Month: December 2022

Synthesis and structure-activity relationships of potent antitumor active quinoline and naphthyridine derivatives was written by Srivastava, Sanjay K.;Jha, Amrita;Agarwal, Shiv K.;Mukherjee, Rama;Burman, Anand C.. And the article was included in Anti-Cancer Agents in Medicinal Chemistry in 2007.Recommanded Product: 96568-04-6 This article mentions the following:

The disease of cancer has been ranked second after cardiovascular diseases and plant-derived mols. have played an important role for the treatment of cancer. Nine cytotoxic plant-derived mols. such as vinblastine, vincristine, navelbine, etoposide, teniposide, taxol, taxotere, topotecan and irinotecan have been approved as anticancer drugs. Recently, epothilones are being emerging as future potential anti-tumor agents. However, targeted cancer therapy has now been rapidly expanding and small organic mols. are being exploited for this purpose. Amongst target specific small organic mols., quinazoline was found as one of the most successful chem. class in cancer chemotherapy as three drugs namely Gefitinib, Erlotinib and Canertinib belong to this series. Now, quinazoline related chem. classes such as quinolines and naphthyridines are being exploited in cancer chemotherapy and a number of mols. such as compounds EKB-569 (52), HKI-272 (78) and SNS-595 (127a) are in different phases of clin. trials. This review presents the synthesis of quinolines and naphthyridines derivatives, screened for anticancer activity since year 2000. The synthesis of most potent derivatives in each prototype has been delineated. A brief structure activity relationship for each prototype has also been discussed. It has been observed that aniline group at C-4, aminoacrylamide substituents at C-6, cyano group at C-3 and alkoxy groups at C-7 in the quinoline ring play an important role for optimal activity. While aminopyrrolidine functionality at C-7, 2′-thiazolyl at N-1 and carboxy group at C-3 in 1,8-naphthyridine ring are essential for eliciting the cytotoxicity. This review would help the medicinal chemist to design and synthesize mols. for targeted cancer chemotherapy. In the experiment, the researchers used many compounds, for example, Ethyl 3-(2,6-Dichloro-5-fluoro-3-pyridyl)-3-oxopropionate (cas: 96568-04-6Recommanded Product: 96568-04-6).

Ethyl 3-(2,6-Dichloro-5-fluoro-3-pyridyl)-3-oxopropionate (cas: 96568-04-6) 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. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Recommanded Product: 96568-04-6

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

Synthesis and neuroleptic activity of benzamides. cis-N-(1-Benzyl-2-methylpyrrolidin-3-yl)-5-chloro-2-methoxy-4-(methylamino)benzamide and related compounds was written by Iwanami, Sumio;Takashima, Mutsuo;Hirata, Yasufumi;Hasegawa, Osamu;Usuda, Shinji. And the article was included in Journal of Medicinal Chemistry in 1981.HPLC of Formula: 3438-16-2 This article mentions the following:

Fifty-two benzamides were designed and synthesized as potential neuroleptics and were evaluated for their inhibitory effects on apomorphine-induced stereotyped behavior in rats. In the metoclopramide analog (linear benzamides) series, N[2-(N-benzyl-N-methylamino)ethyl]-5-chloro-2-methoxy-4-(methylamino)benzamide-HCl (I) [61694-55-1] was ∼15 times more active than metoclopramide itself. In a cyclic series (benzamides of 1-benzyl-3-aminopyrrolidine), most compounds tested were more active than corresponding linear benzamides. YM-09151-2 (II) [75272-39-8] was the most active compound of all the compounds tested, but it had a high antistereotypic activity-to-cateleptogenicity ratio compared with haloperidol and metoclopramide. In the experiment, the researchers used many compounds, for example, 5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2HPLC of Formula: 3438-16-2).

5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2) 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. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.HPLC of Formula: 3438-16-2

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

Cyclometalation of 6-Phenyl-2,2′-Bipyridine and Iridium: Synthesis, Characterization, and Reactivity Studies was written by Young, Kenneth J. H.;Yousufuddin, Muhammed;Ess, Daniel H.;Periana, Roy A.. And the article was included in Organometallics in 2009.COA of Formula: C8H16Cl2Ir2 This article mentions the following:

Heating the potential tridentate 6-(4-R-phenyl)-2,2′-bipyridine ligand 1a (R = H), and derivatives 1b (R = CMe₃) and 1c (R = OH), with IrCl₃ hydrate in 2-methoxyethanol or acetone/H₂O followed by treatment with pyridine gave the unexpected bidentate cyclometalated NC dinuclear complexes [Ir(NC)Cl₂(C₅H₅N)]₂ (R = H (2aPy), CMe₃ (2bPy), OH (2cPy)), where cyclometalation occurs at the 3-position of the central pyridine ring as the major product. Altering the ligand/metal ratio from 1:1 to 2:1 produced a mixture of bis-cyclometalated complexes, Ir(NNC)(NC)Cl (R = H (3a), CMe₃ (3b), NNC = 6-(2-κ-4-R-C₆H₃)-2,2′-bipyridine-κ²N,N’), with tridentate and bidentate binding modes. Using discrete Ir^I synthons, such as Ir(DMSO)₃Cl or [Ir(cyclooctene)₂Cl]₂, gave a complicated mixture of products. However, when [Ir(C₂H₄)₂Cl]₂ was used, then the desired tridentate cyclometalated Ir(NNC) complex Ir(NNC)Et(C₂H₄)Cl (4) was synthesized cleanly. The dinuclear complex 2a-Py was converted to the corresponding mononuclear dichloride complexes Ir(NC)(NN^tBu)Cl₂ (5a, NN^tBu = κ²N,N’-4,4′-di-tert-butylbipyridine) upon refluxing with 4,4′-di-tert-butylbipyridine in N,N-dimethylacetamide (DMA). Treatment of 5a with ZnMe₂ gives Ir(NC)(NN^tBu)MeCl (6a). Abstraction of the chloride with AgOTf yields Ir(NC)(NN^tBu)MeOTf (7a). Complex 7a undergoes stoichiometric CH activation with arenes and shows catalytic activity for the H/D exchange between benzene and (trifluoro)acetic acids. In the experiment, the researchers used many compounds, for example, Chlorobis(ethylene)iridium(I) dimer (cas: 39722-81-1COA of Formula: C8H16Cl2Ir2).

Chlorobis(ethylene)iridium(I) dimer (cas: 39722-81-1) 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. 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.COA of Formula: C8H16Cl2Ir2

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

Rational Design, Optimization, and Biological Evaluation of Novel MEK4 Inhibitors against Pancreatic Adenocarcinoma was written by Kwong, Ada J.;Pham, Thao N. D.;Oelschlager, Hannah E.;Munshi, Hidayatullah G.;Scheidt, Karl A.. And the article was included in ACS Medicinal Chemistry Letters in 2021.Electric Literature of C4H5ClO2 This article mentions the following:

Growth, division, and development of healthy cells relies on efficient response to environmental survival cues. The conserved mitogen-activated protein kinase (MAPK) family of pathways interface extracellular stimuli to intracellular processes for this purpose. Within these pathways, the MEK family has been identified as a target of interest due to its clin. relevance. Particularly, MEK4 has drawn recent attention for its indications in pancreatic and prostate cancers. Here, we report two potent MEK4 inhibitors demonstrating significant reduction of phospho-JNK and antiproliferative properties against pancreatic cancer cell lines. Furthermore, mol. inhibition of MEK4 pathway activates the MEK1/2 pathway, with the combination of MEK1/2 and MEK4 inhibitors demonstrating synergistic effects against pancreatic cancer cells. Our inhibitors provided insight into the crosstalk between MAPK pathways and new tools for elucidating the roles of MEK4 in disease states, findings which will pave the way for better understanding of the MAPK pathways and development of addnl. probes. In the experiment, the researchers used many compounds, for example, (E)-4-Chlorobut-2-enoic acid (cas: 26340-58-9Electric Literature of C4H5ClO2).

(E)-4-Chlorobut-2-enoic acid (cas: 26340-58-9) 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. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.Electric Literature of C4H5ClO2

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

PEPPSI-type 2-methyl-2-propenyl-functionalized N-heterocyclic carbene-palladium complexes: Synthesis, structural characterization and catalytic activity on Suzuki-Miyaura reaction was written by Sahin, Neslihan. And the article was included in Journal of Molecular Structure in 2019.Quality Control of 1-(Chloromethyl)-3-methylbenzene This article mentions the following:

N-Heterocyclic carbenes (NHCs) have been known to be efficient ligands for the Suzuki-Miyaura cross-coupling. In this work, four novel 2-methyl-2-propenyl substituted N-heterocyclic carbene ligands were synthesized. They were used to produce four novel air-stable PEPPSI-type palladium-NHC complexes I (R = Bn, 3-MeC₆H₄CH₂, 1-naphthylmethyl, 9-anthrylmethyl). In addition, prepared complexes I were investigated as catalysts in the Suzuki-Miyaura coupling reaction under very mild conditions using a mixture of i-PrOH/water as a solvent and a base at the room temperature Under optimal reaction conditions, the expected biaryl products were obtained in moderate to high yields. In the experiment, the researchers used many compounds, for example, 1-(Chloromethyl)-3-methylbenzene (cas: 620-19-9Quality Control of 1-(Chloromethyl)-3-methylbenzene).

1-(Chloromethyl)-3-methylbenzene (cas: 620-19-9) belongs to organic chlorides. Chlorinated organic compounds are found in nearly every class of biomolecules and natural products including alkaloids, terpenes, amino acids, flavonoids, steroids, and fatty acids.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.Quality Control of 1-(Chloromethyl)-3-methylbenzene

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

C-H Fluoroalkylsulfinylation/Intramolecular Rearrangement for Precise Synthesis of Fluoroalkyl Sulfoxides was written by Xing, Shuya;Zhu, Yu-Yi;Liu, Wen;Liu, Yong;Zhang, Jing;Zhang, Huarong;Wang, Yan;Ni, Shao-Fei;Shao, Xinxin. And the article was included in Organic Letters in 2022.Recommanded Product: 2-Chlorobenzo[d]isothiazol-3(2H)-one 1,1-dioxide This article mentions the following:

An efficient methodol. to access various fluoroalkyl sulfoxides bearing ortho/para-functionalized amine scaffolds, e.g. I from arylhydroxylamines was described. The transformation was featured with new electrophilic trifluoromethylthiolated reagents, good functional group tolerance, and late-stage modification of complex bioactive scaffolds, providing a rapid access to prepare numerous trifluoromethyl- and difluoromethyl-substituted sulfoxides. Mechanism studies and d. functional theory calculations suggest this reaction goes through a nucleophilic trifluoromethylthiolation of arylhydroxylamine and subsequent internal 2,3-sigmatropic rearrangement involving a sulfur and oxygen transfer process. In the experiment, the researchers used many compounds, for example, 2-Chlorobenzo[d]isothiazol-3(2H)-one 1,1-dioxide (cas: 14070-51-0Recommanded Product: 2-Chlorobenzo[d]isothiazol-3(2H)-one 1,1-dioxide).

2-Chlorobenzo[d]isothiazol-3(2H)-one 1,1-dioxide (cas: 14070-51-0) belongs to organic chlorides. Chlorinated organic compounds are found in nearly every class of biomolecules and natural products including alkaloids, terpenes, amino acids, flavonoids, steroids, and fatty acids. 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: 2-Chlorobenzo[d]isothiazol-3(2H)-one 1,1-dioxide

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

Fengycin A analogs with enhanced chemical stability and antifungal properties was written by Gimenez, Diana;Phelan, Aoife;Murphy, Cormac D.;Cobb, Steven L.. And the article was included in Organic Letters in 2021.Formula: C19H15Cl This article mentions the following:

Fengycins are cyclic lipo-depsipeptides produced by Bacillus spp. that display potent antifungal properties but are chem. unstable. This instability has meant that no total synthesis of any fengycin has been published. Here we report the synthesis of fengycin A analogs that display enhanced antifungal properties and chem. stability under both basic and acidic conditions. The analogs prepared also demonstrate that the fengycin core structure can be modified and simplified without the loss of antifungal activity. In the experiment, the researchers used many compounds, for example, (Chloromethanetriyl)tribenzene (cas: 76-83-5Formula: C19H15Cl).

(Chloromethanetriyl)tribenzene (cas: 76-83-5) 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.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.Formula: C19H15Cl

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

Practical chemoselective aromatic substitution: the synthesis of N-(4-halo-2-nitrophenyl)benzenesulfonamide through the efficient nitration and halogenation of N-phenylbenzenesulfonamide was written by Yu, Xiao;Zhu, Wenjing;Liu, Hongyan;Liu, Yi;Li, Hongshuang;Han, Junfen;Duan, Guiyun;Bai, Zhushuang;Zhang, Pengfei;Xia, Chengcai. And the article was included in Organic & Biomolecular Chemistry in 2022.Name: 3-(Trifluoromethyl)benzene-1-sulfonyl chloride This article mentions the following:

A novel route involving the metal-promoted tandem nitration and halogenation of N-phenylbenzenesulfonamide to synthesize N-(4-halo-2-nitrophenyl)benzenesulfonamide derivatives has been developed. The method shows highly practical chemoselective and functional group compatibility. In addition, it employs insensitive and inexpensive Cu(NO₃)₂·3H₂O, Fe(NO₃)₃·9H₂O, and NH₄NO₃ as the nitration reagents, and it provides a direct approach for the preparation of 4-halo-2-nitroaniline, which is a crucial intermediate for the synthesis of benzimidazoles and quinoxaline derivatives 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. Organochlorines stimulate the central nervous system and cause convulsions, tremor, nausea, and mental confusion. Examples are dichlorodiphenyltrichloroethane (DDT), chlordane, lindane, endosulfan, and dieldrin. Alkyl chlorides readily react with amines to give substituted amines. Alkyl chlorides are substituted by softer halides such as the iodide in the Finkelstein reaction.Name: 3-(Trifluoromethyl)benzene-1-sulfonyl chloride

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

Photochemical Regioselective C(sp³)-H Amination of Amides Using N-Haloimides was written by Pan, Lei;Elmasry, Joseph;Osccorima, Tomas;Cooke, Maria Victoria;Laulhe, Sebastien. And the article was included in Organic Letters in 2021.Formula: C7H4ClNO3S This article mentions the following:

A metal-free regioselective C(sp³)-H amination of amides using N-haloimides in the presence of lithium tert-butoxide and visible light is presented herein. This photoexcited approach is straightforward, and it aminates a wide variety of amides under mild conditions without the use of photocatalysts, external radical initiators, or oxidants. A halogen-bonded intermediate between the tert-butoxide base and the N-haloimide is proposed to be responsible for the increased photoreactivity. Calculations show that the formation of this electron donor-acceptor complex presents an exergonic energy profile. In the experiment, the researchers used many compounds, for example, 2-Chlorobenzo[d]isothiazol-3(2H)-one 1,1-dioxide (cas: 14070-51-0Formula: C7H4ClNO3S).

2-Chlorobenzo[d]isothiazol-3(2H)-one 1,1-dioxide (cas: 14070-51-0) 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. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.Formula: C7H4ClNO3S

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

Preparation gemini non-ionic surfactants-based polyethylene oxide with variable hydrophobic tails for controlling the catalytic and antimicrobial activity of AgNPs was written by Shaban, Samy M.;Hamed, Eman H.;Elsharif, Asma M.;Elged, Ahmed H.;El Basiony, N. M.. And the article was included in Journal of Molecular Liquids in 2022.Name: 3,7-Bis(dimethylamino)phenothiazin-5-ium chloride This article mentions the following:

Three gemini non-ionic surfactant-based polyethylene oxide with variable hydrophobic tails; 8 carbons (GPEOC), 12 carbons (GPEOL), and 16 carbons (GPEOP) have been synthesized successfully. The synthesized gemini surfactant regulated the preparation of the nano-catalyst AgNPs for toxic materials removal. The AgNPs were prepared via photo-chem. reduction reaction based on using the sun light and the gemini surfactants as reducing and capping agents, resp. The surfactant′s tail exhibited a substantial impact on regulating the AgNPs preparation as confirmed by TEM, UV-vis, and DLS measurements. The surfactant GPEOP produced AgNPs with a uniform, dispersibility and smaller particles size 14.8 ± 5.4 nm comparing to other two gemini surfactants GPEOC and GPEOL with shorter hydrophobic tail. The surface and thermodn. performance of the GPEOC, GPEOL and GPEOP gemini non-ionic surfactants were dependent on both solution temperature and surfactant′s tail hydrophobicity. The adsorption ability is significantly improved as functional of temperature or hydrophobicity. Elongation the surfactant′s tail and increasing the temperature, promote lowering the critical micelle concentration and enhance the adsorption affinity at interfaces. The study was extended to investigate how the surfactant′s tail improve the catalytic performance of the AgNPs-based catalyst. The surfactant′s tail controlled the catalytic performance of the AgNPs regarding the methylene blue and p-nitrophenol removal, where the GPEOP/AgNPs exhibited highest catalytic activity. Addnl., the surfactant′s tail controlled the antimicrobial of the prepared surfactant and surfactant/AgNPs hybrid system. In the experiment, the researchers used many compounds, for example, 3,7-Bis(dimethylamino)phenothiazin-5-ium chloride (cas: 61-73-4Name: 3,7-Bis(dimethylamino)phenothiazin-5-ium chloride).

3,7-Bis(dimethylamino)phenothiazin-5-ium chloride (cas: 61-73-4) 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. 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: 3,7-Bis(dimethylamino)phenothiazin-5-ium chloride

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