Day: January 18, 2022

An article Novel benzothiazole hybrids targeting EGFR: Design, synthesis, biological evaluation and molecular docking studies WOS:000664244600016 published article about THIOUREA DERIVATIVES BEARING; ANTITUMOR-ACTIVITY; INHIBITORY-ACTIVITY; CANCER; SENSITIVITY; MOIETY in [Abd El-Meguid, Eman A.] Natl Res Ctr, Pharmaceut & Drug Ind Res Div, Dept Chem Nat & Microbial Prod, Cairo 12622, Egypt; [Moustafa, Gaber O.] Natl Res Ctr, Chem Ind Res Div, Peptide Chem Dept, Cairo 12622, Egypt; [Awad, Hanem M.] Natl Res Ctr, Dept Tanning Mat & Leather Technol, Cairo 12622, Egypt; [Zaki, Eman R.] Natl Res Ctr, Dept Mol Biol, Cairo 12622, Egypt; [Nossier, Eman S.] Al Azhar Univ, Fac Pharm Girls, Dept Pharmaceut Med Chem, Cairo 11754, Egypt in 2021, Cited 47. The Name is Benzoic anhydride. Through research, I have a further understanding and discovery of 93-97-0. Category: isothiazole

Novel benzo[d] thiazole-based analogues were synthesized with the aim of screening their in vitro anticancer activity. All the new derivatives 4-21 were evaluated against human hepatocellular carcinoma (HepG-2) and breast cancer cells (MCF-7) using doxorubicin as a reference drug. All compounds exhibited excellent potency against MCF-7 (IC50 values ranging from 0.71 +/- 0.4 to 1.04 +/- 0.7 mu M) and variable promising potency against HepG-2 (IC50 ranged from 2.53 +/- 2.5 to 3.47 +/- 3.4 mu M) comparing with the standard (IC50 = 1.03 +/- 0.8 mu M and 2.85 +/- 1.9 mu M, respectively) in addition to their safety towards the normal cell line. Compounds 5, 6, 7, 13 and 16 having the highest cytotoxic activity, were further evaluated for their EGFR inhibitory activity using Erlotinib as a reference drug. Molecular docking studies were performed for the promising compounds 5, 6 and 7 to interpret their detected enzymatic activities based upon their binding interactions with the receptor. Moreover, cell cycle analysis and detection of apoptosis induction illustrated that compounds 5 and 6 exhibited a significant pre G(1) and G(2)/M cell cycle arrest, in comparison with the untreated MCF-7 cells. In addition, compounds 5 and 6 elevated the levels of the oncogenic parameters; Bax, p53 and caspase-3 with decreased level of Bcl-2. These previous encouraging results of biological evaluation of the newly synthesized benzothiazoles could recommend an excellent framework toward the detection of new potent antitumor leads. (C) 2021 Elsevier B.V. All rights reserved.

Category: isothiazole. Bye, fridends, I hope you can learn more about C14H10O3, If you have any questions, you can browse other blog as well. See you lster.

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

Formula: C7H4F2O2. Authors 20220118 in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER published article about in [Lin, Tingting; Jiang, Hualiang; Chen, Kaixian; Luo, Cheng] ShanghaiTech Univ, Shanghai Inst Adv Immunochem Studies, Shanghai 200031, Peoples R China; [Lin, Tingting; Jiang, Hualiang; Chen, Kaixian; Luo, Cheng] ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai 200031, Peoples R China; [Lin, Tingting; Li, Jiacheng; Liu, Liping; Li, Yuanqing; Jiang, Hualiang; Chen, Kaixian; Xu, Pan; Luo, Cheng] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Ctr Chem Biol,Drug Discovery & Design Ctr, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; [Lin, Tingting; Zhou, Bing] Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; [Lin, Tingting; Li, Jiacheng; Liu, Liping; Li, Yuanqing; Jiang, Hualiang; Chen, Kaixian; Luo, Cheng; Zhou, Bing] Univ Chinese Acad Sci, 19 Yuquan Rd, Beijing 100049, Peoples R China in 2021, Cited 39. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2

Cyclin-dependent kinases play significant roles in cell cycle progression and are promising targets for cancer therapy. However, most potent CDK inhibitors lack the balance between efficacy and safety because of poor selectivity. Given the roles of CDK2 in tumorigenesis, selective CDK2 inhibition may provide therapeutic benefits against certain cancer. In this study, a series of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives were designed, synthesized, and evaluated. The most selective compound DC-K2in212 in this series exhibited high potency towards CDK2 and had effective anti-proliferative activity against A2058 melanoma cell line and MV4-11 leukemia cell line while exhibiting low toxic effect on human normal cell lines MRC5 and LX2. The molecular modeling illustrated that compound DC-K2in212 had the similar binding mode with CDK2 as C-73, the most selective CDK2 inhibitor reported so far, which might account for selectivity against CDK2 over CDK1. Further biological studies revealed that compound DC-K2in212 suppressed CDK2-associated downstream signaling pathway, blocked cell cycle progression, and induced cellular apoptosis. Therefore, compound DC-K2in212 could serve as a potential CDK2 inhibitor for further development. (c) 2021 Elsevier Masson SAS. All rights reserved.

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

Safety of 3-Methylbenzoic acid. Authors 20220118 in ROYAL SOC CHEMISTRY published article about in [Yuan, Tao; Zheng, Meifang; Wang, Xinchen] Fuzhou Univ, Coll Chem, State Key Lab Photocatalysis Energy & Environm, Fuzhou 350116, Peoples R China; [Antonietti, Markus] Max Planck Inst Colloids & Interfaces, Dept Colloid Chem, Res Campus Golm, D-14424 Potsdam, Germany in 2021, Cited 61. The Name is 3-Methylbenzoic acid. Through research, I have a further understanding and discovery of 99-04-7

Photochemistry provides a sustainable pathway for organic transformations by inducing radical intermediates from substrates through electron transfer process. However, progress is limited by heterogeneous photocatalysts that are required to be efficient, stable, and inexpensive for long-term operation with easy recyclability and product separation. Here, we report that boron carbonitride (BCN) ceramics are such a system and can reduce organic halides, including (het)aryl and alkyl halides, with visible light irradiation. Cross-coupling of halides to afford new C-H, C-C, and C-S bonds can proceed at ambient reaction conditions. Hydrogen, (het)aryl, and sulfonyl groups were introduced into the arenes and heteroarenes at the designed positions by means of mesolytic C-X (carbon-halogen) bond cleavage in the absence of any metal-based catalysts or ligands. BCN can be used not only for half reactions, like reduction reactions with a sacrificial agent, but also redox reactions through oxidative and reductive interfacial electron transfer. The BCN photocatalyst shows tolerance to different substituents and conserved activity after five recycles. The apparent metal-free system opens new opportunities for a wide range of organic catalysts using light energy and sustainable materials, which are metal-free, inexpensive and stable.

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

In 2021 SYNTHESIS-STUTTGART published article about C-H BOND; ANTRODIA-CAMPHORATA; SELECTIVE SYNTHESIS; MICHAEL ADDITION; CYCLIC IMIDES; DERIVATIVES; INDOLES; 1,4-ADDITION; CONSTRUCTION; ALKYLATION in [Gairola, Deepti; Peddinti, Rama Krishna] Indian Inst Technol Roorkee, Dept Chem, Roorkee 247667, Uttarakhand, India in 2021, Cited 49. The Name is 1,3-Dimethoxybenzene. Through research, I have a further understanding and discovery of 151-10-0. Name: 1,3-Dimethoxybenzene

Friedel-Crafts reaction is widely used for the C-C bond forming reaction to enable the direct connection of electron-rich arenes to electron-deficient olefins with high regioselectivity. Herein, a highly efficient, metal-free, and environmentally benign F-C strategy of electron-rich arenes with N-arylmaleimides has been developed for the construction of 3-arylsuccinimides in the presence of a green reagent methanesulfonic acid under mild reaction conditions. This highly facile and high-yielding protocol has compatibility with different electron-rich arenes.

Welcome to talk about 151-10-0, If you have any questions, you can contact 20220118 or send Email.. Name: 1,3-Dimethoxybenzene

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

Application In Synthesis of Benzoic anhydride. Recently I am researching about SUPPORTED IRON CATALYST; BORON-NITRIDE; FACILE FABRICATION; MANGANESE; PHASE; MOSSBAUER; OLEFINS; HYDROGENATION; NANOPARTICLES; OXIDES, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [21673273, 91545109]; Synfuels China Technology Co., Ltd.. Published in ELSEVIER in AMSTERDAM ,Authors: 20220118. The CAS is 93-97-0. Through research, I have a further understanding and discovery of Benzoic anhydride

A series of Fe/h-BN catalysts promoted with Cu or Mn were prepared for Fischer-Tropsch synthesis (FTS). The physicochemical properties, crystal structures and morphologies of the catalysts were characterized by N-2 physisorption, FT-IR, TPR, XPS, XRD, MES and TEM. It is found that iron oxide nanoparticles are highly dispersed on h-BN matrix due to the anchoring effect of surface defects and the accommodation of porous structures of h-BN. The characterization results indicate that strong interaction between iron oxide and h-BN is present on un-promoted catalyst, which endows the h-BN supported iron catalyst with stable properties under FTS conditions but severely retards reduction of the catalyst. The addition of Cu to Fe/h-BN can to some extent overcome the strong interaction by introducing more sites for dissociating H-2. It is observed that Cu promoter can increase the reduction or carburization degree and thus enhance the FTS activity. The addition of Mn to Fe/h-BN can weaken the strong interaction by altering the electron structure of iron species. And the electron-rich Fe species are responsible for easy reduction and the enhanced FTS performance. Besides, a higher activity can be realized by co-adding Cu and Mn to the Fe/h-BN catalyst. These results suggest that the synergistic effect of Mn and Cu can largely improve the performance of Fe/h-BN catalyst without impairing the stability of the catalyst. The present study paves a way to tailor the performances of FTS catalysts with h-BN as support.

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

In 2019.0 ORG LETT published article about SOLUTION-PHASE PREPARATION; PICTET-SPENGLER REACTION; ASYMMETRIC-SYNTHESIS; BOBBITT SYNTHESIS; UGI; ALKALOIDS; EFFICIENT; MCR; FUNCTIONALIZATION; QUINOLINES in [Wang, Yuanze; Patil, Pravin; Domling, Alexander] Univ Groningen, Drug Design, Deusinglaan 1, NL-7313 AV Groningen, Netherlands; [Kurpiewska, Katarzyna; Kalinowska-Tluscik, Justyna] Jagiellonian Univ, Fac Chem, 3 Ingardena St, PL-30060 Krakow, Poland in 2019.0, Cited 74.0. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7. Recommanded Product: 93-02-7

The Pomeranz-Fritsch reaction and its Schlittler-Muller modification were successfully applied in the Ugi postcyclization strategy by using orthogonally protected aminoacetaldehyde diethyl acetal and complementary electron rich building blocks. Several scaffolds, including isoquinolines, carboline, alkaloid-like tetrazole-fused tetracyclic compounds, and benzo[d]azepinone scaffolds, were synthesized in generally moderate to good yield. All our syntheses provide a short MCR-based sequence to novel or otherwise difficult to access scaffolds. Hence, we foresee multiple applications of these synthesis technologies.

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

Name: 1,3-Dimethoxybenzene. Recently I am researching about LEWIS-BASE CATALYSIS; SELECTIVE HALOGENATION; AROMATIC-COMPOUNDS; EFFICIENT; FUNCTIONALIZATION; BIOSYNTHESIS; BROMINATION; ACTIVATION; TRYPTOPHAN; EVOLUTION, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [21602005, 21632001, 81821004]; National Basic Research Program of China (973 Program)National Basic Research Program of China [2015CB856600]; Drug Innovation Major Project [2018ZX09711-001]; Open Fund of State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, China [KF-GN-201906]. Published in NATURE RESEARCH in BERLIN ,Authors: 20220118. The CAS is 151-10-0. Through research, I have a further understanding and discovery of 1,3-Dimethoxybenzene

The chlorination of a bioactive compound can change its physiological properties and improve its pharmacokinetic and pharmacological profiles. It therefore has been an important strategy for drug discovery and development. However, the direct aromatic chlorination of complex bioactive molecules is too difficult to be practical. In fact, many functional groups such as hydroxyls, amines, amides or carboxylic acids may strongly restrain the reactivity of Cl+ by forming a halogen bond. Here we report a highly efficient aromatic chlorination of arenes that is catalysed by dimethyl sulfoxide with N-chlorosuccinimide as the chloro source. The mild conditions, easy-availability and stability of the catalyst and reagents, as well as good functional-group tolerance, showed the approach to be a versatile protocol for the late-stage aromatic chlorination of complex natural products, drugs and peptides. The multi-gram experiment and low-cost of N-chlorosuccinimide and dimethyl sulfoxide shows great potential for drug discovery and development in industrial applications. Late-stage aromatic chlorination of active pharmaceutical ingredients has enormous potential in drug discovery yet still features limited applicability due to issues of functional-group tolerance. Now, dimethyl sulfoxide is reported as catalyst for the chlorination of a diverse family of bioactive molecules in combination with N-chlorosuccinimide.

Name: 1,3-Dimethoxybenzene. Bye, fridends, I hope you can learn more about C8H10O2, If you have any questions, you can browse other blog as well. See you lster.

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

Safety of Benzoic anhydride. Authors 20220118 in NATURE RESEARCH published article about in [Sakai, Takayuki; Tsuji, Mieko; Hirayama, Tasuku; Nagasawa, Hideko] Gifu Pharmaceut Univ, Lab Pharmaceut & Med Chem, Gifu, Gifu 5011196, Japan; [Matsuo, Yoshiyuki; Hirota, Kiichi] Kansai Med Univ, Inst Biomed Sci, Dept Human Stress Response Sci, 2-5-1 Shin Machi, Hirakata, Osaka 5731010, Japan; [Okuda, Kensuke] Kobe Pharmaceut Univ, Lab Bioorgan & Nat Prod Chem, 4-19-1 Motoyama Kita, Kobe, Hyogo 6588558, Japan in 2021, Cited 52. The Name is Benzoic anhydride. Through research, I have a further understanding and discovery of 93-97-0

To develop antitumor drugs capable of targeting energy metabolism in the tumor microenvironment, we produced a series of potent new biguanide derivatives via structural modification of the arylbiguanide scaffold. We then conducted biological screening using hypoxia inducible factor (HIF)-1- and unfolded protein response (UPR)-dependent reporter assays and selective cytotoxicity assay under low glucose conditions. Homologation studies of aryl-(CH2)(n)-biguanides (n=0-6) yielded highly potent derivatives with an appropriate alkylene linker length (n=5, 6). The o-chlorophenyl derivative 7l (n=5) indicated the most potent inhibitory effects on HIF-1- and UPR-mediated transcriptional activation (IC50; 1.0 +/- 0.1 mu M, 7.5 +/- 0.1 mu M, respectively) and exhibited selective cytotoxicity toward HT29 cells under low glucose condition (IC50; 1.9 +/- 0.1 mu M). Additionally, the protein expression of HIF-1 alpha induced by hypoxia and of GRP78 and GRP94 induced by glucose starvation was markedly suppressed by the biguanides, thereby inhibiting angiogenesis. Metabolic flux and fluorescence-activated cell sorting analyses of tumor cells revealed that the biguanides strongly inhibited oxidative phosphorylation and activated compensative glycolysis in the presence of glucose, whereas both were strongly suppressed in the absence of glucose, resulting in cellular energy depletion and apoptosis. These findings suggest that the pleiotropic effects of these biguanides may contribute to more selective and effective killing of cancer cells due to the suppression of various stress adaptation systems in the tumor microenvironment.

Welcome to talk about 93-97-0, If you have any questions, you can contact 20220118 or send Email.. Safety of Benzoic anhydride

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

Recommanded Product: 1,3-Dimethoxybenzene. In 2019 ORG LETT published article about C-H; STEREOSPECIFIC SYNTHESIS; ELECTROPHILIC AMINATION; CATALYZED AMINATION; BONDS in [Munnuri, Sailu; Anugu, Raghunath Reddy; Falck, John R.] Univ Texas Southwestern Med Ctr Dallas, Dept Biochem, Div Chem, Dallas, TX 75390 USA in 2019, Cited 32. The Name is 1,3-Dimethoxybenzene. Through research, I have a further understanding and discovery of 151-10-0.

Cu(II)-mediated direct NH2 and NH alkyl aryl aminations and olefin aziridinations are described. These room temperature, one-pot, environmentally friendly procedures replace costly Rh-2 catalysts and, in some instances, display important differences with comparable Rh-2- and Fe-supported reactions.

Welcome to talk about 151-10-0, If you have any questions, you can contact 20220118 or send Email.. Recommanded Product: 1,3-Dimethoxybenzene

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

I found the field of Biochemistry & Molecular Biology; Chemistry very interesting. Saw the article Synthesis and application of a F-19-labeled fluorescent nucleoside as a dual-mode probe for i-motif DNAs published in 2021. Product Details of 93-97-0, Reprint Addresses Sugiyama, H; Park, S (corresponding author), Kyoto Univ, Grad Sch Sci, Dept Chem, Sakyo Ku, Kitashirakawa Oiwakecho, Kyoto 6068502, Japan.; Sugiyama, H (corresponding author), Kyoto Univ, Inst Integrated Cell Mat Sci iCeMS, Sakyo Ku, Yoshida Ushinomiyacho, Kyoto 6068501, Japan.. The CAS is 93-97-0. Through research, I have a further understanding and discovery of Benzoic anhydride

Because of their stable orientations and their minimal interference with native DNA interactions and folding, emissive isomorphic nucleoside analogues are versatile tools for the accurate analysis of DNA structural heterogeneity. Here, we report on a bifunctional trifluoromethylphenylpyrrolocytidine derivative ((FP)dC) that displays an unprecedented quantum yield and highly sensitive F-19 NMR signal. This is the first report of a cytosine-based dual-purpose probe for both fluorescence and F-19 NMR spectroscopic DNA analysis. (FP)dC and (FP)dC-containing DNA were synthesized and characterized; our robust dual probe was successfully used to investigate the noncanonical DNA structure, i-motifs, through changes in fluorescence intensity and F-19 chemical shift in response to i-motif formation. The utility of (FP)dC was exemplified through reversible fluorescence switching of an (FP)dC-containing i-motif oligonucleotide in the presence of Ag(i) and cysteine.

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