Tag: M.W=150-200

Listro, R; Stotani, S; Rossino, G; Rui, M; Malacrida, A; Cavaletti, G; Cortesi, M; Arienti, C; Tesei, A; Rossi, D; Di Giacomo, M; Miloso, M; Collina, S in [Listro, Roberta; Stotani, Silvia; Rossino, Giacomo; Rui, Marta; Rossi, Daniela; Di Giacomo, Marcello; Collina, Simona] Univ Pavia, Dept Drug Sci, Med Chem & Pharmaceut Technol Sect, Pavia, Italy; [Stotani, Silvia] Taros Chem GmbH & Co KG, Med Chem, Dortmund, Germany; [Malacrida, Alessio; Cavaletti, Guido; Miloso, Mariarosaria] Univ Milano Bicocca, Expt Neurol Unit, Sch Med & Surg, Monza, Italy; [Malacrida, Alessio; Cavaletti, Guido; Miloso, Mariarosaria] Univ Milano Bicocca, Milan Ctr Neurosci, Monza, Italy; [Cortesi, Michela; Arienti, Chiara; Tesei, Anna] Ist Sci Romagnolo Studio & Cura Tumori IRCCS, Biosci Lab, Meldola, Italy published Exploring the RC-106 Chemical Space: Design and Synthesis of Novel (E)-1-(3-Arylbut-2-en-1-yl)-4-(Substituted) Piperazine Derivatives as Potential Anticancer Agents in 2020, Cited 65. SDS of cas: 385-00-2. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2.

Despite the fact that significant advances in treatment of common cancers have been achieved over the years, orphan tumors still represent an important unmet medical need. Due to their complex multifactorial origin and limited number of cases, such pathologies often have very limited treatment options and poor prognosis. In the search for new anticancer agents, our group recently identifiedRC-106, a Sigma receptor modulator endowed with proteasome inhibition activity. This compound showed antiproliferative activity toward different cancer cell lines, among them glioblastoma (GB) and multiple myeloma (MM), two currently unmet medical conditions. In this work, we directed our efforts toward the exploration of chemical space aroundRC-106to identify new active compounds potentially useful in cancer treatment. Thanks to a combinatorial approach, we prepared 41 derivatives of the compound and evaluated their cytotoxic potential against MM and GB. Three novel potential anticancer agents have been identified.

Welcome to talk about 385-00-2, If you have any questions, you can contact Listro, R; Stotani, S; Rossino, G; Rui, M; Malacrida, A; Cavaletti, G; Cortesi, M; Arienti, C; Tesei, A; Rossi, D; Di Giacomo, M; Miloso, M; Collina, S or send Email.. SDS of cas: 385-00-2

Reference:
Isothiazole – Wikipedia,
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Saglik, BN; Osmaniye, D; Levent, S; Cevik, UA; Cavusoglu, BK; Ozkay, Y; Kaplancikli, ZA in [Saglik, Begum Nurpelin; Osmaniye, Derya; Levent, Serkan; Cevik, Ulviye Acar; Ozkay, Yusuf; Kaplancikli, Zafer Asim] Anadolu Univ, Fac Pharm, Dept Pharmaceut Chem, TR-26470 Eskisehir, Turkey; [Saglik, Begum Nurpelin; Osmaniye, Derya; Levent, Serkan; Cevik, Ulviye Acar; Ozkay, Yusuf] Anadolu Univ, Fac Pharm, Doping & Narcot Cpds Anal Lab, TR-26470 Eskisehir, Turkey; [Cavusoglu, Betul Kaya] Zonguldak Bulent Ecevit Univ, Fac Pharm, Dept Pharmaceut Chem, TR-67600 Zonguldak, Turkey published Design, synthesis and biological assessment of new selective COX-2 inhibitors including methyl sulfonyl moiety in 2021, Cited 44. Quality Control of 2,5-Dimethoxybenzaldehyde. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7.

Nonsteroidal anti-inflammatory drugs (NSAIDs) cause peptic lesions in the gastrointestinal mucosa by inhibiting the cyclooxygenase-1 (COX-1) enzyme. Selective COX-2 inhibition causes decreased side effects over current NSAIDs. Therefore, the studies about selective inhibition of COX-2 enzyme are very important for new drug development. The design, synthesis and biological activity evaluation of novel derivatives bearing thiazolylhydrazine-methyl sulfonyl moiety as selective COX-2 inhibitors were aimed in this paper. The structures of synthesized compounds were assigned using different spectroscopic techniques such as H-1 NMR, C-13 NMR and HRMS. In addition, the estimation of ADME parameters for all compounds was carried out using in silico process. The evaluation of in vitro COX-1/COX-2 enzyme inhibition was applied according to the fluorometric method. According to the enzyme inhibition results, synthesized compounds showed the selectivity against COX-2 enzyme inhibition as expected. Compounds 3a, 3e, 3f, 3g, 3i and 3j demonstrated significant COX-2 inhibition potencies. Among them, compound 3a was found to be the most effective derivative with an IC50 value of 0.140 +/- 0.006 mM. Moreover, it was seen that compound 3a displayed a more potent inhibition profile at least 12-fold than nimesulide (IC50 = 1.684 +/- 0.079 mu M), while it showed inhibitory activity at a similar rate of celecoxib (IC50 = 0.132 +/- 0.005 mu M). Molecular modelling studies aided in the understanding of the interaction modes between this compound and COX-2 enzyme. It was found that compound 3a had a significant binding property. In addition, the selectivity of obtained derivatives on COX-2 enzyme could be explained and discussed by molecular docking studies. (C) 2020 Elsevier Masson SAS. All rights reserved.

Welcome to talk about 93-02-7, If you have any questions, you can contact Saglik, BN; Osmaniye, D; Levent, S; Cevik, UA; Cavusoglu, BK; Ozkay, Y; Kaplancikli, ZA or send Email.. Quality Control of 2,5-Dimethoxybenzaldehyde

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Quality Control of 2,5-Dimethoxybenzaldehyde. Authors de Barros, WA; Queiroz, MP; Neto, LD; Borges, GM; Martins, FT; de Fatima, A in PERGAMON-ELSEVIER SCIENCE LTD published article about in [de Barros, Wellington Alves; Queiroz, Marcelo Pereira; Neto, Leonardo da Silva; Borges, Graziele Martins; de Fatima, Angelo] Univ Fed Minas Gerais, Inst Ciencias Exatas, Dept Quim, BR-31270901 Belo Horizonte, MG, Brazil; [Martins, Felipe Terra] Univ Fed Goias, Inst Quim, CP 131, BR-74001970 Goiania, Go, Brazil in 2021.0, Cited 31.0. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7

An expeditious method is reported for the synthesis of three NBOHs (25H-, 25I- and 25B-NBOH; 9-38% overall yield) and three NBOMes (25H-, 25I- and 25B-NBOMe; 7-33% overall yield) from salicylaldehyde and 2-methoxyaldehyde, respectively. The X-ray structures of 25H-, 25I- and 25B-NBOH center dot HCl were also determined. Our approach should provide a general entry for preparing such a class of substances for pharmacological and forensic purposes. (C) 2021 Elsevier Ltd. All rights reserved.

Quality Control of 2,5-Dimethoxybenzaldehyde. Welcome to talk about 93-02-7, If you have any questions, you can contact de Barros, WA; Queiroz, MP; Neto, LD; Borges, GM; Martins, FT; de Fatima, A or send Email.

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I found the field of Crystallography very interesting. Saw the article Three closely related 1-[(1,3-benzodioxol-5-yl)-methyl]-4-(halobenzoyl)pinerazines: similar molecular structures but different intermolecular interactions published in 2019. Category: isothiazole, Reprint Addresses Yathirajan, HS (corresponding author), Univ Mysore, Dept Studies Chem, Mysuru 570006, India.. The CAS is 385-00-2. Through research, I have a further understanding and discovery of 2,6-Difluorobenzoic acid

In each of the compounds 1-[(1,3-benzodioxol-5-yl)methyl]-4-(3-fluorobenzoyl)piperazine, C19H19 FN2O3 (I), 1-[(1,3-benzodioxol-5-yl)methyl]-4-(2,6-difluorobenzoyl)piperazine, C19H18F2N2O3 (II), and 1-[(1,3-benzodioxol-5-yl)methyl]-4-(2,4-dichlorobenzoyl)piperazine, C19H19Cl2N2O3 (III), the piperazine rings adopt a chair conformation with the (1,3-benzodioxol-5-yl)methyl substituent occupying an equatorial site: the five-membered rings are all slightly folded across the O center dot center dot center dot O line leading to envelope conformations. The dihedral angle between the planar amidic fragment and the haloaryl ring is 62.97 (5)degrees in (I) but 77.72 (12)degrees and 75.50 (5)degrees in (II) and (III), respectively. Despite their similarity in constitution and conformation, the supramolecular interactions in (I)-(III) differ: in (I), a combination of C-H center dot center dot center dot O and C-H center dot center dot center dot pi(arene) hydrogen bonds links the molecules into a three-dimensional framework structure, but there are no hydrogen bonds of any sort in either (II) or (III), although the structure of (III) contains a short Cl center dot center dot center dot Cl contact between inversion-related pairs of molecules.

Welcome to talk about 385-00-2, If you have any questions, you can contact Mahesha, N; Sagar, BK; Yathirajan, HS; Furuya, T; Haraguchi, T; Akitsu, T; Glidewell, C or send Email.. Category: isothiazole

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Authors Hoffman, RL; Kania, RS; Brothers, MA; Davies, JF; Ferre, RA; Gajiwala, KS; He, MY; Hogan, RJ; Kozminski, K; Li, LLY; Lockner, JW; Lou, JH; Marra, MT; Mitchell, LJ; Murray, BW; Nieman, JA; Noell, S; Planken, SP; Rowe, T; Ryan, K; Smith, GJ; Solowiej, JE; Steppan, CM; Taggart, B in AMER CHEMICAL SOC published article about CYSTEINE PROTEASE; ALDEHYDE INHIBITORS; IN-VITRO; BIOLOGICAL EVALUATION; ANTIVIRAL ACTIVITY; SARS-CORONAVIRUS; FORMAZAN ASSAY; DESIGN; AG7088; PAPAIN in [Hoffman, Robert L.; Kania, Robert S.; Brothers, Mary A.; Davies, Jay F.; Ferre, Rose A.; Gajiwala, Ketan S.; He, Mingying; Kozminski, Kirk; Li, Lilian Y.; Lockner, Jonathan W.; Lou, Jihong; Marra, Michelle T.; Mitchell, Lennert J., Jr.; Murray, Brion W.; Nieman, James A.; Noell, Stephen; Planken, Simon P.; Ryan, Kevin; Smith, George J., III; Solowiej, James E.; Steppan, Claire M.] Pfizer Worldwide Res & Dev, San Diego, CA 92121 USA; [Hogan, Robert J.; Rowe, Thomas; Taggart, Barbara] Southern Res Inst, Birmingham, AL 35205 USA in 2020, Cited 45. COA of Formula: C7H4F2O2. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2

The novel coronavirus disease COVID-19 that emerged in 2019 is caused by the virus SARS CoV-2 and named for its close genetic similarity to SARS CoV-1 that caused severe acute respiratory syndrome (SARS) in 2002. Both SARS coronavirus genomes encode two overlapping large polyproteins, which are cleaved at specific sites by a 3C-like cysteine protease (3CL(pro)) in a post-translational processing step that is critical for coronavirus replication. The 3CL(pro) sequences for CoV-1 and CoV-2 viruses are 100% identical in the catalytic domain that carries out protein cleavage. A research effort that focused on the discovery of reversible and irreversible ketone-based inhibitors of SARS CoV-1 3CL(pro) employing ligand-protease structures solved by X-ray crystallography led to the identification of 3 and 4. Preclinical experiments reveal 4 (PF-00835231) as a potent inhibitor of CoV-2 3CL(pro) with suitable pharmaceutical properties to warrant further development as an intravenous treatment for COVID-19.

COA of Formula: C7H4F2O2. About 2,6-Difluorobenzoic acid, If you have any questions, you can contact Hoffman, RL; Kania, RS; Brothers, MA; Davies, JF; Ferre, RA; Gajiwala, KS; He, MY; Hogan, RJ; Kozminski, K; Li, LLY; Lockner, JW; Lou, JH; Marra, MT; Mitchell, LJ; Murray, BW; Nieman, JA; Noell, S; Planken, SP; Rowe, T; Ryan, K; Smith, GJ; Solowiej, JE; Steppan, CM; Taggart, B or concate me.

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

Authors Sharma, MG; Vala, RM; Patel, HM in ROYAL SOC CHEMISTRY published article about ONE-POT; REGIOSELECTIVE SYNTHESIS; MANNICH PRODUCTS; FACILE SYNTHESIS; DERIVATIVES; EFFICIENT; GREEN; WATER in [Sharma, Mayank G.; Vala, Ruturajsinh M.; Patel, Hitendra M.] Sardar Patel Univ, Dept Chem, Univ Campus, Vallabh Vidyanagar 388120, Gujarat, India in 2020.0, Cited 38.0. Name: 2,5-Dimethoxybenzaldehyde. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7

Green synthesis of pyrazolo[3,4-b]quinolinones was designed using bioproduct pyridine-2-carboxylic acid (P2CA) as a green and efficient catalyst. The multi-component reaction of aldehydes, 1,3-cyclodiones and 5-amino-1-phenyl-pyrazoles regioselectively produced pyrazolo[3,4-b]quinolinones in excellent yield (84-98%). Recyclization of the catalyst was also investigated. The electronic effect of the various substituents in aromatic rings indicated that the reaction proceeded through the carbocation intermediate. This newly designed protocol very quickly constructed products conventionally under milder conditions.

Name: 2,5-Dimethoxybenzaldehyde. Welcome to talk about 93-02-7, If you have any questions, you can contact Sharma, MG; Vala, RM; Patel, HM or send Email.

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Isothiazole – Wikipedia,
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Recently I am researching about CARBON-HETEROATOM BONDS; GRIGNARD-REAGENTS; AROMATIC KETONES; ARYL HALIDES; NI; ETHERS; ACTIVATION; CLEAVAGE; EXPLORATION; ANISOLES, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [21572175, 21702028, 21871186, 21971168]; Department of Science and Technology of Jilin Province [20180520206JH]. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Tang, JH; Liu, LL; Yang, SR; Cong, XF; Luo, MM; Zeng, XM. The CAS is 93-02-7. Through research, I have a further understanding and discovery of 2,5-Dimethoxybenzaldehyde. Recommanded Product: 2,5-Dimethoxybenzaldehyde

We report here the first example of cross-coupling between two different and unactivated C(aryl)-O bonds with chromium catalysis. The combination of a low-cost Cr(II) salt, 4,4′-di-tart-butyl-2,2′-dipyridyl (dtbpy) as the ligand, and magnesium as the reductant shows high reactivity in promoting the reductive cross-coupling of aryl methyl ether derivatives with aryl esters by cleavage and coupling of two different C(aryl)-O bonds under mild conditions. The formation of active low-valent Cr species by reduction of CrCl2 with Mg can be considered, which prefers to initially activate the C(aryl)-O bond of phenyl methyl ether with the chelation help of dtbpy and an o-imine auxiliary. The subsequent consecutive reduction, second C(aryl)-O activation, and reductive elimination allow for the achievement of selective cross-coupling of C(aryl)-O/C(aryl)-O bonds.

Recommanded Product: 2,5-Dimethoxybenzaldehyde. Bye, fridends, I hope you can learn more about C9H10O3, If you have any questions, you can browse other blog as well. See you lster.

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

An article Synthetic Approach to the ABCD Ring System of Anticancer Agent Fredericamycin A via Claisen Rearrangement and Ring-Closing Metathesis as Key Steps WOS:000492429100004 published article about DIELS-ALDER REACTION; STRATEGY; MODEL; BIOSYNTHESIS; POLYCYCLICS; DERIVATIVES; PROTOCOL; DESIGN in [Kotha, Sambasivarao; Cheekatla, Subba Rao; Fatma, Ambareen] Indian Inst Technol, Dept Chem, Mumbai 400076, Maharashtra, India in 2019.0, Cited 68.0. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7. Application In Synthesis of 2,5-Dimethoxybenzaldehyde

A new synthetic strategy to the ABCD ring system of the anticancer agent fredericamycin A (NSC-305263) was realized by the Diels-Alder reaction and olefin metathesis as key steps. The tactics developed here for the construction of the ABCD ring system also involve double Claisen rearrangement followed by a retro-Diels-Alder reaction and ring-closing metathesis. The metathesis approach performs a key role in the construction of A and D rings of the ABCD core unit. More importantly, ABCD fragment synthesis was accomplished without the involvement of protecting groups.

Welcome to talk about 93-02-7, If you have any questions, you can contact Kotha, S; Cheekatla, SR; Fatma, A or send Email.. Application In Synthesis of 2,5-Dimethoxybenzaldehyde

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,Isothiazole – ScienceDirect.com

Category: isothiazole. Chen, XM; Dang, LM; Yang, H; Huang, XW; Yu, XL 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 published Machine learning-based prediction of toxicity of organic compounds towards fathead minnow in 2020, Cited 30. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2.

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.

Welcome to talk about 385-00-2, If you have any questions, you can contact Chen, XM; Dang, LM; Yang, H; Huang, XW; Yu, XL or send Email.. Category: isothiazole

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COA of Formula: C7H4F2O2. 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.

COA of Formula: C7H4F2O2. Bye, fridends, I hope you can learn more about C7H4F2O2, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Isothiazole – Wikipedia,
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