- COMPOUNDS AND METHODS FOR TREATING CANCER
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The present invention relates to novel compounds, compositions and methods of preparation thereof, as well as uses thereof for treating cancer of various types, including: pancreatic, liver, breast, colon, brain and lung cancer.
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Paragraph 0079
(2019/06/23)
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- One-Step Transformation of Coenzyme A into Analogues by Transamidation
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Several coenzyme A (CoA) analogues are made in a single step under mild conditions via transamidation reactions catalyzed by boric acid in water. This approach offers rapid access to compounds useful for the study of a wide spectrum of enzyme catalyzed re
- Sanichar, Randy,Vederas, John C.
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supporting information
p. 1950 - 1953
(2017/04/28)
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- New series of avenanthramides in oat seed
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Avenanthramides are characteristic constituents of oat seeds. We analyzed the methanol extract of oat seeds by HPLC and detected three compounds 1, 2, and 3 eluted at retention times similar to avenanthramides. The three compounds were purified by column
- Ishihara, Atsushi,Kojima, Kana,Fujita, Takeshi,Yamamoto, Yuya,Nakajima, Hiromitsu
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p. 1975 - 1983
(2015/03/18)
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- Leaf-opening Substance in the Nyctinastic Plant, Albizzia julibrissin Durazz
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cis-p-Coumaroylagmatine (1) was isolated from Albizzia julibrissin Durazz, a nyctinastic plant, as a leaf-opening substance. The compound was quite effective for opening the plant leaves at 5 × 10-6 M at night, but was not effective for other nyctinastic plants. The bioactive fraction with leaf-closing activity was also separated from the plant extract. Although the leaf-opening activity of the plant extract changed between the day and night, the content of 1 was almost constant through a 24-h day. These results suggest that the change in content of an unknown leaf-closing factor induced balance between the two leaf-movement factors through a 24-h day.
- Ueda, Minoru,Sawai, Yoshiyuki,Shibazaki, Yuichiro,Tashiro, Chitose,Ohnuki, Takashi,Yamamura, Shosuke
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p. 2133 - 2137
(2007/10/03)
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- DERIVATIVES OF TETRAPEPTIDES AS CCK AGONISTS
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Selective and potent Type-A CCK receptor agonists of formula (I):X--Y--Z--Q (I)or a pharmaceutically acceptable salt thereof, wherein,X is selected from STR1 Y is selected from STR2 Z is STR3 and Q is STR4 or pharmaceutically-acceptable
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- Development of Potent and Selective CCK-A Receptor Agonists from Boc-CCK-4: Tetrapeptides Containing Lys(Nε)-Amide Residues
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A series of Boc-CCK-4 derivatives represented by the general structure Boc-Trp-Lys(Nε-COR)-Asp-Phe-NH2, where R is an aromatic, heterocyclic, or aliphatic group, are potent and selective CCK-A receptor agonists.These amide-bearing compounds complement the previously described urea-based tetrapeptides (Shiosaki et al.J.Med.Chem. 1991,34,2837-2842); structure-activity studies revealed parallel as well as divergent trends between these two series.A significant correlation was observed between pancreatic binding affinity and the resonance constant R of the phenyl substituent in one particular series of derivatives.Sulfation of phenolic amides appended onto the ε-amino group of the lysine did not affect affinity for the CCK-A receptor in contrast to the 500-fold increase in binding potency observed upon sulfation of CCK-8, suggesting that the lysine appendage and the sulfated tyrosine in CCK-8, both key structural elements that impart high affinity for the CCK-A receptor, are interacting differently with the receptor.The amide-bearing tetrapeptides are full agonists relative to CCK-8 in stimulating pancreatic amylase release while being partial agonists in eliciting phosphoinositide (PI) hydrolysis.Both effects were blocked by selective CCK-A receptor antagonists
- Shiosaki, Kazumi,Lin, Chun Wel,Kopecka, Hana,Craig, Richard A.,Bianchi, Bruce R.,et al.
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p. 2007 - 2014
(2007/10/02)
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- QUINOLIZIDINE ALKALOIDS AND THE ENZYMATIC SYNTHESIS OF THEIR CINNAMIC AND HYDROXYCINNAMIC ACID ESTERS IN LUPINUS ANGUSTIFOLIUS AND L. LUTEUS
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The accumulation pattern of quinolizidine alkaloids during development of seedings and young plants of Lupinus angustifolius and L. luteus are described.The enzymes catalysing the syntheses of the cinnamic acid O-ester of 13-hydroxylupanine and hydroxycinnamic acid O-esters of lupinine (4-coumaroyl- and feruloyllupinine) are characterized and classified as cinnamoyl-CoA:13-hydroxylupanine O-cinnamoyltransferase (EC 2.3.1.-) and hydroxy cinnamoyl-CoA:lupinine O-hydroxycinnamoyltransferase (EC 2.3.1.-). Key Word Index - Lupinus angustifolius; L. luteus; Fabaceae; quinolizidine alkaloids; hydroxycinnamic acid esters; acyltransferase; hydroxycinnamoyl-coenzyme A; biosynthesis.
- Strack, Dieter,Becher, Andrea,Brall, Sabine,Witte, Ludger
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p. 1493 - 1498
(2007/10/02)
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- THE PHOSPHOHYDROLYSIS OF HYDROXYCINNAMOYL-COENZIME A THIOESTERS IN PLANT EXTRACTS
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In barley seedling extracts, p-coumaroyl-CoA is rapidly hydrolysed to p-coumaroyl-dephospho-CoA, p-coumaroyl-4'-phosphopantetheine and p-coumaroyl-pantetheine. p-Coumaroyl-4'-phosphopantetheine is active as a substrate of agmatine coumaroyl transferase in the formation of p-coumaroyl agmatine, but p-coumaroyl-pantetheine is inactive.The phosphohydrolysis can be partly inhibited by inorganic pyrophosphate, sodium fluoride and purine nucleotides.A simplified method for the synthesis of N-hydroxysuccinimide esters of hydroxycinnamic acids, used in the synthesis of CoA thioesters, is also described.Key Word Index -- Hordeum vulgare; Gramineae; barley seedlings; plant extracts; phosphohydrolysis; hydroxycinnamoyl-CoA; p-coumaroylagmatine.
- Negrel, Jonathan,Smith, Terence A.
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