Month: February 2023

Design and Synthesis of TASIN Analogues Specifically Targeting Colorectal Cancer Cell Lines with Mutant Adenomatous Polyposis Coli (APC) was written by Wang, Wentian;Zhang, Lu;Morlock, Lorraine;Williams, Noelle S.;Shay, Jerry W.;De Brabander, Jef K.. And the article was included in Journal of Medicinal Chemistry in 2019.Reference of 1138-56-3 This article mentions the following:

Despite advances in targeted anticancer therapies, there are still no small-mol.-based therapies available that specifically target colorectal cancer (CRC) development and progression, the second leading cause of cancer deaths. We previously disclosed the discovery of truncating adenomatous polyposis coli (APC)-selective inhibitor 1 (TASIN-1), a small mol. that specifically targets colorectal cancer cells lines with truncating mutations in the adenomatous polyposis coli (APC) tumor suppressor gene through inhibition of cholesterol biosynthesis. Here, we report a medicinal chem. evaluation of a collection of TASIN analogs and activity against colon cancer cell lines and an isogenic cell line pair reporting on the status of APC-dependent selectivity. A number of potent and selective analogs were identified, including compounds with good metabolic stability and pharmacokinetic properties. The compounds reported herein represent a first-in-class genotype-selective series that specifically target apc mutations present in the majority of CRC patients and serve as a translational platform toward a targeted therapy for colon cancer. In the experiment, the researchers used many compounds, for example, 4-Butoxybenzene-1-sulfonyl chloride (cas: 1138-56-3Reference of 1138-56-3).

4-Butoxybenzene-1-sulfonyl chloride (cas: 1138-56-3) belongs to organic chlorides. Organic chlorides can cause corrosion in pipelines, valves and condensers, and cause catalyst poisoning. The hydrocarbon processing industry (HPI) and others are affected by damage caused by these substances. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. However, the extent of chlorination is difficult to control.Reference of 1138-56-3

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Chlorogenic acids protect organic dyes against self-catalyzed photobleaching was written by Tsuchida, Kino;Okumura, Hisako;Ikarashi, Taro;Takahashi, Yukiko. And the article was included in Journal of Photochemistry and Photobiology, A: Chemistry in 2022.SDS of cas: 61-73-4 This article mentions the following:

An environmentally benign method for preventing the photofading of organic dyes was developed using chlorogenic acids, also known as caffeoylquinic acids (CQAs), which can be obtained in large quantities from agricultural wastes. In this study, 5-caffeoylquinic acid (5-CQA) and 4,5-dicaffeolyquinic acid (4,5-diCQA) were used as singlet oxygen (¹O₂) quenchers, and their suppression mechanisms were evaluated by the self-catalyzed photobleaching reactions of methylene blue (MB) and rose bengal (RB) in aqueous solutions at different pH values. Light irradiation experiments, half-wave oxidation potentials measurements, LC-MS, and NMR demonstrated that CQAs effectively inhibited the photofading of the dyes in the pH range of 4-9 with two independent reaction mechanisms. 4,5-diCQA was more effective in preventing the photofading than 5-CQA. The kinetic anal. estimated the ¹O₂ quenching constants of CQAs (kq = 7.22 x 10⁷ M^-1 s^-1 and 9.33 x 10⁷ M^-1 s^-1 for 5-CQA and 4,5-diCQA) and the bimol. rate constant for the chem. quenching of ¹O₂ by MB (kf = 2.88 x 10⁴ M^-1 s^-1). Comparing these rate constants revealed that the quenching reactions of ¹O₂ by CQAs were more predominantly than the photofading reaction of MB. In the experiment, the researchers used many compounds, for example, 3,7-Bis(dimethylamino)phenothiazin-5-ium chloride (cas: 61-73-4SDS of cas: 61-73-4).

3,7-Bis(dimethylamino)phenothiazin-5-ium chloride (cas: 61-73-4) belongs to organic chlorides. An organic chloride is an organic compound containing at least one covalently bonded atom of chlorine. Their wide structural variety and divergent chemical properties lead to a broad range of names and applications. The haloform reaction, using chlorine and sodium hydroxide, is also able to generate alkyl halides from methyl ketones, and related compounds. Chloroform was formerly produced thus.SDS of cas: 61-73-4

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

One stone two birds: cobalt-catalyzed in-situ generation of isocyanates and benzyl alcohols for the synthesis of N-aryl carbamates was written by Li, Sida;Khan, Ruhima;Zhang, Xia;Yang, Yong;Wang, Zheting;Zhan, Yong;Dai, Yuze;Liu, Yue-e;Fan, Baomin. And the article was included in Organic & Biomolecular Chemistry in 2019.Category: chlorides-buliding-blocks This article mentions the following:

An efficient method for the synthesis of N-aryl carbamates RNHC(O)OR¹ [R = Ph, 4-FC₆H₄, 4-O₂NC₆H₄, etc.; R¹ = Et, Bn, 4-BrC₆H₄CH₂, etc.] from N-Boc-protected amines and benzyl formates/alcs. was developed. The cobalt-catalyzed in situ generation of isocyanates from N-Boc-protected amines and benzyl alcs. from benzyl formates was achieved for the first time, which in turn furnished the corresponding benzyl carbamates in moderate to high yields. The reaction was catalyzed by CoI₂ with tris-(4-dimethylaminophenyl)-phosphine as the ligand and zinc powder as the reductant. The developed reaction conditions were found to be compatible for aromatic amines with both electron-donating and -withdrawing substituents. In the experiment, the researchers used many compounds, for example, tert-Butyl (4-chlorophenyl)carbamate (cas: 18437-66-6Category: chlorides-buliding-blocks).

tert-Butyl (4-chlorophenyl)carbamate (cas: 18437-66-6) belongs to organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. The haloform reaction, using chlorine and sodium hydroxide, is also able to generate alkyl halides from methyl ketones, and related compounds. Chloroform was formerly produced thus.Category: chlorides-buliding-blocks

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Effect of meta-substituents on aromatic nucleophilic substitution was written by Bevan, C. W. L.;Hirst, J.;Una, S. J.. And the article was included in Chemistry & Industry (London, United Kingdom) in 1966.Recommanded Product: 4815-64-9 This article mentions the following:

Displacement of F in 3,5-R(O₂N)C₆H₃F by OMe ions in MeOH varied by a factor of 10⁴ depending on the group R. The rate decreased as A varied in the order NO₂ > SO₂Me > CF₃ > Br > Cl > I > F > Ac > H > OMe > Me > CMe₃ > CO₂^– > NH₂. For PhF (no other substituent on the ring), the rate was 10^-4 which was the slowest of the meta-nitro-substituted series. All reactions were run at 100°. Despite an overall difference of 10⁸ in rates, the log B factor in the Arrhenius equation k = Be^-Ε/RT remained constant at approx. 12.5. The vast difference in rates was attributed to the changes in the activation energy. The reaction series was sensitive to electronic effects. Somewhat abnormal results, obtained where R was NH₂ or OMe, were attributed to 2nd-order effects in reactions especially sensitive to the charge d. on the C atoms ortho to that bonded to F. In the experiment, the researchers used many compounds, for example, 1-Chloro-3-fluoro-5-nitrobenzene (cas: 4815-64-9Recommanded Product: 4815-64-9).

1-Chloro-3-fluoro-5-nitrobenzene (cas: 4815-64-9) belongs to organic chlorides. Organochlorines are organic compounds having multiple chlorine atoms. They were the first synthetic pesticides that were used in agriculture. They are resistant to most microbial and chemical degradations. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. However, the extent of chlorination is difficult to control.Recommanded Product: 4815-64-9

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Finding of the low molecular weight inhibitors of resuscitation promoting factor enzymatic and resuscitation activity was written by Demina, Galina R.;Makarov, Vadim A.;Nikitushkin, Vadim D.;Ryabova, Olga B.;Vostroknutova, Galina N.;Salina, Elena G.;Shleeva, Margarita O.;Goncharenko, Anna V.;Kaprelyants, Arseny S.. And the article was included in PLoS One in 2009.Recommanded Product: 16588-16-2 This article mentions the following:

Background: Resuscitation promoting factors (RPF) are secreted proteins involved in reactivation of dormant actinobacteria, including Mycobacterium tuberculosis. They have been considered as prospective targets for the development of new anti-tuberculosis drugs preventing reactivation of dormant tubercle bacilli, generally associated with latent tuberculosis. However, no inhibitors of Rpf activity have been reported so far. The goal of this study was to find low mol. weight compounds inhibiting the enzymic and biol. activities of Rpfs. Methodol./Principal Findings: Here the authors describe a novel class of 2-nitrophenylthiocyanates (NPT) compounds that inhibit muralytic activity of Rpfs with IC₅₀ 1-7 μg/mL. Fluorescence studies revealed interaction of active NPTs with the internal regions of the Rpf mol. Candidate inhibitors of Rpf enzymic activity showed a bacteriostatic effect on growth of Micrococcus luteus (in which Rpf is essential for growth protein) at concentrations close to IC₅₀. The candidate compounds suppressed resuscitation of dormant (“non-culturable”) cells of M. smegmatis at 1 μg/mL or delayed resuscitation of dormant M. tuberculosis obtained in laboratory conditions at 10 μg/mL. However, they did not inhibit growth of active mycobacteria under these concentrations Conclusions/Significance: NPT are the first example of low mol. weight compounds that inhibit the enzymic and biol. activities of Rpf proteins. In the experiment, the researchers used many compounds, for example, Ethyl 4-chloro-3-nitrobenzoate (cas: 16588-16-2Recommanded Product: 16588-16-2).

Ethyl 4-chloro-3-nitrobenzoate (cas: 16588-16-2) belongs to organic chlorides. Chlorination modifies the physical properties of hydrocarbons in several ways. These compounds are typically denser than water due to the higher atomic weight of chlorine versus hydrogen. Alkyl chlorides are versatile building blocks in organic chemistry. While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available.Recommanded Product: 16588-16-2

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Structural (X-ray), spectral (FT-IR and Raman) and quantum chemical investigations of a series of 6-benzylaminopurine derivatives was written by Cajan, Michal;Travnicek, Zdenek. And the article was included in Journal of Molecular Structure in 2011.Name: 2,6-Dichloro-9-isopropyl-9H-purine This article mentions the following:

The structural and spectroscopic properties of 6-(2-methylbenzylamino)purine 1, 6-(4-methylbenzylamino)purine 2, 6-(3,4-dimethoxybenzylamino)purine 3, 2-chloro-6-(3-bromobenzylamino)-9-isopropylpurine 4 and 2-chloro-6-(3,4-dichlorobenzylamino)-9-isopropylpurine 5 have been investigated by means of single crystal X-ray diffraction anal., FT-IR and Raman spectroscopy, and quantum chem. calculations, where HF, DFT, RI-MP2 and MP2 methods in combination with the cc-pVDZ basis set have been used. The theor. obtained structural as well as spectral parameters have been compared with those exptl. obtained. One of the unusual structural features is the finding that the electroneutral form of 6-(2-methylbenzylamino)purine 1 is protonated at the N7 position of the purine ring, which is not a typical protonation site for N9-unsubstituted adenine derivatives In the experiment, the researchers used many compounds, for example, 2,6-Dichloro-9-isopropyl-9H-purine (cas: 203436-45-7Name: 2,6-Dichloro-9-isopropyl-9H-purine).

2,6-Dichloro-9-isopropyl-9H-purine (cas: 203436-45-7) belongs to organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Name: 2,6-Dichloro-9-isopropyl-9H-purine

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Light-promoted N,N-dimethylation of amine and nitro compound with methanol catalyzed by Pd/TiO₂ at room temperature was written by Zhang, Lina;Zhang, Yan;Deng, Youquan;Shi, Feng. And the article was included in RSC Advances in 2015.Quality Control of 2-Chloro-N,N-dimethylaniline This article mentions the following:

A series of TiO₂ supported nano-Pd catalysts (Pd/TiO₂) were prepared and used for the N,N-dimethylation of different amines and nitro compounds with methanol under UV irradiation at room temperature A wide range of N,N-di-Me amines were one-pot synthesized with up to 98% by applying aliphatic secondary amines, aromatic primary amines, aliphatic primary amines and aromatic nitro compounds as starting materials. It is noteworthy that up to 90% yield of 4-chloro-N,N-dimethylaniline was obtained by adjusting the Pd loadings on the TiO₂ and the dehalogenation reaction was inhibited. Finally, a reaction mechanism is discussed, involving PhN=CH₂ and PhNHCH₃ as reaction intermediates. In the experiment, the researchers used many compounds, for example, 2-Chloro-N,N-dimethylaniline (cas: 698-01-1Quality Control of 2-Chloro-N,N-dimethylaniline).

2-Chloro-N,N-dimethylaniline (cas: 698-01-1) belongs to organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. Alkyl chlorides are versatile building blocks in organic chemistry. While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available.Quality Control of 2-Chloro-N,N-dimethylaniline

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Sulfonamido-2-arylbenzoxazole GroEL/ES Inhibitors as Potent Antibacterials against Methicillin-Resistant Staphylococcus aureus (MRSA) was written by Abdeen, Sanofar;Kunkle, Trent;Salim, Nilshad;Ray, Anne-Marie;Mammadova, Najiba;Summers, Corey;Stevens, Mckayla;Ambrose, Andrew J.;Park, Yangshin;Schultz, Peter G.;Horwich, Arthur L.;Hoang, Quyen Q.;Chapman, Eli;Johnson, Steven M.. And the article was included in Journal of Medicinal Chemistry in 2018.Name: 3-(Trifluoromethyl)benzene-1-sulfonyl chloride This article mentions the following:

Extending from a study we recently published examining the anti-trypanosomal effects of a series of GroEL/ES inhibitors based on a pseudo-sym. bis-sulfonamido-2-phenylbenzoxazole scaffold, here, we report the antibiotic effects of asym. analogs of this scaffold against a panel of bacteria known as the ESKAPE pathogens (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter species). While GroEL/ES inhibitors were largely ineffective against K. pneumoniae, A. baumannii, P. aeruginosa, and E. cloacae (Gram-neg. bacteria), many analogs were potent inhibitors of E. faecium and S. aureus proliferation (Gram-pos. bacteria – EC₅₀ values of the most potent analogs were in the 1-2 μM range). Furthermore, even though some compounds inhibit human HSP60/10 biochem. functions in vitro (IC₅₀ values in the 1-10 μM range), many of these exhibited moderate to low cytotoxicity to human liver and kidney cells (CC₅₀ values >20 μM). In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Name: 3-(Trifluoromethyl)benzene-1-sulfonyl chloride).

3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. Chlorination modifies the physical properties of hydrocarbons in several ways. These compounds are typically denser than water due to the higher atomic weight of chlorine versus hydrogen. Alkyl chlorides are versatile building blocks in organic chemistry. While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available.Name: 3-(Trifluoromethyl)benzene-1-sulfonyl chloride

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

A mild light-induced cleavage of the S-O bond of aryl sulfonate esters enables efficient sulfonylation of vinylarenes was written by Ratushnyy, Maxim;Kamenova, Monika;Gevorgyan, Vladimir. And the article was included in Chemical Science in 2018.Related Products of 777-44-6 This article mentions the following:

A new mode of S-O bond activation has been discovered, which constitutes novel reactivity of easily available and bench-stable arylsulfonate phenol esters. This protocol enables access to putative sulfonyl radical intermediates, which enable straightforward access to valuable vinyl sulfones I (R = H, 4-OMe, 4-CN, 2-Cl, etc…). In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Related Products of 777-44-6).

3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. Organic chlorides can be used in production of: PVC, pesticides, chloromethane, teflon, insulators. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Related Products of 777-44-6

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Robust polyamide-PTFE hollow fibre membranes for harsh organic solvent nanofiltration was written by Francis, Verona Nithya;Chong, Jeng Yi;Yang, Guoying;Che, Lei;Wang, Rong. And the article was included in Chemical Engineering Journal (Amsterdam, Netherlands) in 2023.Category: chlorides-buliding-blocks This article mentions the following:

Polymeric membranes have been extensively studied for organic solvent nanofiltration (OSN) but many fail to show sufficient chem. resistance in strong solvents like DMF (DMF) and DMSO (DMSO). This study focuses on harnessing the outstanding chem. resistance of polytetrafluoroethylene (PTFE), to develop polyamide-PTFE thin film composite (TFC) membranes that are resistant to such aprotic solvents. A defect-free polyamide thin film layer was successfully synthesized on the microfiltration PTFE hollow fiber substrates, overcoming challenges such as large and uneven pore size, and hydrophobicity of the PTFE substrates. A simple polydopamine (PDA) coating was carried out to improve the substrate’s hydrophilicity prior to the polyamide synthesis via interfacial polymerization (IP). Polyethyleneimine (PEI) and trimesoyl chloride (TMC) were used as the monomers and a two-time IP method was employed to obtain a defect-free polyamide coating. The synthesized membranes showed high acetonitrile (ACN) and DMF permeabilities of 7.94 and 3.70 lm^-2h^-1bar^-1, resp., with acid fuchsin (585 Da) rejections of > 90%. The mol. weight cut-off (MWCO) of the membranes could be further reduced to ∼300 Da by the addition of piperazine (PIP) monomers. The membranes also showed excellent stability and performance in a 72-h OSN test performed in DMF indicating their great potential in effective mol. separation in harsh solvents. This study demonstrates how a simple modification and coating technique can transform com. available microfiltration PTFE hollow fibers into durable and high value OSN membranes. In the experiment, the researchers used many compounds, for example, Trimesoylchloride (cas: 4422-95-1Category: chlorides-buliding-blocks).

Trimesoylchloride (cas: 4422-95-1) belongs to organic chlorides. Organic chlorides can be used in production of: PVC, pesticides, chloromethane, teflon, insulators.While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available. Alkyl chlorides readily undergo attack by nucleophiles.Category: chlorides-buliding-blocks

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics