Tag: M.W=200-250

Arseniyadis, Simeon; Kyler, Keith S.; Watt, David S. published the artcile< Addition and substitution reactions of nitrile-stabilized carbanions>, Recommanded Product: 3-Chlorophenethyl Bromide, the main research area is review Carbanions; review Reactions; review Nitrile Stabilized; review Addition; review Substitution.

A review of the article Addition and substitution reactions of nitrile-stabilized carbanions.

Organic Reactions (Hoboken, NJ, United States) published new progress about Aminoplasts Role: RGT (Reagent), RACT (Reactant or Reagent). 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, Recommanded Product: 3-Chlorophenethyl Bromide.

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

Tu, Guangliang; Wang, Dongjie; Yuan, Chunchen; Zhang, Jingyu; Zhao, Yingsheng published the artcile< Palladium-Catalyzed Para-Selective Difluoromethylation of Arene Esters>, Related Products of 162046-61-9, the main research area is palladium catalyzed regioselective fluoromethylation arene ester.

Highly efficient, palladium-catalyzed, para-selective difluoromethylation of arene esters has been developed using [1,1′-biphenyl-2-yl]dicyclohexylphosphine as the effective ligand. A wide variety of arene esters bearing various functional groups were all compatible with the reaction conditions, leading to para-difluoromethylated products in moderate to good yields. Moreover, benzamide and benzenesulfonamide were also well-tolerated, suggesting that this novel catalyst system has broad applications to a variety of substrates.

Journal of Organic Chemistry published new progress about Arenesulfonamides Role: RCT (Reactant), RACT (Reactant or Reagent). 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Related Products of 162046-61-9.

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

Chen, Zhenliang; Chen, Zhiyong; Jiang, Yaozhong; Hu, Wenhao published the artcile< The synthesis of baclofen and GABOB via Rh(II) catalyzed intramolecular C-H insertion of α-diazoacetamides>, Related Products of 16799-05-6, the main research area is amino acid derivative gabapentin baclofen GABOB preparation; diazoacetamide insertion rhodium catalyst gamma lactam hydrolytic ring opening.

The synthesis of gabapentin, baclofen and GABOB is reported via hydrolysis of the corresponding N-tert-Bu γ-lactams, which were obtained from Rh(II) catalyzed intramol. C-H insertion of α-diazoacetamides.

Tetrahedron published new progress about Amino acids Role: SPN (Synthetic Preparation), PREP (Preparation). 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, Related Products of 16799-05-6.

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

Zeng, Jie; Zhang, Zhijun; Zhu, Qi; Jiang, Zhiyan; Zhong, Guohua published the artcile< Simplification of natural β-carboline alkaloids to obtain indole derivatives as potent fungicides against rice sheath blight>, Safety of 2-(Trifluoromethoxy)benzoyl chloride, the main research area is indole preparation Agrochem fungicide SAR; Rhizoctonia solani; fungicidal activity; indole; simplification; β-carboline.

The increasing resistance of rice sheath blight caused by Rhizoctonia solani highlights the need for highly effective and environmentally benign agents. Natural β-carboline alkaloids were simplified to obtain a series of indole derivatives, and their fungicidal activity and preliminary mode of action against R. solani were also evaluated. The initial hit indole displayed significant fungicidal activity with an EC50 value of 25.56μg/mL, and was selected for further optimization. Importantly, compound 4-fluroindole the most active compound, had an EC50 value of 0.62μg/mL, and approx. 300-fold more potent than validamycin A (EC50 = 183.00μg/mL). In-vivo bioassay also demonstrated that compound 4-fluoroindole showed better fungicidal activities than validamycin A. Moreover, the mechanism studies revealed that compound 4-fluoroindole not only caused remarkable morphol. and structural alterations of R. solani hyphae, but also induced the loss of mitochondrial membrane potential and interfered with DNA synthesis. Therefore, compound 4-fluoroindole showed superior fungicidal activity against R. solani, and the elucidated mode of action supported the potential application of compound 4-fluoroindole against rice sheath blight.

Molecules published new progress about Agrochemical fungicides. 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Safety of 2-(Trifluoromethoxy)benzoyl chloride.

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

Li, Xin-yang; Wang, De-pu; Li, Shuai; Xue, Wen-han; Qian, Xin-hua; Liu, Kai-li; Li, Yu-heng; Lin, Qi-qi; Dong, Gang; Meng, Fan-hao; Jian, Ling-yan published the artcile< Discovery of N-(1,3,4-thiadiazol-2-yl)benzamide derivatives containing a 6,7-methoxyquinoline structure as novel EGFR/HER-2 dual-target inhibitors against cancer growth and angiogenesis>, Category: chlorides-buliding-blocks, the main research area is dimethoxy quinolinyloxymethyl thiazolyl benzamide preparation EGFR HER2 inhibition antitumor; Angiogenesis; Dual-target inhibitor; EGFR; HER-2.

Targeting EGFR and HER-2 is an essential direction for cancer treatment. Here, a series of N-(1,3,4-thiadiazol-2-yl)benzamide derivatives containing a 6,7-methoxyquinoline structure was designed and synthesized to serve as EGFR/HER-2 dual-target inhibitors. The kinase assays verified that target compounds could inhibit the kinase activity of EGFR and HER-2 selectively. The results of CCK-8 and 3D cell viability assays confirmed that target compounds had excellent anti-proliferation ability against breast cancer cells (MCF-7 and SK-BR-3) and lung cancer cells (A549 and H1975), particularly against SK-BR-3 cells, while the inhibitory effect on healthy breast cells (MCF-10A) and lung cells (Beas-2B) was weak. Among them, the hit compound YH-9 binded to EGFR and HER-2 stably in mol. dynamics studies. Further studies found that YH-9 could induce the release of cytochrome c and inhibit proliferation by promoting ROS expression in SK-BR-3 cells. Moreover, YH-9 could diminish the secretion of VEGF and bFGF factors in SK-BR-3 cells, then inhibited tube formation and angiogenesis. Notably, YH-9 could effectively inhibit breast cancer growth and angiogenesis with little toxicity in the SK-BR-3 cell xenograft model. Taken together, in vitro and in vivo results revealed that YH-9 had high drug potential as a dual-target inhibitor of EGFR/HER-2 to inhibit breast cancer growth and angiogenesis.

Bioorganic Chemistry published new progress about Angiogenesis. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Category: chlorides-buliding-blocks.

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

Pettersson, Martin; Johnson, Douglas S.; Subramanyam, Chakrapani; Bales, Kelly R.; am Ende, Christopher W.; Fish, Benjamin A.; Green, Michael E.; Kauffman, Gregory W.; Mullins, Patrick B.; Navaratnam, Thayalan; Sakya, Subas M.; Stiff, Cory M.; Tran, Tuan P.; Xie, Longfei; Zhang, Liming; Pustilnik, Leslie R.; Vetelino, Beth C.; Wood, Kathleen M.; Pozdnyakov, Nikolay; Verhoest, Patrick R.; O’Donnell, Christopher J. published the artcile< Design, Synthesis, and Pharmacological Evaluation of a Novel Series of Pyridopyrazine-1,6-dione γ-Secretase Modulators>, Application of C8H8BrCl, the main research area is gamma secretase modulator pyridopyrazinedione design synthesis beta amyloid reduction.

Herein we describe the design and synthesis of a novel series of γ-secretase modulators (GSMs) that incorporates a pyridopiperazine-1,6-dione ring system. To align improved potency with favorable ADME and in vitro safety, we applied prospective physicochem. property-driven design coupled with parallel medicinal chem. techniques to arrive at a novel series containing a conformationally restricted core. Lead compound I exhibited good in vitro potency and ADME, which translated into a favorable in vivo pharmacokinetic profile. Furthermore, robust reduction of brain Aβ42 was observed in guinea pig at 30 mg/kg dosed orally. Through chem. biol. efforts involving the design and synthesis of a clickable photoreactive probe, we demonstrated specific labeling of the presenilin N-terminal fragment (PS1-NTF) within the γ-secretase complex, thus gaining insight into the binding site of this series of GSMs.

Journal of Medicinal Chemistry published new progress about Affinity chromatography (with streptavidin). 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, Application of C8H8BrCl.

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

Akama, Tsutomu; Dong, Chen; Virtucio, Charlotte; Freund, Yvonne R.; Chen, Daitao; Orr, Matthew D.; Jacobs, Robert T.; Zhang, Yong-Kang; Hernandez, Vincent; Liu, Yang; Wu, Anne; Bu, Wei; Liu, Liang; Jarnagin, Kurt; Plattner, Jacob J. published the artcile< Discovery and structure-activity relationships of 6-(benzoylamino)benzoxaboroles as orally active anti-inflammatory agents>, Application In Synthesis of 162046-61-9, the main research area is benzoxaborole amid preparation structure activity relationship antiinflammatant; Anti-inflammatory; Benzoxaborole; Collagen-induced arthritis; Cytokine; Interleukin-1beta; Interleukin-6; Pharmacokinetics; Structure–activity relationships; Tumor necrosis factor-alpha.

Structure-activity relationships of 6-(benzoylamino)benzoxaborole analogs were investigated for the inhibition of TNF-α, IL-1β, and IL-6 from lipopolysaccharide stimulated peripheral blood mononuclear cells. One compound showed potent activity against all three cytokines with IC50 values between 0.19-0.50 μM, inhibited LPS-induced TNF-α and IL-6 elevation in mice and improved collagen-induced arthritis in mice. This compound is considered to be a promising lead for novel anti-inflammatory agent with an excellent pharmacokinetic profile.

Bioorganic & Medicinal Chemistry Letters published new progress about Anti-inflammatory agents. 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Application In Synthesis of 162046-61-9.

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

Amperayani, Karteek Rao; Parimi, Uma Devi published the artcile< Effect of silk strength by dietary supplementation of silk worm with 1,3,4-thiadiazoles, in silico and in vitro Bombyx mori DNA binding studies>, Product Details of C8H6ClN3S, the main research area is Bombyx silk strength feeding thiadiazole DNA binding.

In silico and in vitro DNA binding studies were carried out on silk worm DNA to determine the efficiency of 1,3,4-thiadiazoles (Th1-9) on Bombyx mori larvae during their 5th instar larval stage to increase the tensile strength, quality and quantity of biopolymer silk. These compounds were synthesized using ultrasonication method and supplied in ultra-dose as food supplement along with mulberry leaves to Bombyx mori and recorded the growth and other parameters of silkworm, cocoon parameters and mech. testing of silk filament. Tensile Strength, elongation and quantity of the silk was higher in larvae fed with synthesized compound in comparison with control larvae. This increase in strength and quality was due to the strong binding interactions of thiadiazoles moiety with silk worm DNA which was confirmed by higher binding energy values showed in In silco studies and DNA binding assay results.

Pharma Chemica published new progress about Binding energy. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Product Details of C8H6ClN3S.

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

Park, Seojeong; Hong, Eunji; Kwak, Soo Yeon; Jun, Kyu-Yeon; Lee, Eung-Seok; Kwon, Youngjoo; Na, Younghwa published the artcile< Synthesis and biological evaluation of C1-O-substituted-3-(3-butylamino-2-hydroxy-propoxy)-xanthen-9-one as topoisomerase IIα catalytic inhibitors>, COA of Formula: C8H8BrCl, the main research area is xanthone preparation topoisomerase IIa catalytic inhibitory anticancer activity; Anticancer agents; C1-alkyl and arylalkyl substituted xanthones; Topoisomerase IIα catalytic inhibitor.

Topoisomerase II poison blocks the transitorily generated DNA double-strand breaks (DSBs) from religation, thereby causes severe DNA damage and gene toxicity. While topoisomerase II catalytic inhibitor does not form cleavable DNA-enzyme complex because its function attributes to inhibition of the catalytic steps of the enzyme such as before generating DNA DSBs or in the last step of the catalytic cycle after religation. It has been reported that the stabilizing effect of etoposide on transient cleavable DNA-topoisomerase IIβ complex attributes to its secondary malignancy. Therefore, topoisomerase IIα has been considered as more attractive target than topoisomerase IIβ for the development of chemotherapeutic agents. In the previous work, we reported compounds as novel topoisomerase IIα catalytic inhibitors targeting for ATP binding site of human topoisomerase IIα ATP-binding domain. As a continuous work, we have designed and synthesized 43 compounds of C1-O-alkyl and arylalkyl substituted compounds with or without methoxy group on ring A. In the topoisomerase IIα inhibitory test, among the tested C1-O-4-chlorophenethyl substituted compounds I (R1 = H, OMe) were more active than others, and compound I (R1 = H) showed strongest topoisomerase IIα inhibitory activity with 94.4% and 23.0% inhibition, resp., at 100 and 20 μM. Compounds I (R1 = H, OMe) have also showed much enhanced cytotoxic activity against T47D cells; IC50 (μM): 0.63 ± 0.01 and 0.19 ± 0.02, resp., which are stronger than reference drugs. Band depletion assay and cleavage complex assay results showed compounds I (R1 = H, OMe) were potential topoisomerase IIα catalytic inhibitor with low DNA damage.

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, COA of Formula: C8H8BrCl.

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

Chiu, George; Li, Shengjian; Connolly, Peter J.; Pulito, Virginia; Liu, Jingchun; Middleton, Steven A. published the artcile< (Phenylpiperidinyl)cyclohexylsulfonamides: Development of α1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS)>, HPLC of Formula: 351003-34-4, the main research area is phenylpiperidinylcyclohexyl benzenesulfonamide preparation alpha1a alpha1d selective adrenergic receptor antagonist; benign prostatic hyperplasia lower urinary tract drug phenylpiperidinylcyclohexyl benzenesulfonamide.

Although α1 adrenergic receptor blockers can be very effective for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS), their usage is limited by CV-related side-effects that are caused by the subtype non-selective nature of the current drugs. To overcome this problem, it was hypothesized that a α1a/1d subtype selective antagonist would bring more benefit for the therapy of BPH/LUTS. In developing such selective α1a/1d ligands, (phenylpiperidinyl)cyclohexylsulfonamides (e.g. N-[cis-4-[4-(2-isopropoxyphenyl)piperidin-1-yl]cyclohexyl]-3,4-dimethoxybenzenesulfonamide) were synthesized and evaluated for binding to three cloned human α1-adrenergic receptor subtypes. Many compounds showed equal affinity for both α1a and α1d subtypes with good selectivity vs. the α1b subtype.

Bioorganic & Medicinal Chemistry Letters published new progress about Arenesulfonamides Role: PAC (Pharmacological Activity), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), PREP (Preparation), USES (Uses). 351003-34-4 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H5ClF2O3S, HPLC of Formula: 351003-34-4.

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