Day: February 27, 2023

Design and synthesis of 1,2,3-triazole incorporated pyrimidine-benzoxazole derivatives as anticancer agents was written by Sudhakar, D. G. S.;Rao, A. Srinivasa;Reddy, Ch. Venkata Ramana;Somaiah, Nalla. And the article was included in Chemical Data Collections in 2022.Recommanded Product: (2-Amino-1,3-benzoxazol-5-yl)boronic acid hydrochloride This article mentions the following:

A new library of 1,2,3-triazole linked pyrimidine-benzoxazole derivatives I [Ar = pyridin-4-yl, 4-ClC₆H₄, pyrimidin-2-yl, etc.] was synthesized and characterized. Further, the preliminary anticancer activities of compounds I were tested on four human cancer cell lines such as prostate cancer (PC3 and DU-145), lung cancer (A549) and breast cancer (MCF-7) by using of MTT method. These activities were compared with clin. drug candidate etoposide. Among the screened compounds, five compounds I [R = pyridin-4-yl, pyrimidin-2-yl, 3,5-(Me)₂C₆H₃, 3,5-(OMe)₂C₆H₃, 3,4,5-(OMe)₃C₆H₂] exhibited considerable activities on four cell lines. In which one compound I [R = pyrimidin-2-yl] showed most promising activity among the synthesized compounds In the experiment, the researchers used many compounds, for example, (2-Amino-1,3-benzoxazol-5-yl)boronic acid hydrochloride (cas: 1404480-15-4Recommanded Product: (2-Amino-1,3-benzoxazol-5-yl)boronic acid hydrochloride).

(2-Amino-1,3-benzoxazol-5-yl)boronic acid hydrochloride (cas: 1404480-15-4) belongs to benzoxazole derivatives. Benzoxazole derivatives have different biological activities. Benzoxazoles are prominent in medicinal chemistry due to their wide spectrum of pharmacological activities such as anti-inflammatory, antimycobacterial, antihistamine.Recommanded Product: (2-Amino-1,3-benzoxazol-5-yl)boronic acid hydrochloride

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Silver-mediated direct amination of benzoxazoles: tuning the amino group source from formamides to parent amines was written by Cho, Seung Hwan;Kim, Ji Young;Lee, S. Yunmi;Chang, Sukbok. And the article was included in Angewandte Chemie, International Edition in 2009.Recommanded Product: 5-Methoxybenzo[d]oxazole This article mentions the following:

Decarbonylative amination of benzoxazole derivatives with formamides was achieved in presence of Ag₂CO₃ and p-anisic acid. The aminobenzoxazole derivatives were obtained in good yields using this method. Meanwhile, silver-mediated direct amination of benzoxazole with amines were also performed in good yields under same reaction conditions. In the experiment, the researchers used many compounds, for example, 5-Methoxybenzo[d]oxazole (cas: 132227-03-3Recommanded Product: 5-Methoxybenzo[d]oxazole).

5-Methoxybenzo[d]oxazole (cas: 132227-03-3) belongs to benzoxazole derivatives. Benzoxazole derivatives have gained a lot of importance in the past few years because of their use in intermediates for the preparation of new biological materials. In the past years, numerous benzoxazole derivatives have been synthesised and evaluated for their biological potential.Recommanded Product: 5-Methoxybenzo[d]oxazole

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Defluorinative Functionalization of Pd(II) Fluoroalkyl Complexes was written by Wade Wolfe, Michael M.;Shanahan, James P.;Kampf, Jeff W.;Szymczak, Nathaniel K.. And the article was included in Journal of the American Chemical Society in 2020.Safety of 5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)benzo[d]oxazole This article mentions the following:

When subjected to arylboranes, anionic trifluoromethyl and difluorobenzyl palladium(II) complexes undergo fluoride abstraction followed by 1,1-migratory insertion. The resulting intermediate fluoroalkyl species can be induced to undergo a subsequent transmetalation and reductive elimination from either an in situ formed fluoroboronate (FB(Ar₃)^–) or an exogenous boronic acid/ester (ArB(OR)₂) and nucleophilic activator, representing a net defluorinative arylation reaction. The latter method enabled a structurally diverse substrate scope to be prepared from either an isolated palladium-CF₃ complex, or from Pd(PPh₃)₄ and other com. available reagents. In the experiment, the researchers used many compounds, for example, 5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)benzo[d]oxazole (cas: 936902-12-4Safety of 5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)benzo[d]oxazole).

5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)benzo[d]oxazole (cas: 936902-12-4) belongs to benzoxazole derivatives. Benzoxazole derivatives have gained a lot of importance in the past few years because of their use in intermediates for the preparation of new biological materials. Benzoxazoles are prominent in medicinal chemistry due to their wide spectrum of pharmacological activities such as antiparkinson, inhibition of hepatitis C virus, 5-HT3 antagonistic effect.Safety of 5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)benzo[d]oxazole

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Cu^II/H-USY as a regenerable bifunctional catalyst for the additive-free C-H amination of azoles was written by Henrion, Mickael;Smolders, Simon;De Vos, Dirk E.. And the article was included in Catalysis Science & Technology in 2020.Application In Synthesis of 5-Methoxybenzo[d]oxazole This article mentions the following:

A copper-exchanged H-USY zeolite catalyst was developed for the direct C-H amination of azoles with secondary amines in HFIP. The reaction was performed under air without any external additive. The Cu/H-USY catalyst could be regenerated for further re-use without significant decrease in activity. In the experiment, the researchers used many compounds, for example, 5-Methoxybenzo[d]oxazole (cas: 132227-03-3Application In Synthesis of 5-Methoxybenzo[d]oxazole).

5-Methoxybenzo[d]oxazole (cas: 132227-03-3) belongs to benzoxazole derivatives. Benzoxazole derivatives have gained a lot of importance in the past few years because of their use in intermediates for the preparation of new biological materials. A number of marketed drugs are available having benzoxazole as core active moiety like, nonsteroidal anti-inflammatory drug (NSAID)—flunoxaprofen, benoxaprofen, antibiotic—calcimycin.Application In Synthesis of 5-Methoxybenzo[d]oxazole

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Merging the ring opening of benzoxazoles with secondary amines and an iron-catalyzed oxidative cyclization towards the environmentally friendly synthesis of 2-aminobenzoxazoles was written by Xu, Daqian;Wang, Wenfang;Miao, Chengxia;Zhang, Qiaohong;Xia, Chungu;Sun, Wei. And the article was included in Green Chemistry in 2013.Electric Literature of C8H7NO2 This article mentions the following:

A facile and environmentally friendly method was developed through merging the ring opening of benzoxazoles with secondary amines and an iron-catalyzed oxidative cyclization towards the synthesis of 2-aminobenzoxazoles. In the oxidative cyclization step, with catalytic amounts of FeCl and aqueous H₂O₂ as a green oxidant, highly desirable 2-aminobenzoxazoles were isolated in excellent yields of up to 97%. A plausible radical process is proposed for the oxidative cyclization on the basis of mechanistic studies. In the experiment, the researchers used many compounds, for example, 5-Methoxybenzo[d]oxazole (cas: 132227-03-3Electric Literature of C8H7NO2).

5-Methoxybenzo[d]oxazole (cas: 132227-03-3) belongs to benzoxazole derivatives. Although benzoxazole itself is of little practical value, many derivatives of benzoxazoles are commercially important. Benzoxazoles are prominent in medicinal chemistry due to their wide spectrum of pharmacological activities such as antibacterial, antifungal, anticancer.Electric Literature of C8H7NO2

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Cobalt-Catalyzed Cross-Dehydrogenative Coupling Reactions of (Benz)oxazoles with Ethers was written by Li, Yanrong;Wang, Mengshi;Fan, Wei;Qian, Fen;Li, Guigen;Lu, Hongjian. And the article was included in Journal of Organic Chemistry in 2016.Recommanded Product: 132227-03-3 This article mentions the following:

The cobalt-catalyzed cross-dehydrogenative coupling of (benz)oxazoles and ethers is described. Access to some important bioactive heteroaryl ether derivatives was achieved using CoCO₃ as an inexpensive catalyst at levels as low as 1.0 mol %. Investigation of the mechanism indicates a catalytic cycle involving a radical process. In the experiment, the researchers used many compounds, for example, 5-Methoxybenzo[d]oxazole (cas: 132227-03-3Recommanded Product: 132227-03-3).

5-Methoxybenzo[d]oxazole (cas: 132227-03-3) belongs to benzoxazole derivatives. Its aromaticity makes it relatively stable, although as a heterocycle, it has reactive sites which allow for functionalization. Benzoxazoles are prominent in medicinal chemistry due to their wide spectrum of pharmacological activities such as antibacterial, antifungal, anticancer.Recommanded Product: 132227-03-3

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Copper-Catalyzed Alkylation of Benzoxazoles with Secondary Alkyl Halides was written by Ren, Peng;Salihu, Isuf;Scopelliti, Rosario;Hu, Xile. And the article was included in Organic Letters in 2012.Quality Control of 5-Methoxybenzo[d]oxazole This article mentions the following:

Copper-catalyzed direct alkylation of benzoxazoles using nonactivated secondary alkyl halides has been developed. The best catalyst is a new copper(I) complex and the reactions are promoted by bis[2-(N,N-dimethylamino)ethyl]ether. In the experiment, the researchers used many compounds, for example, 5-Methoxybenzo[d]oxazole (cas: 132227-03-3Quality Control of 5-Methoxybenzo[d]oxazole).

5-Methoxybenzo[d]oxazole (cas: 132227-03-3) belongs to benzoxazole derivatives. Its aromaticity makes it relatively stable, although as a heterocycle, it has reactive sites which allow for functionalization. The wide range in therapeutic potential of benzoxazole derivatives is related to the favourable interactions of the benzoxazole moiety with different protein targets.Quality Control of 5-Methoxybenzo[d]oxazole

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Structure-activity relationship studies of tolfenpyrad reveal subnanomolar inhibitors of Haemonchus contortus development was written by Le, Thuy G.;Kundu, Abhijit;Ghoshal, Atanu;Nguyen, Nghi H.;Preston, Sarah;Jiao, Yaqing;Ruan, Banfeng;Xue, Lian;Huang, Fei;Keiser, Jennifer;Hofmann, Andreas;Chang, Bill C. H.;Garcia-Bustos, Jose;Wells, Timothy N. C.;Palmer, Michael J.;Jabbar, Abdul;Gasser, Robin B.;Baell, Jonathan B.. And the article was included in Journal of Medicinal Chemistry in 2019.Quality Control of 5-Methoxybenzo[d]oxazole This article mentions the following:

Recently, we have discovered that the registered pesticide, tolfenpyrad, unexpectedly and potently inhibits the development of the L4 larval stage of the parasitic nematode Haemonchus contortus with an IC₅₀ value of 0.03 μM while displaying good selectivity, with an IC₅₀ of 37.9 μM for cytotoxicity. As a promising mol. template for medicinal chem. optimization, we undertook anthelmintic structure-activity relationships for this chem. Modifications of the left-hand side (LHS), right-hand side (RHS), and middle section of the scaffold were explored to produce a set of 57 analogs. Analogs I, II, and III were shown to be the most potent compounds of the series, with IC₅₀ values at a subnanomolar level of potency against the chemotherapeutically relevant fourth larval (L4) stage of H. contortus. Selected compounds from the series also showed promising activity against a panel of other different parasitic nematodes, such as hookworms and whipworms. In the experiment, the researchers used many compounds, for example, 5-Methoxybenzo[d]oxazole (cas: 132227-03-3Quality Control of 5-Methoxybenzo[d]oxazole).

5-Methoxybenzo[d]oxazole (cas: 132227-03-3) belongs to benzoxazole derivatives. Being a heterocyclic compound, benzoxazole finds use in research as a starting material for the synthesis of larger, usually bioactive structures. Due to its versatile biological properties, benzoxazole has been incorporated as an essential pharmacophore and substructure in many medicinal compounds.Quality Control of 5-Methoxybenzo[d]oxazole

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Discovery of 4-Arylindolines Containing a Thiazole Moiety as Potential Antitumor Agents Inhibiting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction was written by Qin, Mingze;Meng, Yangyang;Yang, Haoshen;Liu, Lei;Zhang, Haotian;Wang, Simeng;Liu, Chunyang;Wu, Xia;Wu, Di;Tian, Ye;Hou, Yunlei;Zhao, Yanfang;Liu, Yajing;Xu, Congjun;Wang, Lihui. And the article was included in Journal of Medicinal Chemistry in 2021.SDS of cas: 936902-12-4 This article mentions the following:

Through specific structural modification of a 4-phenylindoline precursor, new 4-arylindolines containing a thiazole moiety were developed and found to be promising modulators of the programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) axis. Compound A30(I) exhibited outstanding biochem. activity, with an IC₅₀ of 11.2 nM in a homogeneous time-resolved fluorescence assay. In the cell-based assay, A30 significantly promoted IFN-γ secretion and rescued T-cell proliferation, which were inhibited by PD-1 activation. Furthermore, A30 showed favorable in vivo antitumor activity in a mouse 4T1 breast carcinoma model. Moreover, in mouse CT26 colon carcinoma models, A30 potently suppressed the growth of CT26/PD-L1 tumor but did not obviously affect the growth of CT26/vector tumor. The results of flow cytometry anal. indicated that A30 inhibited tumor growth by activating the immune microenvironment. We concluded that A30 is a new starting point for further development of PD-1/PD-L1 interaction inhibitors as antitumor agents. In the experiment, the researchers used many compounds, for example, 5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)benzo[d]oxazole (cas: 936902-12-4SDS of cas: 936902-12-4).

5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)benzo[d]oxazole (cas: 936902-12-4) belongs to benzoxazole derivatives. Benzoxazole derivatives have different biological activities. Benzoxazoles are prominent in medicinal chemistry due to their wide spectrum of pharmacological activities such as antibacterial, antifungal, anticancer.SDS of cas: 936902-12-4

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Sulfenylation of β-Diketones Using C-H Functionalization Strategy was written by Varun, Begur Vasanthkumar;Gadde, Karthik;Prabhu, Kandikere Ramaiah. And the article was included in Organic Letters in 2015.Reference of 23417-29-0 This article mentions the following:

Sulfenylation of β-diketones is challenging as β-diketones undergo deacylation after sulfenylation in the reaction medium. The sulfenylation of β-diketones without deacylation under metal-free conditions at ambient temperature via a cross dehydrogenative coupling (CDC) strategy is reported. The resultant products can be further manipulated to form α,α-disubstituted β-diketones and pyrazoles. In the experiment, the researchers used many compounds, for example, 6-Methyl-1,3-benzoxazole-2-thiol (cas: 23417-29-0Reference of 23417-29-0).

6-Methyl-1,3-benzoxazole-2-thiol (cas: 23417-29-0) belongs to benzoxazole derivatives. Benzoxazole derivatives have different biological activities. In the past years, numerous benzoxazole derivatives have been synthesised and evaluated for their biological potential.Reference of 23417-29-0

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem