83544-05-2Relevant academic research and scientific papers
RADIOTRACER PRECURSOR BANI FOR IMAGING OF HYPOXIC TISSUE, RADIOTRACER, AND METHOD FOR PREPARING THE SAME
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Paragraph 0050, (2015/02/18)
The present invention relates to a radiotracer precursor for imaging of hypoxic tissues, a radiotracer and a method for preparing the same. The radiotracer precursor, BANI, includes a nitroimidazole functional group with a feature of retention in hypoxic
RADIOTRACER PRECURSOR FOR IMAGING OF HYPOXIC TISSUE, RADIOTRACER, AND METHOD FOR PREPARING THE SAME
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Paragraph 0033; 0039; 0047, (2015/01/06)
A radiotracer precursor for imaging of hypoxic tissues, a radiotracer and a method for preparing the same are revealed. The radiotracer precursor, DANI, includes a nitroimidazole functional group with a feature of retention in hypoxic tissues and a bifunc
Bifunctional compound containing amino group and diaminedithiol ligand and manufacturing method thereof
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Page/Page column 2; Sheet 4, (2011/04/14)
A bifunctional compound containing an amino group and diaminedithiol ligand and a manufacturing method thereof are revealed, the bifunctional compound includes at least one amino group and a diaminedithiol (N2S2) ligand. The amino gr
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum
Chen, Yufeng,Lopez-Sanchez, Miriam,Savoy, Doris N.,Billadeau, Daniel D.,Dow, Geoffrey S.,Kozikowski, Alan P.
supporting information; scheme or table, p. 3437 - 3448 (2009/04/07)
The discovery of the rules governing the inhibition of the various HDAC isoforms is likely to be key to identifying improved therapeutics that act as epigenetic modulators of gene transcription. Herein we present results on the modification of the CAP reg
Functional differences in epigenetic modulators - Superiority of mercaptoacetamide-based histone deacetylase inhibitors relative to hydroxamates in cortical neuron neuroprotection studies
Kozikowski, Alan P.,Chen, Yufeng,Gaysin, Arsen,Chen, Bin,D'Annibale, Melissa A.,Suto, Carla M.,Langley, Brett C.
, p. 3054 - 3061 (2008/02/09)
We compare the ability of two structurally different classes of epigenetic modulators, namely, histone deacetylase (HDAC) inhibitors containing either a hydroxamate or a mercaptoacetamide as the zinc binding group, to protect cortical neurons in culture from oxidative stress-induced death. This study reveals that some of the mercaptoacetamide-based HDAC inhibitors are fully protective, whereas the hydroxamates show toxicity at higher concentrations. Our present results appear to be consistent with the possibility that the mercaptoacetamide-based HDAC inhibitors interact with a different subset of the HDAC isozymes [less activity at HDAC1 and 2 correlates with less inhibitor toxicity], or alternatively, are interacting selectively with only the cytoplasmic HDACs that are crucial for protection from oxidative stress.
Stabilizing and destabilizing effects of phenylalanine → F 5-phenylalanine mutations on the folding of a small protein
Woll, Matthew G.,Hadley, Erik B.,Mecozzi, Sandro,Gellman, Samuel H.
, p. 15932 - 15933 (2007/10/03)
We report a systematic evaluation of phenylalanine-to-pentafluorophenylalanine (Phe → F5-Phe) mutants for the 35-residue chicken villin headpiece subdomain (c-VHP), the hydrophobic core of which features a cluster of three Phe side chains (residues 6, 10, and 17). Phe → F5-Phe mutations are interesting because aryl-perfluoroaryl interactions of optimal geometry are intrinsically more favorable than aryl-aryl interactions and because perfluoroaryl units are more hydrophobic than are analogous aryl units. One mutant, Phe-10 → F5-Phe, provides enhanced tertiary structural stability relative to the native sequence. The other six mutants analyzed caused a decrease in stability. Copyright
Histone deacetylase inhibitors and methods of use thereof
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Page/Page column 31, (2008/06/13)
The invention provides novel classes of HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided as well as methods for treating cancer and methods for treating neurological diseases. Additionally, t
Chemistry and biology of mercaptoacetamides as novel histone deacetylase inhibitors
Chen, Bin,Petukhov, Pavel A.,Jung, Mira,Velena, Alfredo,Eliseeva, Elena,Dritschilo, Anatoly,Kozikowski, Alan P.
, p. 1389 - 1392 (2007/10/03)
A series of mercaptoacetamides were designed and synthesized as novel histone deacetylase inhibitors with the aid of modeling. Their ability to inhibit HDAC activity and their effects on cancer cell growth were investigated. Some compounds exhibit better
Method of selectively inhibiting prostaglandin G/H synthase-2
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, (2008/06/13)
The present invention provides a method of selectively inhibiting prostaglandin G/H synthase-2 that comprises administering to a patient in need of such inhibition an inhibiting amount of a compound having the Formula I, II or III STR1 wherein the R group
Synthesis of -Catenanes from -Rotaxanes
Schill, Gottfried,Schweickert, Norbert,Fritz, Hans,Vetter, Walter
, p. 961 - 970 (2007/10/02)
Starting from the rotaxane 18a a mixture of catenane 21 and rotaxane 23 is obtained by attaching a polymethylene bridge between the methylene groups in α-position of the sulfonyl groups.The isocyclic catenane 28 containing a 28- and a 46-membered ring is
