- Anti-tumor application of tocopheroxyl nitrogen oxide as HDAC (Histone Deacetylase) inhibitor
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The invention discloses anti-tumor application of tocopheroxyl nitrogen oxide as an HDAC (Histone Deacetylase) inhibitor. A compound has a structural general formula as shown in a formula (I), and the compound has a potential inhibition effect on HDAC, so that more nitrogen and oxygen can be further provided for a ZBG (Zinc Binding Group), multi-length survey and the like can be carried out on a linker, structure modification can be carried out on the existing basis, and the functions of an inhibitor having good selectivity on HDAC subtype and other target points are expected to be found. According to the anti-tumor application disclosed by the invention, synthetic raw materials are relatively cheap, the technology is simple, the purity is higher, the cost is lower, and used reagents are all relatively safe. The compound is expected to be used as a novel HDAC inhibitor type anti-tumor medicine which is strong in selectivity, high in efficiency and low in toxicity.
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Paragraph 0040-0042
(2017/09/18)
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- NITROGEN-CONTAINING HETEROCYCLIC RING SUBSTITUTED DIHYDROARTEMISININ DERIVATIVES AND USE THEREOF
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The present invention belongs to the field of medicinal technique, specifically relates to nitrogen-containing heterocyclic ring-substituted dihydroartemisinin derivatives and their optical isomers according to formula I or II; wherein substituent X, Y, r
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Paragraph 0246; 0247
(2016/03/01)
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- A straightforward synthesis of N-monosubstituted α-keto amides via aerobic benzylic oxidation of amides
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An efficient sodium bicarbonate promoted aerobic oxidation reaction to prepare N-monosubstituted α-keto amides in the presence of n-tetrabutylammonium hydrogensulfate (TBAHS) was described. This reaction provides a very simple and convenient synthetic route to N-monosubstituted α-keto amides from easily available aryl- or heteroarylacetamides in good to high yields without using toxic reagents and harsh conditions.
- Shao, Jun,Huang, Xiaomei,Wang, Siyuan,Liu, Bingxin,Xu, Bin
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supporting information; experimental part
p. 573 - 579
(2012/01/13)
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- Synthesis of novel 2-(4-(2-morpholinoethoxy)phenyl)-N-phenylacetamide analogues and their antimicrobial study
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A new class of potential biologically active 2-(4-(2-morpholinoethoxy) phenyl)-N-phenylacetamides has been synthesized from hydroxyphenylacetic acid. The products were characterized through IR, 1H NMR, mass spectral studies and elemental analys
- Jayadevappa,Nagendrappa,Umesh,Chandrashekar
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p. 1019 - 1023
(2013/03/14)
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- A highly convenient, efficient, and selective process for preparation of esters and amides from carboxylic acids using Fe3+-K-10 montmorillonite clay
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In the presence of Fe3+-K-10 montmorillonite clay as a catalyst, aliphatic carboxylic acids selectively produced the corresponding esters in the presence of aromatic carboxylic acids by treatment with alcohols. Both the aliphatic and aromatic carboxylic acids formed the amides by reacting with the aliphatic amines, but only the aliphatic carboxylic acids yielded the anilides by treatment with aromatic amines. The catalyst is recoverable and recyclable.
- Srinivas,Das, Biswanath
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p. 1165 - 1167
(2007/10/03)
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- Efficient synthesis of resin-bound α-TMSdiazoketones and their use in solid-phase organic synthesis
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α-TMSdiazoketones on a solid support could be simply and efficiently prepared by reaction of the corresponding resin-bound acid chlorides with excess TMSdiazomethane, without any bases. These α-TMSdiazoketones were used via carbenes or carbenoids for a variety of solid-phase reactions. These useful solid-phase reactions allow efficient construction of diverse compound libraries by use of combinatorial chemistry, due to the high reactivity and wide applications of the carbenes or carbenoids. (C) 2000 Elsevier Science Ltd.
- Iso, Yasuyoshi,Shindo, Hirohisa,Hamana, Hiroshi
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p. 5353 - 5361
(2007/10/03)
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- Allosteric Modifiers of Hemoglobin. 1. Design, Synthesis, Testing, and Structure-Allosteric Activity Relationship of Novel Hemoglobin Oxygen Affinity Decreasing Agents
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Three isomeric series of 2-(aryloxy)-2-methylpropionic acids were prepared and studied for their ability to decrease the oxygen affinity of human hemoglobin A.The isomeric aryloxy groups included 4-methyl>phenoxy, 4-(arylacetamido)phenoxy, and 4-methyl>phenoxy.A total of 20 compounds were synthesized and tested.Structure-activity relationships are presented.Several of the new compounds were found to be strong allosteric effectors of hemoglobin.The two most active compounds are 2-methyl>phenoxy>-2-methylpropionic acid and the corresponding 3,5-dimethyl derivative.The latter two compounds have been compared to other known potent allosteric effectors in the same assay and show greater activity.Both compounds also exhibit a right shift in the oxygen equilibrium curve when incubated with whole blood.The new compounds may be of interest in clinical or biological areas that require or would benefit from a reversal of depleted oxygen supply (i.e., ischemia, stroke, tumor radiotherapy, blood storage, blood substitutes, etc.).They are also structurally related to several marketed antilipidemic agents.
- Randad, Ramnarayan S.,Mahran, Mona A.,Mehanna, Ahmed S.,Abraham, Donald J.
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p. 752 - 757
(2007/10/02)
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