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Design and synthesis of 2-amino-6-(1H,3H-benzo[de]isochromen-6-yl)-1,3,5- triazines as novel Hsp90 inhibitors

A novel series of 2-amino-1,3,5-triazines bearing a tricyclic moiety as heat shock protein 90 (Hsp90) inhibitors is described. Molecular design was performed using X-ray cocrystal structures of the lead compound CH5015765 and natural Hsp90 inhibitor geldanamycin with Hsp90. We optimized affinity to Hsp90, in vitro cell growth inhibitory activity, water solubility, and liver microsomal stability of inhibitors and identified CH5138303. This compound showed high binding affinity for N-terminal Hsp90alpha (Kd = 0.52 nM) and strong in vitro cell growth inhibition against human cancer cell lines (HCT116 IC50 = 0.098 muM, NCI-N87 IC50 = 0.066 muM) and also displayed high oral bioavailability in mice (F = 44.0%) and potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model (tumor growth inhibition = 136%).

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H1403NO – PubChem

 

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Iodine-catalyzed direct allylation of chiral oxazolidinones by the amide-aldehyde-alkene condensation

An iodine-catalyzed direct allylation of chiral oxazolidinones with aldehydes and alkenes has been developed. The reaction proceeds, without use of any bases or metals, directly converted the 3-chiral oxazolidinones into N-allylated oxazolidinones. Additionally, the 3-chiral allylamine skeleton was constructed and the diastereomers were isolated by simple column chromatography.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2069NO – PubChem

 

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 39657-45-9, name is Isoxazolidine hydrochloride, introducing its new discovery. SDS of cas: 39657-45-9

A 6 – chlorophenyl and oxazole […] amide compound and use thereof (by machine translation)

This invention relates to a 6 – chlorophenyl and oxazole […] amide compounds and their use as herbicides, the compound such as formula (I) as shown: Wherein: C W is selected from1 – 4 Alkylene. The compounds of this invention not only has excellent herbicidal activity, but also safe to the crop. (by machine translation)

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Oxazolidine – Wikipedia,
Oxazolidine | C3H1266NO – PubChem

 

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Related Products of 102029-44-7, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 102029-44-7, Name is (R)-4-Benzyl-2-oxazolidinone,introducing its new discovery.

The tandem chain extension aldol reaction used for synthesis of ketomethylene tripeptidomimetics targeting hPEPT1

The rationale for targeting the human di-/tripeptide transporter hPEPT1 for oral drug delivery has been well established by several drug and prodrug cases. The aim of this study was to synthesize novel ketomethylene modified tripeptidomimetics and to investigate their binding affinity for hPEPT1. Three related tripeptidomimetics of the structure H-Phe-psi[COCH2]- Ser(Bz)-Xaa-OH were synthesized applying the tandem chain extension aldol reaction, where amino acid derived beta-keto imides were stereoselectively converted to alpha-substituted gamma-keto imides. In addition, three corresponding tripeptides, composed of amide bonds, were synthesized for comparison of binding affinities. The six investigated compounds were all defined as high affinity ligands (Ki-values <0.5 mM) for hPEPT1 by measuring the concentration dependent inhibition of apical [ 14C]Gly-Sar uptake in Caco-2 cells. Consequently, the ketomethylene replacement for the natural amide bond and alpha-side chain modifications appears to offer a promising strategy to modify tripeptidic structures while maintaining a high affinity for hPEPT1. We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 102029-44-7, and how the biochemistry of the body works.Related Products of 102029-44-7

Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H2051NO – PubChem

 

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Total Synthesis of Al-77-B

Stereoselective hydroxylation of the beta-lactam ester 8 is a key step in a total synthesis of Al-77-B 1.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H375NO – PubChem

 

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Follow-on drugs: How far should chemists look?

A major remark made by observers relates to the focus of the pharmaceutical industry on ‘me-too’ drugs rather than ‘first-in-class’ drugs, the latter are considered to be ‘truly’ innovative medicines. Although the subject is heavily debated, chemists in project teams around the globe are routinely following up compounds from competitors. An important strategic consideration is the degree of chemical modification of the original structure required for success. Here, we present an analysis of the DiMasi and Faden set of first-in-class and follow-on drug pairs (n = 74); showing that 70% of them are structurally very similar, meaning that they are characterized by minimal structural variations. This highlights the fact that even simple atomic variations can cause drastic changes in molecular properties responsible for therapeutic advantages.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H557NO – PubChem

 

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The role of oxazolidine derivatives in the treatment of infectious and chronic diseases

Background: Despite being known for their antibacterial activity, the oxazolidines are molecules with wide pharmacological action and may act as anticonvulsants, anti-inflammatory and antineoplasic agents. However, such activities have been poorly explored and only two oxazolidinic derivatives hit the market until now. Therefore, this review covers the main biological activities of oxazolidines, indicating which of the classes and substituents have the best biological results as well as the synthesis methodology used to obtain them. Methods: The search for bibliographic data was made using a question focused on the oxazolidine structure and their respective activities, besides using inclusion/exclusion criteria clearly defined. The selected papers were subjected to qualitative content analysis methodology to be used in this review. Results: The oxazolidines remain excellent candidates for antibacterial, presenting three compounds in clinical testing phase (Radezolide, Cadezolide and Sutezolide), besides being a good candidate as antitubercular agents. Other less explored activities have niches with a great therapeutic potential such as the oxazolidines acting on 5-HT receptors (anticonvulsant) and Zolmitriptan (anti-migraine), and also mefloquine-oxazolidine derivatives which may act as antineoplasic and antitubercular agents. Conclusion: This review summarizes the versatility and great therapeutic potential that oxazolidines can offer, reinforcing the need for further studies and investments for this class of molecules.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H366NO – PubChem

 

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1,8-DIAZABICYCLO<5.4.0>UNDEC-7-ENE(DBU): AN EFFECTIVE BASE FOR THE INTRODUCTION OF t-BUTYLDIMETHYLSILYL GROUP IN ORGANIC COMPOUNDS.

Reaction of alcohols, thiols, amines, carboxylic acids, phenols, hydroquinones, ketoesters and amides with equimolecular amounts of t-butyldimethylchlorosilane and DBU, even in solvents other than dimethylformamide affords the corresponding t-butyldimethylsilyl derivatives in high yield.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H277NO – PubChem

 

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Cyclization reactions through DDQ-mediated vinyl oxazolidinone oxidation

Vinyl oxazolidinones react with DDQ to form alpha,beta-unsaturated acyliminium ions in a new method for forming electrophiles under oxidative conditions. Appended nucleophiles undergo 1,4-addition reactions with these intermediates to form cyclic vinyl oxazolidinones with good levels of diastereocontrol, highlighting a new approach to utilizing oxidative carbon-hydrogen bond functionalization to increase molecular complexity.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H760NO – PubChem

 

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Highly Efficient Aza-Michael Reactions of Enones with Carbamates Using a Combination of Quaternary Ammonium Salts and BF3¡¤OEt 2 as a Catalyst

Aza-Michael reactions of enones with carbamates took efficiently in the presence of a catalytic amount of quaternary ammonium salts and BF 3¡¤OEt2 to afford the total products in high yields. The new catalytic system was also efficient in the aza-Michael reaction of chalcone, which was difficult to react with carbamates by transition metal salts catalysts.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H1152NO – PubChem