56271-33-1

Upstream product

• 150-30-1 Phenylalanine 
• 22509-74-6 N-ethoxycarbonylphthalimide 
• 85-44-9 phthalic anhydride 
• 63-91-2 L-phenylalanine 
• 3588-64-5 phthalyl-L-phenylalanine 
• 673-06-3 D-β-Phenyl-α-alanine 
• 3588-64-5 2-(1,3-Dioxo-1,3-dihydro-isoindol-2-yl)-3-phenyl-propionic acid 
• 3588-64-5 N-phthaloylphenylalanine 

Downstream Products

• 98847-93-9 N-<3-Diazo-2-oxo-1-(phenylmethyl)propyl>phthalimide 
• 7146-63-6 methyl 2-(1,3-dioxoisoindolin-2-yl)-3-phenylpropanoate 
• 111639-19-1 ethyl 2-(1,3-dioxoisoindolin-2-yl)-3-phenylpropanoate 
• 1171-98-8 N-(N,N-phthaloyl-phenylalanyl)-alanine 
• 7447-49-6 (Ξ)-phenylalanine-[(1RS,2RS)-2-hydroxy-1-hydroxymethyl-2-(4-nitro-phenyl)-ethylamide] 
• 76249-23-5 N-(N,N-phthaloyl-DL-phenylalanyl)-glycin-ethyl ester 
• 140244-47-9 N,N-phthaloyl-phenylalanine-p-anisidide 
• 114302-44-2 N,N-phthaloyl-thiophenylalanine-S-(2,4,5-trichloro-phenyl ester) 
• 99481-69-3 2-phthalimido-N,3-diphenylpropanamide 
• 95169-36-1 N-(N,N-phthaloyl-DL-phenylalanyl)-glycine 
• 98863-04-8 N-(N,N-phthaloyl-phenylalanyl)-glycin-amide 
• 124270-62-8 N,N-phthaloyl-phenylalanine-(4-sulfanilyl-anilide) 
• 111978-68-8 N,N-phthaloyl-DL-phenylalanine-butyl ester 
• 104117-43-3 N,N-phthaloyl-DL-phenylalanine-phenyl ester 

Relevant academic research and scientific papers

Amino acid conjugates of aminothiazole and aminopyridine as potential anticancer agents: Synthesis, molecular docking and in vitro evaluation

Purpose: The development of resistance to available anticancer drugs is increasingly becoming a major challenge and new chemical entities could be unveiled to compensate this therapeutic failure. The current study demonstrated the synthesis of 2-aminothiazole [S3 (a-d) and S5(a-d)] and 2-aminopyridine [S4(a-d) and S6(a-d)] derivatives that can target multiple cellular networks implicated in cancer development. Methods: Biological assays were performed to investigate the antioxidant and anticancer potential of synthesized compounds. Redox imbalance and oxidative stress are hallmarks of cancer, therefore, synthesized compounds were preliminarily screened for their antioxidant activity using DPPH assay, and further five derivatives S3b, S3c, S4c, S5b, and S6c, with significant antioxidant potential, were selected for investigation of in vitro anticancer potential. The cytotoxic activities were evaluated against the parent (A2780) and cisplatin-resistant (A2780CISR) ovarian cancer cell lines. Further, Molecular docking studies of active compounds were performed to determine binding affinities. Results: Results revealed that S3c, S5b, and S6c displayed promising inhibition in cisplatin-resistant cell lines in comparison to parent cells in terms of both resistance factor (RF) and IC50 values. Moreover, S3c proved to be most active compound in both parent and resistant cell lines with IC50 values 15.57 μM and 11.52 μM respectively. Our docking studies demonstrated that compounds S3c, S5b, and S6c exhibited significant binding affinity with multiple protein targets of the signaling cascade. Conclusion: Anticancer activities of compounds S3c, S5b, and S6c in cisplatin-resistant cell lines suggested that these ligands may contribute as lead compounds for the development of new anticancer drugs.

NOVEL TRF1 MODULATORS AND ANALOGUES THEREOF

Novel TRF1 modulators and analogues thereof. There is provided compounds of Formula I, wherein R, R1, R2 and X have meanings written in the description. Such compounds are useful as TRF1 inhibitors and, for that reason, as medicaments, in the treatment of cancer, particularly high cancer stem cell cancer like glioblastoma and lung cancer, and can be also useful for the development of additional TRF1 inhibitors and increasing knowledge about TRF1 activity.

A Novel Class of 7-Membered Heterocyclic Compounds

The work presented herein describes the synthesis of a formerly inaccessible class of heterocyclic compounds. The reaction relies on α-phthalimido-amides, which are readily prepared from amino acids in 2 simple reactions steps. Under amide activation conditions in which classical keteniminium ions are not formed, the nitrile solvent is incorporated into the new fused 7-membered ring system. Due to the absence of a keteniminium intermediate, the stereogenic information in the α-position is fully retained.

Kinetic investigation of the cyclopropanation process of fullerene C60 by halogenmethyl ketones under the conditions of the Bingel reaction

The kinetics of the Bingel reaction with halogenmethyl ketones and C60 fullerene has been studied in streaming mode by sampling the reaction mixture at different time intervals and separating the components using HPLC. A quantum-chemical simulation of this cyclopropanation process has been carried out with the DFT method. The activation parameters of the cycloaddition process were determined theoretically and experimentally and correlated with each other. It has been revealed that the use of chloromethyl ketone as the cyclopropanation agent is preferable to its brominated analogue, and a two-fold excess of the substrate with respect to fullerene is the best option for the selective synthesis of mono-adducts.

AMINO ACID DERIVATIVES FOR THE TREATMENT OF INFLAMMATORY DISEASES

The present disclosure provides certain amino acid derivatives that inhibit NF-kB activation and are therefore useful for the treatment of inflammatory diseases. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Quinazolinyl carboxylic ester derivative containing isoindolone group and application thereof

The invention discloses a quinazolinyl carboxylic ester derivative containing an isoindolone group, and the derivative has a structural general formula shown as the specification, wherein R is aryl substituted alkyl, aryl substituted cyclolky or biaryl. According to the invention, the novel isoindolone group-containing quinazolinyl carboxylic ester derivative is synthesized, can effectively inhibit the growth of antibiotic-sensitive or drug-resistant bacteria, and has a new action mechanism.

Carboxy Group as a Remote and Selective Chelating Group for C?H Activation of Arenes

The first example of carboxy group assisted, remote-selective C(sp2)?H activation with a PdII catalyst has been developed and proceeds through a possible κ2 coordination of the carboxy group, thus suppressing the ortho-C?H activation through κ1 coordination. Besides meta-C?H olefination, direct meta-arylation of hydrocinnamic acid derivatives with low-cost aryl iodides has been achieved for the first time. These findings may motivate the exploration of novel reactivities of the carboxy assisted C?H activation reactions with intriguing selectivities.

Synthesis and study of modified polyvinyl alcohol containing amino acid moieties as anticancer agent

A series of new phthalimides compounds[3-7]a-i were synthesized from reaction of Malic anhydride, phthalic anhydride, nitro phthalic anhydride, 2-phenyl-4H-benzo[d][1,3]oxazin-4-one, 2-(4-nitrophenyl)-4H-benzo[d][1,3]oxazin-4-one with different amino acids as glycine, alanine, valine, leucine, isoleucine, serine, threonine, tyrosine and Phenyl alanine [1]a-i under fusion conditions. Compounds [3-7]a-i react with SOCl2 in the presence of benzene to produce compounds [8-12]a-i. Chemical modification of Poly(vinyl alcohol)were obtained by reaction of PVA with compounds [8-12]a-i using the dimethyl formamide to give compounds [13-17]a-i. The structure of the synthesized compounds was characterized by their analytical and spectral data as, IR spectra, 1H, 13C-NMR, Elemental analysis (CHN), UV-Vis Spectroscopy, Scanning electron microscopy (SEM), Antibacterial activity were screened via two kinds of bacteria. Also, anticancer activity were examined for most of the modified polyvinyl alcohol.

Directing Group Participated Benzylic C(sp3)-H/C(sp2)-H Cross-Dehydrogenative Coupling (CDC): Synthesis of Azapolycycles

An efficient method to construct azapolycycles via directing group participated benzylic C(sp3)-H/C(sp2)-H cross-dehydrogenative coupling reactions is described. The reaction proceeded through a palladium catalyzed C(sp3)-H activation followed by coupling with a C(sp2)-H bond of quinoline to afford the azapolycyclic compounds. The reaction works with a broad substrate scope affording the products in moderate to good yields with excellent diastereoselectivities. Control experiments further supported the proposed mechanism.

Bioinspired Deamination of α-Amino Acid Derivatives Catalyzed by a Palladium/Nickel Complex

An efficient bioinspired deamination method of both natural and unnatural amino acid derivatives has been developed. This method provides easy access to a wide variety of useful α, β-unsaturated carbonyl compounds. The reaction is realized with two transition metal catalysts (palladium and Nickel) in-easy handling procedure. A possible reaction pathway is also proposed and the control experiments support the involvement of the palladium-catalyzed inert sp3 C?H activation as one of the key steps. (Figure presented.).