- Synthesis and Biological Evaluation of a Series of Novel Celastrol Derivatives with Amino Acid Chain
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The synthesis of celastrol analogues containing amino acid ester at the C(29) position and their evaluation for cytotoxic activities in?vitro were reported. The MTT test showed that a set of derivatives with lower IC50 values than that of the positive control group cisplatin and the parent compound celastrol, which exhibited greater antiproliferative activities. The most potent title compounds 2a and 2e exhibited cytotoxic activities in?vitro against HeLa and A549 cell lines with IC50 values of 0.371 and 0.237?μm, 0.235 and 0.109?μm, respectively. The apoptosis assay demonstrated that 2a and 2e can induces of A549 cell apoptosis in low concentrations. These results showed that 2a and 2e may be promising for further research as antitumor agents.
- Pang, Chaohai,Luo, Jinhui,Liu, Chunhua,Wu, Xuejin,Wang, Dingyong
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- Production technology of cycloserine
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The invention belongs to the field of chemical synthesis, and particularly relates to a production technology of cycloserine. According to the synthesis technology, D-serine is used as a starting material, three reactions of esterification, chlorination and cyclization are performed, and the cycloserine is obtained. The technological process is simple, the yield is high, and the purity is high. During the esterification reaction, diethyl ether is replaced with ethyl acetate, no 8-hydroxyquinoline is added for crude product preparation after the cyclization reaction, and usage of reagent diethyl ether likely to produce toxicity and the dangerous product 8-hydroxyquinoline is avoided. Meanwhile, the synthesis route is short, the cost is low, and the obtained product is stable in yield and controllable in quality.
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Paragraph 0032; 0033; 0034; 0035; 0036
(2016/10/31)
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- DIPEPTIDE AND TRIPEPTIDE EPOXY KETONE PROTEASE INHIBITORS
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Provided herein are dipeptide and tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X): and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of proliferative diseases including cancer and autoimmune diseases.
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Paragraph 00319; 00320
(2014/10/04)
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- Concise synthesis of (+)-serinolamide A
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Serinolamide A, isolated from a species of marine cyanobacteria, exhibits a moderate agonist effect and selectivity for the CB1 cannabinoid receptor, which is unusual for marine natural products. Herein, we reported a highly efficient enantiospecific first total synthesis of (+)-serinolamide A from l-serine in nine steps with 30% overall yield. The synthesis method provides a facile, practicable, and economical approach for the preparation of other similar endocanabinoid lipids.
- Gao, Ya-Ru,Guo, Shi-Huan,Zhang, Zhuan-Xiang,Mao, Shuai,Zhang, Yan-Lei,Wang, Yong-Qiang
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supporting information
p. 6511 - 6513
(2013/11/19)
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- NUCLEOSIDE DERIVATIVES, SYNTHESIS METHODS AND USES THEREOF FOR PREPARING ANTI-TUMOR AND ANTI-VIRUS MEDICAMENTS
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The present invention relates to the field of pharmacochemistry. Disclosed are fluorinated and azido-substituted pyrimidine nucleoside derivatives, and preparation methods and uses thereof. The structural formula is as shown (I). These compounds can be used for preparing medicaments for treating diseases such as tumors and viral infections, and can be used separately or in combination with other medicaments. The compounds also have effective activity against diseases such as tumors and viral infections, while having few side effects, and thus have potential application value.
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Paragraph 0062
(2013/07/25)
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- PYRIMIDINE NUCLEOSIDE DERIVATIVES, SYNTHESIS METHODS AND USES THEREOF FOR PREPARING ANTI-TUMOR AND ANTI-VIRUS MEDICAMENTS
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The present invention relates to the field of pharmacochemistry. Disclosed are fluorinated and azido-substituted pyrimidine nucleoside derivatives, and preparation methods and uses thereof. The structural formula is as shown (I). These compounds can be used for preparing medicaments for treating diseases such as tumors and viral infections, and can be used separately or in combination with other medicaments. The compounds also have effective activity against diseases such as tumors and viral infections, while having few side effects, and thus have potential application value.
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Paragraph 0068
(2013/11/19)
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- Telomestatin: Formal total synthesis and cation-mediated interaction of its seco-derivatives with G-quadruplexes
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The structurally unique natural product telomestatin incorporates seven oxazole rings and one sulfur-containing thiazoline in a macrocyclic arrangement. The compound is a potent inhibitor of the enzyme telomerase and therefore provides a structural framework for developing new potential therapeutic agents for cancer. An efficient formal total synthesis of telomestatin is reported in which the key steps are the use of dirhodium-(II)-catalyzed reactions of diazocarbonyl compounds to generate six oxazole rings, demonstrating the power of rhodium carbene methodology in organic chemical synthesis. CD spectroscopy establishes that seco-derivatives of telomestatin are potent stabilizers of G-quadruplex structures derived from the human telomeric repeat sequence. Mass spectrometry studies, confirmed by molecular dynamics simulations, provide the first evidence that high affinity binding to terminal G-tetrads in both 1:1 and 2:1 ligand complexes is mediated through the macrocycle coordinating a monovalent cation, with selectivity for the antiparallel structure.
- Linder, Joerg,Garner, Thomas P.,Williams, Huw E. L.,Searle, Mark S.,Moody, Christopher J.
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supporting information; experimental part
p. 1044 - 1051
(2011/04/16)
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- Expanded scope for the iridium-catalyzed asymmetric isomerization of primary allylic alcohols using readily accessible second-generation catalysts
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A second generation of chiral (P,N)-iridium catalysts - readily accessible from inexpensive l-serine - displays expanded scope for the asymmetric isomerization of primary allylic alcohols.
- Mantilli, Luca,Mazet, Clement
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supporting information; scheme or table
p. 445 - 447
(2010/04/04)
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- Synthesis of enantiopure quaternary prolines by a metathesis process of 2,5-ethenoproline derivatives
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A novel azabicyclic amino acid was synthesized in both enantiopure forms. The ring-opening metathesis of methyl N-(tert-butoxycarbonyl)-7-azabicyclo[2.2. 1]hept-2-ene-1-carboxylates was used as a method for accessing a new family of enantiopure proline analogues. Georg Thieme Verlag Stuttgart New York.
- Carreras, Javier,Avenoza, Alberto,Busto, Jesus H.,Peregrina, Jesus M.
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experimental part
p. 3353 - 3357
(2010/11/20)
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- METHODS FOR INDUCING THE DIFFERENTIATION OF HEMATOPOIETIC STEM CELLS INTO MEGAKARYOCYTES AND PLATELETS, AND GENE CONTROLLING THE DIFFERENTIATION
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The present invention relates to a method for inducing the differentiation of CD34+ hematopoietic stem cells into megakaryocytes and platelets, more particularly, a method for inducing the differentiation of CD34+ hematopoietic stem cells into megakaryocytes and platelets comprising the steps of coculturing CD34+ hematopoietic stem cells with stromal cells and adding the compound of Formula 1. Further, the present invention relates to a composition for detecting the differentiation of hematopoietic stem cells into megakaryocytes and platelets, comprising an agent measuring expression level of a gene that is selected from the group consisting of KLF2 (Kiruppel-like factor2), LOC138255 (OTTHUMP00000021439), GDF15 (growth differentiation factor 15) and INHBE (inhibin, betaE), a kit comprising the composition, a method for detecting the differentiation into megakaryocytes and platelets by using the marker genes, a method for regulating the differentiation into megakaryocytes and platelets, and a method for screening a candidate compound that regulates the differentiation into megakaryocytes and platelets.
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- Light-sensitive protecting groups for amines and alcohols: The photosolvolysis of n-substituted 7-nitroindolines
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Representative examples of primary and secondary amines were protected as urea derivatives 4 of 5-bromo-7-nitroindoline and even more efficiently as ureas 8 derived from 5,7-dinitroindoline, via high-yield reactions with carbamoyl chlorides 3 and 7, respectively. Deprotection of 4 or 8 was achieved in high yields by UV irradiation at room temperature in Pyrex vessels under neutral conditions and exclusion of air. In a similar manner the dinitroindolines serve as protecting groups for alcohols and phenols; the derived carbamates 5 and 9 can likewise be deprotected photochemically in high yields. Georg Thieme Verlag Stuttgart.
- Hassner, Alfred,Yagudayev, Diana,Pradhan, Tarun K.,Nudelman, Abraham,Amit, Boaz
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p. 2405 - 2409
(2008/03/27)
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- Method of producing halogenated and alpha-aminoalchohols
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A process for the manufacture of N-protected α-aminoketones and N-protected α-aminoalcohols of the formula STR1 wherein X is halogen, one of Q1 and Q2 is hydrogen and the other is hydroxy or Q1 and Q2 together are oxo, R1 is an amino protecting group and R2 is hydrogen or the characterizing group of an α-aminocarboxylic acid, starting from the corresponding lower alkyl N-protected α-aminocarboxylates via corresponding lower alkyl N-silyl protected α-aminocarboxylates.
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- Preparation and isolation of mineral acid salt of an amino acid methyl ester
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A cyclical process for producing and isolating a mineral acid salt of an amino acid methyl ester in high purity and yield from the reaction solution produced by esterifying an amino acid with methanol in methanol in the presence of a mineral acid, by cooling the resulting reaction solution to precipitate crystals of the mineral acid salt; filtering the crystals; drying the isolated wet crystals or washing with another organic solvent; and recycling the filtrate for reuse in the esterification reaction.
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- Retro Aza Diels-Alder Reactions of 2-Azanorbornenes: Improved Methods for the Unmasking of Primary Amines
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The unmasking of primary amines via the heterocycloreversion of N-alkyl-2-azanorbornenes can be catalyzed by either copper(II) or a sulfonic acid based ion exchange resin which obviates the necessity of employing a reactive dienophile to trap the cyclopentadiene as it is produced.
- Grieco, Paul A.,Clark, Jerry D.
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p. 2271 - 2272
(2007/10/02)
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- ASYMMETRIC ALDOL REACTION OF α-ISOCYANOCARBOXYLATES WITH PARAFORMALDEHYDE CATALYZED BY CHIRAL FERROCENYLPHOSPHINE-GOLD(I) COMPLEXES: CATALYTIC ASYMMETRIC SYNTHESIS OF α-ALKYLSERINES
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Aldol reaction of methyl α-isocyanocarboxylates (CNCH(R)COOMe: R=H, Me, Et, i-Pr, Ph) with paraformaldehyde in the presence of 1 molpercent of a chiral (aminoalkyl)ferrocenylphosphine-gold(I) complex gave optically active 4-alkyl-2-oxazoline-4-carboxylates (up to 83percent ee) which were readily hydrolyzed to α-alkylserines.
- Ito, Yoshihiko,Sawamura, Masaya,Shirakawa, Eiji,Hayashizaki, Keiichi,Hayashi, Tamio
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p. 235 - 238
(2007/10/02)
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- Method for preparing amino acid ester hydrohalides
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Amino acid ester hydrohalide is produced by reacting amino acid, alcohol, and halocarbonyl compound represented by the formula: STR1 in the presence of an excess of the alcohol and under substantially anhydrous conditions, wherein X1 and X2 are each independently fluoro, chloro, bromo, trichloromethoxy or tribromomethoxy.
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- 2-Azido-3-benzyloxy-propionic acid-benzyl ester, process for its production and its use
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The subject matter of the invention is the new 2-azido-3-benzyloxy-propionic acid benzyl ester which is a valuable intermediate product for the production of D,L-serine or derivatives of D,L-serine. The new compound is produced by reacting 2-chloroacrylonitrile with twice the molar amount of benzyl alcohol to form 3-benzyloxy-2-chloropropionic acid imino benzyl ester, saponifying this with acid to form 3-benzyloxy-2-chloropropionic acid benzyl ester, and finally exchanging the chlorine atom by means of an alkali metal azide in the presence of a phase transfer catalyst for an azido group.
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