Category: 385-00-2

An article Fluorination as tool to improve bioanalytical sensitivity and COX-2-selective antitumor activity of cobalt alkyne complexes WOS:000493493400011 published article about ACETYLSALICYLIC-ACID; ABSORPTION-SPECTROMETRY; PROTEIN-BINDING; MOLECULAR ABSORPTION; METAL-COMPLEXES; CHEMISTRY; EFFICACY; IMPACT; DRUGS; CELLS in [Baecker, Daniel; Obermoser, Victoria; Kirchner, Elisabeth Anna; Hupfauf, Andrea; Gust, Ronald] Univ Innsbruck, CCB, CMBI, Inst Pharm,Dept Pharmaceut Chem, A-6020 Innsbruck, Austria; [Kircher, Brigitte] Innsbruck Med Univ, Dept Internal Med Hematol & Oncol 5, Immunobiol & Stem Cell Lab, Anichstr 35, A-6020 Innsbruck, Austria; [Kircher, Brigitte] Tyrolean Canc Res Inst, Innrain 64, A-6020 Innsbruck, Austria in 2019, Cited 59. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2. HPLC of Formula: C7H4F2O2

The cobalt alkyne complex [(prop-2-ynyl)-2-acetoxybenzoate]dicobalthexacarbonyl (Co-ASS) is an auspicious lead, which exhibits its anticancer activity mainly by inhibition of both cyclooxygenases (COX-1 and COX-2). Since COX-2 participates in carcinogenesis, a selective inhibition of that isoenzyme is aimed. To study if fluorination increases the COX-2/COX-1 inhibition ratio of the lead, substitution was respectively performed in the positions 3, 4, 5, and 6 of the aromatic moiety. The complexes 3/4/5F-Co-ASS and to a much lower extent also 6F-Co-ASS showed cytotoxic, antimetabolic, and apoptotic effects in COX-1/2-positive HT-29 and MDA-MB-231 cells and remarkably less activity in the COX-1/2-negative MCF-7 cell line. The metabolic activity in MCF-7 cells was even unaffected up to a concentration of 40 mu M. With exception of 6F-Co-ASS, the complexes strongly reduced the PGE(2) synthesis in HT-29 cells and all complexes inhibited COX-2 more effectively than COX-1 in an assay at isolated enzymes. These findings point to an interference in the COX cascade as part of the mode of antitumor action. The limited cellular effects of 6F-Co-ASS are related to its poor uptake as determined by HR CS AAS/MAS. Moreover, the cellular uptake studies confirm fluorination as beneficial tool for bioanalytical labeling. The higher quantification of fluorine by HR CS MAS makes this method about 5-fold more sensitive than HR CS AAS measuring cobalt. As a further positive result, 3/4/5/6-Co-ASS demonstrated high selectivity to tumor cells due to lack of antimetabolic activity against the non-tumorigenic bone marrow stromal cell line HS-5.

HPLC of Formula: C7H4F2O2. About 2,6-Difluorobenzoic acid, If you have any questions, you can contact Baecker, D; Obermoser, V; Kirchner, EA; Hupfauf, A; Kircher, B; Gust, R or concate me.

Reference:
Isothiazole – Wikipedia,
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Name: 2,6-Difluorobenzoic acid. In 2020 BIOORGAN MED CHEM published article about BRAF MUTATIONS; SIGNALING PATHWAY; RAF KINASE; MULTIKINASE INHIBITOR; MAPK PATHWAY; MELANOMA; MUTANT; SENSITIVITY; ACTIVATION; SORAFENIB in [Abdel-Maksoud, Mohammed S.] Natl Res Ctr NRC ID 60014618, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Giza 12622, Egypt; [Ali, Eslam M. H.; Ammar, Usama M.; Mersal, Karim I.; Oh, Chang-Hyun] KIST Sch, Korea Inst Sci & Technol, Ctr Biomat, Seoul 02792, South Korea; [Ali, Eslam M. H.; Ammar, Usama M.; Mersal, Karim I.; Oh, Chang-Hyun] Univ Sci & Technol UST, Daejeon 34113, South Korea; [Ali, Eslam M. H.] Modern Univ Technol & Informat MTI, Pharmaceut Chem Dept, Fac Pharm, Cairo 12055, Egypt; [Ammar, Usama M.] Ahram Canadian Univ, Pharmaceut Chem Dept, Fac Pharm, Giza 12566, Egypt; [Yoo, Kyung Ho] Korea Inst Sci & Technol, Chem Kinom Res Ctr, Seoul, South Korea in 2020, Cited 37. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2.

Several pyrrolo[2,3-b]pyridine-based B-RAF inhibitors are well known and some of them are currently FDA approved as anticancer agents. Based on the structure of these FDA approved B-V600E-RAF inhibitors, two series of pyrrolo[2,3-b]pyridine scaffold were designed and synthesized in attempt to develop new potent B-V600E-RAF inhibitors. The 38 synthesized compounds were biologically evaluated for their B-V600E-RAF inhibitory effect at single dose (10 mu M). Compounds with high percent inhibition were tested to determine their IC50 over (V600E)BRAF. Compounds 34e and 35 showed the highest inhibitory effect with IC50 values of 0.085 mu M and 0.080 mu M, respectively. Headed for excessive biological evaluation, the synthesized derivatives were tested over sixty diverse human cancer cell lines. Only compound 35 emerged as a potent cytotoxic agent against different panel of human cancer cell lines.

About 2,6-Difluorobenzoic acid, If you have any questions, you can contact Abdel-Maksoud, MS; Ali, EMH; Ammar, UM; Mersal, KI; Yoo, KH; Oh, CH or concate me.. Name: 2,6-Difluorobenzoic acid

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In 2020 EUR J MED CHEM published article about MULTIDRUG-RESISTANCE; P-GLYCOPROTEIN; CANCER; REVERSAL; MODULATORS; MECHANISMS; AGENTS; CELLS in [Wan, Qi; Guo, Yalan; Yu, Zhihui; Guo, Shiqi; Chen, Ying] Fudan Univ, Sch Pharm, Dept Med Chem, Shanghai, Peoples R China; [Jin, Xin; Liu, Hongrui] Fudan Univ, Sch Pharm, Dept Pharmacol & Biochem, Shanghai, Peoples R China; [Morris-Natschke, Susan; Lee, Kuo-Hsiung] Univ N Carolina, UNC Eshelman Sch Pharm, Nat Prod Res Labs, Chapel Hill, NC 27599 USA; [Lee, Kuo-Hsiung] China Med Univ & Hosp, Chinese Med Res & Dev Ctr, Taichung 40402, Taiwan in 2020, Cited 21. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2. Quality Control of 2,6-Difluorobenzoic acid

Thirty-four seco-3’R,4’R-disubstituted-2′,2′-dimethyldihydropyrano[2,3-f]chromone (seco-DSP) derivatives were designed, synthesized and evaluated for chemo-reversal activity when combined with paclitaxel or vincristine in P-gp overexpressing A2780/T and KB-VIN drug-resistant cancer cell lines. Most of the compounds displayed moderate to significant MDR reversal activities. Compound 7e showed the most potent chemo-sensitization activity with more than 1471 reversal ratio at a concentration of 10 mu M, which was higher than verapamil (VRP) (212-fold). Unexpectedly the newly synthesized compounds did not show chemosensitization activities in a non-P-gp overexpressing cisplatin resistant human ovarian cancer cell line (A2780/CDDP), implying that the MDR reversal effects might be associated with P-gp overexpression. Moreover, the compounds did not exhibit significant anti-proliferative activities against non-tumorigenic cell lines (HUVEC, HOSEC and T29) compared to VRP at the tested concentration and might be safer than VRP. In preliminary pharmacological mechanism studies, the compounds increased accumulation of DOX and promoted P-gp ATPase activity in A2780/T cell lines. Western blot analysis indicated they did not affect the expression level of P-gp in the tested MDR cell lines. Thus, further studies on these seco-DSP derivatives are merited with the goal of developing a desirable chemosensitizer drug candidate. (C) 2020 Elsevier Masson SAS. All rights reserved.

Quality Control of 2,6-Difluorobenzoic acid. About 2,6-Difluorobenzoic acid, If you have any questions, you can contact Wan, Q; Jin, X; Guo, YL; Yu, ZH; Guo, SQ; Morris-Natschke, S; Lee, KH; Liu, HR; Chen, Y or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Product Details of 385-00-2. Authors Wang, R; Liu, H; You, YY; Wang, XY; Lv, BB; Cao, LQ; Xue, JY; Xu, YG; Shi, L in PERGAMON-ELSEVIER SCIENCE LTD published article about in [Wang, Ru; Liu, Hu; You, Yuan-Yuan; Wang, Xin-Yu; Lv, Bing-Bing; Cao, Li-Qin; Xu, Yun-Gen; Shi, Lei] China Pharmaceut Univ, Dept Med Chem, Jiangsu Key Lab Drug Design & Optimizat, Nanjing 210009, Peoples R China; [Xue, Jia-Yu] Jiangsu Prov & Chinese Acad Sci, Inst Bot, Jiangsu Prov Key Lab Plant Ex Situ Conservat, Nanjing 210014, Peoples R China in 2021, Cited 29. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2

VEGF/VEGFR-2 signaling plays a critical part in tumor angiogenesis. Inhibition of this pathway has been considered as a promising approach for cancer treatment. In this work, a series of 6,7-dimethoxy-4-anilinoquinazoline derivatives bearing diarylamide moiety were designed, synthesized and evaluated as potent inhibitors of VEGFR-2 kinase. Their in vitro antiproliferation activities against two human cancer cell lines Hep-G2 and MCF-7 have also been determined. Among them, compound 14b exhibited the most potent inhibitory activity against VEGFR-2 with IC50 value of 0.016 +/- 0.002 mu M and it showed the most potent antiproliferative effect against Hep-G2 and MCF-7 with IC50 values at low-micromolar range. Molecular docking studies revealed that these compounds represented by the most potent compound 14b could bind well to the ATP-binding site of VEGFR-2, which suggested that compound 14b could be a potential anticancer agent targeting VEGFR-2.

About 2,6-Difluorobenzoic acid, If you have any questions, you can contact Wang, R; Liu, H; You, YY; Wang, XY; Lv, BB; Cao, LQ; Xue, JY; Xu, YG; Shi, L or concate me.. Product Details of 385-00-2

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Product Details of 385-00-2. In 2019 INORG CHEM published article about METAL-ORGANIC-FRAMEWORK; ENERGY MIGRATION; UIO-66; MODULATOR; DESIGN; AREAS in [Morris, Amanda J.] Virginia Tech, Dept Chem, Blacksburg, VA 24061 USA; Virginia Tech, Macromol Innovat Inst, Blacksburg, VA 24061 USA in 2019, Cited 44. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2.

The reaction of zirconium salts with meso-tetra(4-carboxyphenyl)porphyrin (TCPP) in the presence of different modulators results in the formation of a diverse set of metal-organic frameworks (MOFs), each displaying distinct crystalline topologies. However, the synthesis of phase-pure crystalline frameworks remains challenging due to the concurrent formation of different polymorphs. The acidity and concentration of the modulator greatly influence the outcome of the MOF synthesis. By systematically varying these two parameters, selective framework formation can be achieved. In the present study, we aimed to elucidate the effect of modulator on the synthesis of zirconium-based TCPP MOFs. With the help of powder X-ray diffraction and scanning electron microscopy, modulator candidates and the optimal synthetic conditions yielding phase-pure PCN-222, PCN-223, and MOF-525 were identified. H-1 nuclear magnetic resonance analysis, thermogravimetric analysis, and N-2 gas sorption measurements were performed on select MOFs to gain insight into the relationship between their defectivity and modulator properties.

Product Details of 385-00-2. About 2,6-Difluorobenzoic acid, If you have any questions, you can contact Shaikh, SM; Usov, PM; Zhu, J; Cai, M; Alatis, J; Morris, AJ or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

COA of Formula: C7H4F2O2. Recently I am researching about BENZOTRIAZOLE RING; FACILE SYNTHESIS; CLEAVAGE; BENZOTHIAZOLES; AMIDES; CONVERSION; PROTOCOL, Saw an article supported by the Science and Engineering Research Board (SERB), New Delhi [EMR/2016/001123]. Published in GEORG THIEME VERLAG KG in STUTTGART ,Authors: Singh, M; Singh, AS; Mishra, N; Agrahari, AK; Tiwari, VK. The CAS is 385-00-2. Through research, I have a further understanding and discovery of 2,6-Difluorobenzoic acid

N-Acylbenzotriazoles are achieved in good yields from the corresponding carboxylic acids by using only 0.35 equivalent of trichloroisocyanuric acid and 1.2 equivalents of PPh3. The salient features of the developed reaction path include an economic, facile, base-free, and equally useful method in milligram to gram scale.

COA of Formula: C7H4F2O2. About 2,6-Difluorobenzoic acid, If you have any questions, you can contact Singh, M; Singh, AS; Mishra, N; Agrahari, AK; Tiwari, VK or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Name: 2,6-Difluorobenzoic acid. Recently I am researching about AROMATIC AMIDES; CATALYZED ALKYLATION; BONDS; DERIVATIVES, Saw an article supported by the MEXTMinistry of Education, Culture, Sports, Science and Technology, Japan (MEXT) [17H06091]. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Das, A; Chatani, N. The CAS is 385-00-2. Through research, I have a further understanding and discovery of 2,6-Difluorobenzoic acid

The Rh-catalyzed C-H alkylation of benzylamine derivatives with unactivated 1-alkenes that proceeds via a picolinamide directing group is reported. The crucial role of an acid additive in this transformation is confirmed. Aromatic acids showed high linear selectivity, and aliphatic acids provided branched alkylation products as the major product. The reaction has a broad scope for benzylamines and alkenes. Deuterium labeling experiments suggest that a Rh-carbene intermediate is involved in the case of linear product formation. A different reaction pathway, however, appears to be involved in the case of branched alkylation products, and this pathway also appeared to be a minor pathway in linear-selective reactions.

About 2,6-Difluorobenzoic acid, If you have any questions, you can contact Das, A; Chatani, N or concate me.. Name: 2,6-Difluorobenzoic acid

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

An article Machine learning-based prediction of toxicity of organic compounds towards fathead minnow WOS:000574586100059 published article about QSAR MODEL; DESCRIPTORS; MOLECULES; CHEMICALS in [Chen, Xingmei; Dang, Limin; Yang, Hai; Huang, Xianwei; Yu, Xinliang] Hunan Inst Engn, Coll Mat & Chem Engn, Hunan Prov Key Lab Environm Catalysis & Waste Reg, Xiangtan 411104, Hunan, Peoples R China; [Yu, Xinliang] Donghu Rd 18, Xiangtan 411104, Hunan, Peoples R China in 2020, Cited 30. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2. Safety of 2,6-Difluorobenzoic acid

Predicting the acute toxicity of a large dataset of diverse chemicals against fathead minnows (Pimephales promelas) is challenging. In this paper, 963 organic compounds with acute toxicity towards fathead minnows were split into a training set (482 compounds) and a test set (481 compounds) with an approximate ratio of 1 : 1. Only six molecular descriptors were used to establish the quantitative structure-activity/toxicity relationship (QSAR/QSTR) model for 96 hourpLC(50)through a support vector machine (SVM) along with genetic algorithm. The optimal SVM model (R-2= 0.756) was verified using both internal (leave-one-out cross-validation) and external validations. The validation results (q(int)(2)= 0.699 andq(ext)(2)= 0.744) were satisfactory in predicting acute toxicity in fathead minnows compared with other models reported in the literature, although our SVM model has only six molecular descriptors and a large data set for the test set consisting of 481 compounds.

Safety of 2,6-Difluorobenzoic acid. About 2,6-Difluorobenzoic acid, If you have any questions, you can contact Chen, XM; Dang, LM; Yang, H; Huang, XW; Yu, XL or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Formula: C7H4F2O2. In 2019 EUR J MED CHEM published article about DRUG SYNTHESIS BIODS in [Hameed, Shehryar; Kanwal; Seraj, Faiza; Rafique, Rafaila; Khan, Khalid Mohammed] Univ Karachi, Int Ctr Chem & Biol Sci, HEJ Res Inst Chem, Karachi 75270, Pakistan; [Chigurupati, Sridevi] Qassim Univ, Coll Pharm, Dept Med Chem & Pharmacognosy, Buraydah 52571, Saudi Arabia; [Wadood, Abdul; Rehman, Ashfaq Ur] Abdul Wali Khan Univ, Dept Biochem, Computat Med Chem Lab, UCSS, Mardan, Pakistan; [Venugopal, Vijayan] AIMST Univ, Fac Pharm, Bedong 08100, Kedah, Malaysia; [Salar, Uzma] Univ Karachi, Int Ctr Chem & Biol Sci, Dr Panjwani Ctr Mol Med & Drug Res, Karachi 75270, Pakistan; [Taha, Muhammad; Khan, Khalid Mohammed] Imam Abdulrahman Bin Faisal Univ, IRMC, Dept Clin Pharm, POB 1982, Dammam 31441, Saudi Arabia in 2019, Cited 29. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2.

Benzotriazoles (4-6) were synthesized which were further reacted with different substituted benzoic acids and phenacyl bromides to synthesize benzotriazole derivatives (7-40). The synthetic compounds (7-40) were characterized via different spectroscopic techniques including EI-MS, HREI-MS, H-1-, and C-13 NMR. These molecules were examined for their anti-hyperglycemic potential hence were evaluated for alpha-glucosidase and alpha-amylase inhibitory activities. All benzotriazoles displayed moderate to good inhibitory activity in the range of IC50 values of 2.00-5.6 and 2.04-5.72 mu M against alpha-glucosidase and alpha-amylase enzymes, respectively. The synthetic compounds were divided into two categories A and B, in order to understand the structure-activity relationship. Compounds 25 (IC50 = 2.41 +/- 131 mu M), (IC50 = 2.5 +/- 1.21 mu M), 36 (IC50= 2.12 +/- 1.35 M), (IC50 = 2.21 +/- 1.08 mu M), and 37 (IC50 = 2.00 +/- 1.22 mu M), (IC50 = 2.04 +/- 1.4 mu M) with chloro substitution/s at aryl ring were found to be most active against alpha-glucosidase and alpha-amylase enzymes. Molecular docking studies on all compounds were performed which revealed that chloro substitutions are playing a pivotal role in the binding interactions. The enzyme inhibition mode was also studied and the kinetic studies revealed that the synthetic molecules have shown competitive mode of inhibition against alpha-amylase and non-competitive mode of inhibition against alpha-glucosidase enzyme. (C) 2019 Elsevier Masson SAS. All rights reserved.

Formula: C7H4F2O2. About 2,6-Difluorobenzoic acid, If you have any questions, you can contact Hameed, S; Kanwal; Seraj, F; Rafique, R; Chigurupati, S; Wadood, A; Rehman, AU; Venugopal, V; Salar, U; Taha, M; Khan, KM or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

An article Palladium-catalyzed salt-free double decarboxylative aryl allylation WOS:000458679200011 published article about CARBOXYLIC-ACIDS; PALLADATION; PERSPECTIVE; OLEFINATION; COMPLEXES in [Daley, Ryan A.; Topczewski, Joseph J.] Univ Minnesota, Dept Chem, Minneapolis, MN 44544 USA in 2019, Cited 26. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2. Application In Synthesis of 2,6-Difluorobenzoic acid

This report describes a palladium-catalyzed decarboxylative aryl allylation between unactivated benzoic acids and allylic carbonates. This transformation successfully couples a variety of carbonates and benzoic acids in good yield (up to 94%) using 1 mol% palladium. This salt free allyl-arylation proceeds without added base, copper, or silver. The only stoichiometric byproducts are carbon dioxide and tert-butanol.

Application In Synthesis of 2,6-Difluorobenzoic acid. About 2,6-Difluorobenzoic acid, If you have any questions, you can contact Daley, RA; Topczewski, JJ or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com