxamides
Bonafoux, Dominique,Bonar, Sheri,Christine, Lori,Clare, Michael,Donnelly, Ann,Guzova, Julia,Kishore, Nandini,Lennon, Patrick,Libby, Adam,Mathialagan, Sumathy,McGhee, William,Rouw, Sharon,Sommers, Cindy,Tollefson, Michael,Tripp, Catherine,Weier, Richard,Wolfson, Serge,Min, Yao
, p. 2870 - 2875 (2007/10/03)
A series of 21 novel 2-[(aminocarbonyl)amino]-5-acetylenyl-3- thiophenecarboxamides were synthesized and evaluated for the inhibition of IKK-2. In spite of their often modest activity on the enzyme, six selected analogs showed significant inhibition of th
Ethynylation of aryl halides by a modified Suzuki reaction: Application to the syntheses of combretastatin A-4, A-5 and lunularic acid
Fuerstner, Alois,Nikolakis, Katharina
, p. 2107 - 2113 (2007/10/03)
On treatment with trimethyl borate sodium acetylide undergoes a palladium-catalyzed cross coupling with functionalized aryl halides or triflates in reasonable to good yields. The ethynylarenes thus obtained serve as building blocks for the formation of the highly effective tubulin polymerization inhibitors combretastatin A-4 (1) and A-5 (2) as well as for the synthesis of the plant-growth regulator lunularic acid (36). VCH Verlagsgesellschaft mbH, 1996.
