M.W=200-250 Archives - Page 83 of 86 - Chlorides-buliding-blocks

Zhou, Zhong-Zhen’s team published research in European Journal of Medicinal Chemistry in 2017-09-29 | 2382-10-7

European Journal of Medicinal Chemistry published new progress about Antiproliferative agents. 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, SDS of cas: 2382-10-7.

Zhou, Zhong-Zhen; Shi, Xiu-Dong; Feng, Hong-Fang; Cheng, Yu-Fang; Wang, Hai-Tao; Xu, Jiang-Ping published the artcile< Discovery of 9H-purines as potential tubulin polymerization inhibitors: Synthesis, biological evaluation and structure-activity relationships>, SDS of cas: 2382-10-7, the main research area is methoxyphenyl aminopurine preparation antitumor cytotoxicity tubulin polymerization inhibitor SAR; benzyl chloropurine preparation antitumor cytotoxicity tubulin polymerization inhibitor apoptosis; 9H-purins; Antiproliferative activity; Apoptosis; Cell cycle arrest; Tubulin-polymerization inhibitors.

Two series of N-(4-methoxyphenyl)-N-methyl-9H-purin-6-amines I [R1 = H, Cl; R2 = H, Me, 4-methoxybenzyl, etc.] and 9-substituted benzyl-6-chloro-9H-purines II [R1 = H, Cl; R2 = 4-methoxybenzyl, 3,4-dimethoxybenzyl, 3,5-dimethoxybenzyl, 3,4,5-trimethoxybenzyl] were designed and synthesized. Their antiproliferative activities against human myelogenous leukemia (K562), human neuroblastoma (SH-SY5Y) and gastric cancer (AGS) cell lines were evaluated using the MTT assay. The preliminary results indicated that compounds I [R1 = Cl; R2 = Me] and II [R1 = Cl; R2 = 4-methoxybenzyl, 3,4-dimethoxybenzyl, 3,5-dimethoxybenzyl, 3,4,5-trimethoxybenzyl] displayed low-micromole GI50 values against all tested cell lines. In addition, compounds I [R1 = H; R2 = 4-methoxybenzyl, 3,4,5-trimethoxybenzyl] showed wonderful antiproliferative activities towards SH-SY5Y cells with selectivity of >230-fold over K562 and AGS cells. Among them, compounds I [R1 = Cl; R2 = Me], [R1 = H; R2 = 3,4-dimethoxybenzyl, 3,4,5-trimethoxybenzyl] and II [R1 = Cl; R2 = 3,5-dimethoxybenzyl] with good antitumor activities exhibited high selectivity for tumor cell lines over immortalized mouse hippocampal (HT22) cell line. Moreover, compound I [R1 = Cl; R2 = Me] with sub-micromole GI50 values toward AGS cells exhibited moderate tubulin polymerization inhibitory activity and induced apoptosis at G2/M phase arrest with a dose-dependent manner in the human AGS cells.

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

Hannout, I B’s team published research in Egyptian Journal of Pharmaceutical Sciences in 1986 | 42413-03-6

Egyptian Journal of Pharmaceutical Sciences published new progress about 42413-03-6. 42413-03-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O2S, Computed Properties of 42413-03-6.

Hannout, I. B.; El-Sharief, A. M. S.; Ismail, I. M.; Mohamed, Y. A.; Ammar, Y. A.; Zahran, M. A. published the artcile< Some alkylated and chlorinated benzenesulfonamides with expected insecticidal and bactericidal activities>, Computed Properties of 42413-03-6, the main research area is benzenesulfonamide chloro preparation bactericide; chlorobenzenesulfonamide preparation bactericide.

Benzenesulfonic acid derivatives I (R1 = alkylamino, cyclohexylamino, substituted anilino, furfurylamino, pyrimidinylamino, substituted phenoxy) and II (R2 = cyclohexylamino, substituted anilino, pyridylamino, piperidino, morpholino) were prepared from the resp. benzenesulfonyl chlorides. I and II exhibited bactericidal activity.

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

Bradley, D C’s team published research in Journal of the Chemical Society in 1964 | 16799-05-6

Journal of the Chemical Society published new progress about Hydrolysis. 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, Synthetic Route of 16799-05-6.

Bradley, D. C.; Prevedorou-Demas, C. published the artcile< Metal oxide trialkylsilyl oxide polymers. II. Zirconium oxide trimethylsilyl oxide polymers>, Synthetic Route of 16799-05-6, the main research area is .

The partial hydrolysis of tetrakis(trimethylsilyloxy)zirconium in dioxane has been studied. Solid polymeric [ZrOx(OSiMe3)4-2x]n, which were soluble in organic solvents, were obtained. The variation of the number average degree of polymerization, n, as a function of the degree of hydrolysis, x, was analyzed in terms of structural models. At 150° in vacuo, the polymers disproportionated to tetrakis(trimethylsilyloxy)zirconium and more highly condensed polymers [ZrOy(OSiMe3)(4-2y)]m, where y > x, and m > n.

Journal of the Chemical Society published new progress about Hydrolysis. 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, Synthetic Route of 16799-05-6.

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

Joseph, Alex’s team published research in Orbital: The Electronic Journal of Chemistry in 2010-06-30 | 70057-67-9

Orbital: The Electronic Journal of Chemistry published new progress about Antitumor agents. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Synthetic Route of 70057-67-9.

Joseph, Alex; Pai, Aravinda; Srinivasan, K. K.; Kedar, Tukaram; Thomas, Angel Treasa; Jessy, E. M.; Singla, Rajeev K. published the artcile< Synthesis and anticancer activity of some novel 3-(1,3,4-thiadiazol-2-yl)-quinazolin-4(3H)-ones>, Synthetic Route of 70057-67-9, the main research area is thiadiazolylquinazolinone preparation anticancer; quinazolinone thiadiazolyl preparation anticancer.

The synthesis of various thiadiazole-substituted quinazolin-4(3H)-ones was reported. Novel 3-(1,3,4-thiadiazol-2-yl)quinazolin-4(3H)-ones were synthesized by reaction of 5-alkyl/aryl-1,3,4-thiadiazol-2-amines with 2-methyl/phenyl-4H-1,3-benzoxazin-4-ones in the presence of pyridine. All the synthesized compounds were characterized by spectra and phys. data. In vitro anticancer activity of all the synthesized compounds was determined by MTT assay on HeLa cells. Most active compounds from in vitro studies were further evaluated for in vivo activity on Liquid tumor (Ehrlich’s Ascites Carcinoma; EAC)-induced mice. The anticancer activity of one of the compounds was comparable to that of cisplatin against HeLa cells, and this compound was also effective in preventing the growth of tumor in mice as indicated by decrease in progressive gain in body weight as well as increase in life span.

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

Wan, Zehong’s team published research in Bioorganic & Medicinal Chemistry Letters in 2003-03-24 | 2382-10-7

Bioorganic & Medicinal Chemistry Letters published new progress about Crystal structure. 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, Safety of 2,6-Dichloro-9-methyl-9H-purine.

Wan, Zehong; Boehm, Jeffrey C.; Bower, Michael J.; Kassis, Shouki; Lee, John C.; Zhao, Baoguang; Adams, Jerry L. published the artcile< N-Phenyl-N-purin-6-yl ureas: The design and synthesis of p38α MAP kinase inhibitors>, Safety of 2,6-Dichloro-9-methyl-9H-purine, the main research area is trisubstituted phenyl purine inhibitor p38 kinase preparation; crystal structure purine inhibitor p38 kinase.

The design, synthesis and SAR of a series of 2,6,9-trisubstituted purine inhibitors of p38α kinase is reported. Synthetic routes were devised to allow for array synthesis in which all three points of diversity could be facilely explored. The binding of this novel series to p38α kinase, which was predicted to have several key interactions in common with SB-203580, was confirmed by x-ray crystallog. of I (p38 IC50=82 nM).

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

Weibel, Peter A’s team published research in Helvetica Chimica Acta in 1973 | 16799-05-6

Helvetica Chimica Acta published new progress about Amines Role: PRP (Properties). 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, Reference of 16799-05-6.

Weibel, Peter A.; Hesse, Manfred published the artcile< Mass spectrometric behavior of nitrogen-containing compounds. 19. Substituent effect on mass spectrometric fragmentation. N-methylβ,β'-diphenyldiethylamines>, Reference of 16799-05-6, the main research area is mass spectra diphenethylamine; amine diphenethyl mass spectra.

The mass spectra of the title amines (I; R = H, p-NO2, m-NH2, p-F, m-OMe, etc.), prepared from N-methylphenethylamine reaction with RC6H4CH2CH2Br (R same as above) were examined The main mass spectral fragmentation mechanisms were discussed.

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

Emert-Sedlak, Lori A’s team published research in Bioorganic & Medicinal Chemistry Letters in 2016-03-01 | 16799-05-6

Bioorganic & Medicinal Chemistry Letters published new progress about AIDS (disease). 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, SDS of cas: 16799-05-6.

Emert-Sedlak, Lori A.; Loughran, H. Marie; Shi, Haibin; Kulp, John L. III; Shu, Sherry T.; Zhao, Jielu; Day, Billy W.; Wrobel, Jay E.; Reitz, Allen B.; Smithgall, Thomas E. published the artcile< Synthesis and evaluation of orally active small molecule HIV-1 Nef antagonists>, SDS of cas: 16799-05-6, the main research area is antiviral HIV AIDS Nef antagonist; Antiretroviral drug discovery; HIV Nef; HIV-1; Nef inhibitors.

The HIV-1 Nef accessory factor enhances viral replication and promotes immune system evasion of HIV-infected cells, making it an attractive target for drug discovery. Recently the authors described a novel class of diphenylpyrazolodiazene compounds that bind directly to Nef in vitro and inhibit Nef-dependent HIV-1 infectivity and replication in cell culture. However, these first-generation Nef antagonists have several structural liabilities, including an azo linkage that led to poor oral bioavailability. The azo group was therefore replaced with either a one- or two-carbon linker. The resulting set of nonazo analogs retained nanomolar binding affinity for Nef by surface plasmon resonance, while inhibiting HIV-1 replication with micromolar potency in cell-based assays without cytotoxicity. Computational docking studies show that these nonazo analogs occupy the same predicted binding site within the HIV-1 Nef dimer interface as the original azo compound Computational methods also identified a hot spot for inhibitor binding within this site that is defined by conserved HIV-1 Nef residues Asp108, Leu112, and Pro122. Pharmacokinetic evaluation of the nonazo B9 analogs in mice showed that replacement of the azo linkage dramatically enhanced oral bioavailability without substantially affecting plasma half-life or clearance. The improved oral bioavailability of nonazo diphenylpyrazolo Nef antagonists provides a starting point for further drug lead optimization in support of future efficacy testing in animal models of HIV/AIDS.

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

Trost, Barry M’s team published research in Angewandte Chemie, International Edition in 2019 | 2382-10-7

Angewandte Chemie, International Edition published new progress about Aldimines Role: RCT (Reactant), RACT (Reactant or Reagent). 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, HPLC of Formula: 2382-10-7.

Trost, Barry M.; Jiao, Zhiwei; Hung, Chao-I. published the artcile< Elaborating Complex Heteroaryl-Containing Cycles via Enantioselective Palladium-Catalyzed Cycloadditions>, HPLC of Formula: 2382-10-7, the main research area is methylenecyclopentane methylenepyrrolidine methylenetetrahydrofuran methylenespirotetrahydrofuranindolon stereoselective preparation; palladium diamidophosphite catalyst regioselective stereoselective cycloaddition heteroaryl allylic carbonate; chalcone nitroalkene aldimine aldehyde stereoselective cycloaddition heteroaryl allylic carbonate; asymmetric catalysis; cycloadditions; heterocycles; palladium; trimethylenemethane.

In the presence of allyl(cyclopentadienyl)palladium and a nonracemic diamidophosphite ligand, allylic carbonates containing heteroaryl and nitrophenyl moieties such as I underwent regioselective, diastereoselective, and enantioselective cycloaddition reactions with chalcones, electron-deficient alkenes, aryl aldimines, and nitrobenzaldehydes or N-methylisatin to yield nonracemic methylenecyclopentanes such as II, methylenepyrrolidines, methylenetetrahydrofurans, and methylenespirotetrahydrofuranindolones. Fused and bridged products were also prepared from nitrocycloalkenes and tropone. Allylic carbonates containing many classes of nitrogen-containing aromatics, including pyridines, quinolines, pyrimidines, various azoles and purines, were compatible substrates.

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

Carroll, William A’s team published research in Bioorganic & Medicinal Chemistry Letters in 2007-07-15 | 2905-54-6

Bioorganic & Medicinal Chemistry Letters published new progress about Analgesics. 2905-54-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6Cl2O2, Formula: C8H6Cl2O2.

Carroll, William A.; Kalvin, Douglas M.; Perez Medrano, Arturo; Florjancic, Alan S.; Wang, Ying; Donnelly-Roberts, Diana L.; Namovic, Marian T.; Grayson, George; Honore, Prisca; Jarvis, Michael F. published the artcile< Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X7 antagonists>, Formula: C8H6Cl2O2, the main research area is purinoceptor antagonist analgesic triazole preparation SAR.

Structure-activity relationship (SAR) studies were conducted around early tetrazole-based leads 3 and 4. Replacements for the tetrazole core were investigated and the pendant benzyl substitution was reoptimized with a triazole isostere. Triazole-based P2X7 antagonists were identified with similar potency to the lead compound 4 but with improved physiochem. properties. Compound 12 (I) was active in a rat model of neuropathic pain.

Bioorganic & Medicinal Chemistry Letters published new progress about Analgesics. 2905-54-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6Cl2O2, Formula: C8H6Cl2O2.

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

Kerru, Nagaraju’s team published research in Monatshefte fuer Chemie in 2020-06-30 | 70057-67-9

Monatshefte fuer Chemie published new progress about Antibacterial agents. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Related Products of 70057-67-9.

Kerru, Nagaraju; Gummidi, Lalitha; Bhaskaruni, Sandeep V. H. S.; Maddila, Surya Narayana; Jonnalagadda, Sreekantha B. published the artcile< Ultrasound-assisted synthesis and antibacterial activity of novel 1,3,4-thiadiazole-1H-pyrazol-4-yl-thiazolidin-4-one derivatives>, Related Products of 70057-67-9, the main research area is diphenylpyrazolyl phenylthiadiazolyl thiazolidinone preparation ultrasonication green chem antibacterial SAR.

An efficient multicomponent method was reported for the synthesis of biol. active 1,3,4-thiadiazole-1H-pyrazol-4-yl-thiazolidin-4-one hybrids I [R = H, 3-Cl, 3,4,5-tri-MeO, etc.] from the reaction of pyrazole-4-carbaldehyde, 5-(substituted phenyl)-1,3,4-thiadiazol-2-amines and 2-mercaptoacetic acid in ethanol under ultrasound irradiation Reactions gave excellent yields (91-97%) of desired products in short times (55-65 min) at 50°C. All the twelve new thiazolidin-4-one derivatives I were fully characterized by spectroscopic techniques and were screened for their antibacterial activity. Among the screened hybrids, derivatives I [R = 3-O2N, 4-O2N] showed fourfold (MBC = 156.3μg/cm3) and twofold (MBC = 312.5μg/cm3) stronger potency against Pseudomonas aeruginosa strain as compared to the standard ciprofloxacin. SAR studies revealed the importance of the functional groups on the Ph ring of 1,3,4-thiadiazol-2-amine moiety for varying bacterial activity. The electron-withdrawing (NO2) group at para- and meta-position played a significant role in enhancing the antibacterial activity. The prominent features of the described protocol are excellent yields, green protocol, catalyst-free, high atom economy (94%) and excellent carbon efficiency (98%).

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