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Design, synthesis and biological evaluation of novel analogs of bortezomib

Novel analogs of bortezomib were designed, synthesized and in vitro biological evaluation was carried out using human tumor cell lines A549 and PC3. Docking studies of these analogs of bortezomib was discussed. According to biological investigations, the inhibitors 4, 6, and 8 were found to be more potent than reference drug candidate bortezomib. A549 cell line showed significant sensitivity towards 4, 6, and 8 with IC50 values 14.03, 18.5, and 12.4 nM, respectively, and PC3 cell line showed IC50 values 26.1, 37.0, and 21.2 nM, respectively. The IC50 values of bortezomib in these cell lines are 27.3 nM and 42.0 nM. Copyright

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Extended knowledge of 2-(tert-Butoxycarbonyl)-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid

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A kind of quinazoline derivatives, its composition and use thereof (by machine translation)

The invention relates to the general formula I shown in the quinazoline derivatives, its composition and their use as PGK1 inhibitor in the preparation of anti-tumor drug use and in treating the malignant tumor in the use thereof. (by machine translation)

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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Zr(IV)-Fe(III), -Ga(III), and -Sn(IV) binary metal complexes as synergistic and reusable esterification catalysts

Synergism in catalytic activity with the combined use of Hf(O-i-Pr) 4 or Zr(O-i-Pr)4 and Fe(O-i-Pr)3 for direct esterification and a very simple method for their extraction with ionic liquids for their recovery and reuse are described. This Zr(IV)-Fe(III) complex is an environmentally benign catalyst due to its high turnover number, extremely mild Lewis acidity, low toxicity, reusability, and commercial availability at low cost.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Top Picks: new discover of 2-(tert-Butoxycarbonyl)-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid

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SALTS OF SUBSTITUTED ALLOPHANATES AND THEIR USE IN DRUGS

The invention relates to salts of substituted allophanates, to methods for producing them, to drugs containing said compounds and to the use of said compounds for producing drugs.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Extracurricular laboratory:new discovery of 2-(tert-Butoxycarbonyl)-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid

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Redox-Active Esters in Fe-Catalyzed C-C Coupling

Cross-couplings of alkyl halides and organometallic species based on single electron transfer using Ni and Fe catalyst systems have been studied extensively, and separately, for decades. Here we demonstrate the first couplings of redox-active esters (both isolated and derived in situ from carboxylic acids) with organozinc and organomagnesium species using an Fe-based catalyst system originally developed for alkyl halides. This work is placed in context by showing a direct comparison with a Ni catalyst for >40 examples spanning a range of primary, secondary, and tertiary substrates. This new C-C coupling is scalable and sustainable, and it exhibits a number of clear advantages in several cases over its Ni-based counterpart.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Archives for Chemistry Experiments of 2-(tert-Butoxycarbonyl)-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid

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MCF-supported boronic acids as efficient catalysts for direct amide condensation of carboxylic acids and amines

For efficient direct amide condensations, a new class of catalysts are developed by immobilizing boronic acids on mesocellular siliceous foam. Associated with their large pores, the microenvironments surrounding the immobilized active species greatly influence the catalytic activity. The fluoroalkyl moieties on the silica surface significantly enhance the catalytic performance along with easy recovery and reuse. This approach proposes a potential way to optimize various types of silica-supported catalysts. the Partner Organisations 2014.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

A new application about 2-(tert-Butoxycarbonyl)-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid

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Diastereoselective alpha-alkoxylation of lactamide N-alkyl groups via intramolecular formation of oxonium ions as the key intermediate

Stereoselective introduction of an alkoxy group to the amine unit of lactamide derivatives, under electrochemical oxidation conditions, was investigated based upon the assumption that a cyclic oxonium ion can be formed between the alkoxy substituent on the chiral center and a carbocation generated at the alpha-position of N-alkyl substituents. With N-monosubstituted lactamides, diastereoselectivity in the N-alpha-alkoxylated product was not observed. With N,N-disubstituted lactamides, however, the selectivity appeared though in low ratios (?2.2). Requisite factors that govern the stereoselectivity, i.e. nucleophilicity of both internal and external nucleophiles and substitution on amine units, were also examined.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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Synthesis and antihypertensive activity of a series of 4-amino-6,7-dimethoxyquinazoline derivatives

A series of N2-[(acylamino)alkyl]-6,7-dimethoxy-2,4-quinazolinediamines was synthesized as potential alpha1-adrenoceptor antagonists. When administered to spontaneously hypertensive rats at 10 mg/kg po, a number of propanediamine derivatives showed good antihypertensive activity, whereas the ethanediamine derivatives, albeit being structurally more closely related to prazosin, were devoid of this property. The most active derivative, N-[3-[(4-amino-6,7-dimethoxy-2-quinazolinyl)methylamino]propyl]tetrahydro- 2-furancarboxamide hydrochloride, alfuzosin, showed high selectivity for peripheral alpha1-postjunctional adrenoceptors. At equiactive antihypertensive doses, its effect on the pressor response to postural changes in conscious dog was less marked than that shown by prazosin. In the light of these results, alfuzosin was selected for clinical evaluation.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

A new application about 2-(tert-Butoxycarbonyl)-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid

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A process for the preparation of the medicament kuikui zuo lin kind improved process (by machine translation)

The invention relates to a process for the preparation of the medicament kuikui zuo lin kind improved process, to provide a 2 – chloro – 4 – amino – 6, 7 – dimethoxy quinazoline as intermediate synthetic route, in particular comprising the following steps: acrylonitrile with the methylamine is mellow solution is amine reaction to obtain the intermediate (I); in triethylamine as acid benzyl chloride under conditions as protection basal into intermediate (II); the use of metal duplicate hydride reduction to produce intermediate (III); with the tetrahydrofuran chloride in the acylation reaction intermediate (IV); intermediate (IV) under the catalysis of palladium hydrogenolysis reaction occurs with the formic acid amine to obtain the intermediate (V); the final with 2 – chloro – 4 – amino – 6, 7 – dimethoxy quinazoline generate condensation reaction, to obtain the drug kuikui zuo lin kind alfuzosin hydrochloride (VI). Compared with the other production process, the present invention provides a simple operation, safety, easy control of reaction conditions, low energy consumption, yield stable production process, and has good prospects for industrial application. (by machine translation)

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Brief introduction of 2-(tert-Butoxycarbonyl)-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid

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The annular structure having a side chain dihydropyrazolone deriv. (by machine translation)

PROBLEM TO BE SOLVED: the present invention, excellent TIP48/TIP49 ATPase activity by the action of the composite body, which is useful for the treatment of compd. oncocyte or a pharmaceutically acceptable salt thereof. SOLUTION: the compound has a structure represented by the general eq. (I), a mixture thereof, or a pharmaceutical composition containing such compounds. [And 1] ( In the formula, R 1, R 2, R 3, R 4, R 5, R 6, R 7, W, Z is defined in this specification. ) Selected drawing: no (by machine translation)

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem