Tag: M.W=150-200

Chen, L; Lin, ZY; Zhang, XF; Tan, LS; Zhang, M; Li, YB in [Chen, Lu; Lin, Zhenyuan; Zhang, Xuefang; Tan, Leshi; Zhang, Min; Li, Yibiao] Wuyi Univ, Sch Biotechnol & Hlth Sci, Jiangmen, Peoples R China published Catalyst-free visible-light induced synthesis of nitrogen- and oxygen-containing heterocycles from 1,3-diketones in 2021.0, Cited 40.0. COA of Formula: C9H10O3. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9.

The synthesis of nitrogen- and oxygen-containing heterocycles has found many applications in the preparation of biomedical intermediates, yet actual synthetic procedures display limitations such as high-loading catalysts, harsh reaction conditions and tedious preparation of heterogeneous catalysts. Alternatively, photocatalysis allows to access functional products with minimum synthetic procedures and waste generation. Here, we present an efficient, simple, green protocol for the synthesis of N- and O-containing six-membered-ring compounds under mild conditions under visible blue light. Various aldehydes and 1,3-diketones can be reacted to afford eight series of corresponding 1,4-dihydropyridines and 4H-benzo[b]pyrans. This protocol has some merits such as the use of abundant and sustainable aqueous ethanol as solvent, short reaction time (within 60 min), no need of catalyst and broad functional group tolerance to afford 81 different series of target molecules in 75-96% yield under mild conditions.

COA of Formula: C9H10O3. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Chen, L; Lin, ZY; Zhang, XF; Tan, LS; Zhang, M; Li, YB or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

An article Design and synthesis of quinoline-pyrimidine inspired hybrids as potential plasmodial inhibitors WOS:000643683200007 published article about MOLECULAR-DYNAMICS; ASSAY in [Kayamba, Francis; Kushwaha, Narva Deshwar; Mahlalela, Mavela; Karpoormath, Rajshekhar] Univ KwaZulu Natal, Coll Hlth Sci, Dept Pharmaceut Chem, ZA-4000 Durban, South Africa; [Malimabe, Teboho; van Zyl, Robyn L.] Univ Witwatersrand, Fac Hlth Sci, Dept Pharm & Pharmacol, Pharmacol Div, ZA-2193 Johannesburg, South Africa; [Malimabe, Teboho; van Zyl, Robyn L.] Univ Witwatersrand, Fac Hlth Sci, WITS Res Inst Malaria WRIM, ZA-2193 Johannesburg, South Africa; [Ademola, Idowu Kehinde; Gordon, Michelle] Univ KwaZulu Natal, Coll Hlth Sci, Sch Lab Med & Med Sci, ZA-4000 Durban, South Africa; [Pooe, Ofentse Jacob] Univ KwaZulu Natal, Sch Life Sci, Discipline Biochem, ZA-4000 Durban, South Africa; [Mudau, Pertunia T.; Zininga, Tawanda] Univ Venda, Sch Math & Nat Sci, Dept Biochem, ZA-0950 Thohoyandou, South Africa; [Zininga, Tawanda; Shonhai, Addmore] Stellenbosch Univ, Dept Biochem, ZA-7600 Stellenbosch, South Africa; [Nyamori, Vincent O.] Univ KwaZulu Natal, Sch Chem & Phys, Westville Campus, ZA-4000 Durban, South Africa in 2021, Cited 43. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9. Application In Synthesis of 3,4-Dimethoxybenzaldehyde

Presently, artemisinin-based combination therapy (ACT) is the first-line therapy of Plasmodium falciparum malaria. With the emergence of malaria parasites that are resistant to ACT, alternative antimalarial therapies are urgently needed. In line with this, we designed and synthesised a series of novel N-(7chloroquinolin-4-yl)-N’-(4,6-diphenylpyrimidin-2-yl)alkanediamine hybrids (6a-7c) and evaluated their inhibitory activity against the NF54 chloroquine-susceptible strain as a promising class of antimalarial compounds. The antiplasmodial screening revealed that seven analogues showed promising to good activity with half-maximal inhibitory concentration ( IC50) = 0.32 mu Me4.30 mM. Compound 7a with 1,4-diamine butyl linker and 4-hydroxyl phenyl on fourth and sixth position of pyrimidine core showed the most prominent activity with an IC50 value of 0.32 +/- 0.06 mM, with a favourable safety profile of 9.79 to human kidney epithelial (HEK293) cells. The remaining six analogues showed moderate activity with IC50 values ranging from 7.50 mM to 83.01 mM. We further investigated the binding affinities of the molecules to two essential cytosolic P. falciparum heat shock protein 70 homologues; PfHsp70-1 and PfHsp70-z. Compound 7a exhibited the highest binding affinity for both PfHsp70s with K-D in a lower nanomolar range (4.4-11.4 nM). Furthermore, molecular docking revealed that compounds 6, 6k, 7b and 7a exhibited better fitness in PfHsp70-1 with compound 7a showing the highest and lowest binding scores of similar to 9.8 kcal/mol. Therefore, we speculate that PfHsp70-1 is one of the targets of these inhibitors. The bioisoteric replacement of the groups at phenyl ring at the fourth and sixth position of the pyrimidine core had a constructive association with antiplasmodial activity. The promising antiplasmodial activity of the synthesised analogues illustrates how crucial molecular hybridisation is as a strategy in the development of quinoline-pyrimidine hybrids as prospective antiprotozoal agents. (C) 2021 Elsevier Masson SAS. All rights reserved.

Application In Synthesis of 3,4-Dimethoxybenzaldehyde. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Kayamba, F; Malimabe, T; Ademola, IK; Pooe, OJ; Kushwaha, ND; Mahlalela, M; van Zyl, RL; Gordon, M; Mudau, PT; Zininga, T; Shonhai, A; Nyamori, VO; Karpoormath, R or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Product Details of 98-17-9. I found the field of Pharmacology & Pharmacy very interesting. Saw the article A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF5) and pentafluoroethyl (C2F5) substituents: Improved antiproliferative agents against prostate cancer published in 2019, Reprint Addresses Pertusati, F (corresponding author), Sch Pharm & Pharmaceut Sci, Redwood Bldg,King Edwards 7 Ave, Cardiff CF10 3NB, S Glam, Wales.. The CAS is 98-17-9. Through research, I have a further understanding and discovery of 3-(Trifluoromethyl)phenol.

SAR studies on bicalutamide, enobosarm and enzalutamide analogues, functionalised with polyfluorinated groups, is presented. Among the novel bicalutamide and enobosarm derivatives synthesised, several displayed significantly improved in vitro anticancer activity, with IC50 values in the low micromolar range against four different prostate cancer cell lines (LNCaP, VCaP, DU-145 and 22Rv1), showing up to 48-fold increase in comparison with the parent structures. In particular, SF5 enobosarm analogues were found to be most potent compounds, full AR antagonists and with favourable ADME properties. The most promising compound (48a) was evaluated for its in vivo efficacy in PC xenograft mouse model (22Rv1) with results comparable to the standard-of-care docetaxel. (C) 2019 Published by Elsevier Masson SAS.

About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Pertusati, F; Ferla, S; Bassetto, M; Brancale, A; Khandil, S; Westwell, AD; McGuigan, C or concate me.. Product Details of 98-17-9

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Recently I am researching about SUPEROLEOPHILIC NANOFIBROUS MEMBRANES; CYCLOTRIPHOSPHAZENE SYNTHESIS; FLUORINATED BENZOXAZINES; POLYBENZOXAZINE; POLYMERIZATION; DESIGN; FABRICATION; STABILITY; CARDANOL; DIAMINES, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [21274049]. Published in BUDAPEST UNIV TECHNOL & ECON in BUDAPEST ,Authors: Ma, HX; Qiu, JJ; Liu, CM. The CAS is 98-17-9. Through research, I have a further understanding and discovery of 3-(Trifluoromethyl)phenol. Name: 3-(Trifluoromethyl)phenol

Six fluorine-containing, mix-substituted phosphazene-based branched benzoxazine monomers with a low melting point were successfully prepared and their chemical structures were verified by H-1, C-13, P-31 and F-19 nuclear magnetic resonance (NMR). These branched benzoxazine resins underwent thermal ring-opening polymerization to form cured polymers with high thermal stability both in N-2 atmosphere and in air. The co-substituents, both m-CF3PhOH andp-CF3PhOH, imposed significant effects on processing, thermal, and surface properties of corresponding polybenzoxazines. Non-isothermal differential scanning calorimetry (DSC) under diverse heating rates was adopted to investigate the curing kinetics and determine the activation energy of polymerization. DSC results indicate that the m-CF3PhO-/p-CF3PhO- groups have the potential to lower ring-opening polymerization temperature. Glass transition temperatures (T(g)s) of polybenzoxazines derived from p-CF3PhOH are higher than that of polymers derived from m-CF3PhOH due to different steric hindrance and crosslinking density. More interesting, all polybenzoxazines show relatively high dielectric constant but exhibit low dielectric loss at ambient temperature.

Name: 3-(Trifluoromethyl)phenol. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Ma, HX; Qiu, JJ; Liu, CM or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

In 2020 ORG LETT published article about NICKEL-CATALYZED BORYLATION; C-H BORYLATION; ALPHA,BETA-UNSATURATED CARBONYL; ALKYLBORONIC ESTERS; COUPLING REACTIONS; SECONDARY; HALIDES; FUNCTIONALIZATION; HYDROBORATION; REACTIVITY in [Verma, Piyush Kumar; Prasad, K. Sujit; Varghese, Dominic; Geetharani, K.] Indian Inst Sci, Dept Inorgan & Phys Chem, Bangalore 560012, Karnataka, India in 2020, Cited 61. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9. COA of Formula: C7H5F3O

A cobalt-complex-catalyzed borylation of a wide range of alkyl halides with a diboron reagent (B(2)pin(2) or B(2 )neop(2)) has been developed under mild reaction conditions, demonstrating the first cobalt-mediated cross-coupling with alkyl electrophiles. This protocol allows alkyl boronic esters to be accessed from alkyl halides, including alkyl chlorides, which were used rarely as coupling partners. Mechanistic studies reveal the possible involvement of an alkyl radical intermediate in this cobalt-mediated catalytic cycle.

COA of Formula: C7H5F3O. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Verma, PK; Prasad, KS; Varghese, D; Geetharani, K or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Recently I am researching about MULTIKINASE INHIBITOR; DISCOVERY; RESISTANCE; SORAFENIB; MUTATIONS; PATHWAY, Saw an article supported by the National Science FoundationNational Science Foundation (NSF) [CHE-1455306]; Canadian Cancer Society Research InstituteCanadian Cancer Society (CCS) [704116]; Canada Research Chair ProgramCanada Research Chairs; Canadian Institutes for Health ResearchCanadian Institutes of Health Research (CIHR) [FDN143277]; Stauffer Endowed Fellowship, USC Graduate School; USC Dornsife Chemical Biology Training Program; TD Bank postdoctoral fellowship; NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCESUnited States Department of Health & Human ServicesNational Institutes of Health (NIH) – USANIH National Institute of General Medical Sciences (NIGMS) [P30GM124165] Funding Source: NIH RePORTER. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Assadieskandar, A; Yu, CQ; Maisonneuve, P; Kunnov, I; Sicheri, F; Zhang, C. The CAS is 98-17-9. Through research, I have a further understanding and discovery of 3-(Trifluoromethyl)phenol. Category: indole-building-block

One effective means to achieve inhibitor specificity for RAF kinases, an important family of cancer drug targets, has been to target the monomeric inactive state conformation of the kinase domain, which, unlike most other kinases, can accommodate sulfonamide-containing drugs such as vemurafenib and dabrafenib because of the presence of a unique pocket specific to inactive RAF kinases. We previously reported an alternate strategy whereby rigidification of a nonselective pyrazolo[3,4-d]pyrimidine-based inhibitor through ring closure afforded moderate but appreciable increases in selectivity for RAF kinases. Here, we show that a further application of the rigidification strategy to a different pyrazolopyrimidine-based scaffold dramatically improved selectivity for RAF kinases. Crystal structure analysis confirmed our inhibitor design hypothesis revealing that 21 engages an active-like state conformation of BRAF normally associated with poorly discriminating inhibitors. When screened against a panel of distinct cancer cell lines, the optimized inhibitor 21 primarily inhibited the proliferation of the expected BRAF(V600E)-harboring cell lines consistent with its kinome selectivity profile. These results suggest that rigidification could be a general and powerful strategy for enhancing inhibitor selectivity against protein kinases, which may open up therapeutic opportunities not afforded by other approaches.

Category: indole-building-block. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Assadieskandar, A; Yu, CQ; Maisonneuve, P; Kunnov, I; Sicheri, F; Zhang, C or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

An article Regio- and Stereoselective Synthesis of Enynyl-Aryl Ethers Enabled by Copper/Iodide Tandem Catalysis WOS:000481018100001 published article about C-H BOND; TERMINAL ALKYNES; COPPER; PALLADIUM; HALIDES; ALKENES; ESTERS; IODINATION; COMPLEXES; PHENOLS in [Wu, Yun-Bin; Xiao, Lin; Mao, Chun-Li; Zang, Zhong-Lin; Zhou, Cheng-He; Cai, Gui-Xin] Southwest Univ, Key Lab Luminescent & Real Time Analyt Chem, Minist Educ,Sch Chem & Chem Engn, Key Lab Appl Chem Chongqing Municipal,Inst Bioorg, Chongqing 400715, Peoples R China; [Cai, Gui-Xin] Beijing Natl Lab Mol Sci, Beijing 100190, Peoples R China in 2019, Cited 82. Category: indole-building-block. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9

An approach to preparing enynyl-aryl ethers from phenols and phenylacetylenes is described. This method without extra ligands, overcoming the favored Glaser-Hay dimerization of alkyne, features a wide substrate scope (38 examples including endofolliculina and indole) and the merits of high atom and step economy, good regio- and stereoselectivity (Z-isomers major) in moderate to good isolated yields. Mechanistic studies show that the reaction is enabled by distinctive copper/iodide tandem catalysis.

Category: indole-building-block. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Wu, YB; Xiao, L; Mao, CL; Zang, ZL; Zhou, CH; Cai, GX or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Authors Aly, AA; Hassan, AA; Mohamed, NK; Abd El-Haleem, LE; Brase, S in SAGE PUBLICATIONS LTD published article about in [Aly, Ashraf A.; Hassan, Alaa A.; Mohamed, Nasr K.; Abd El-Haleem, Lamiaa E.] Menia Univ, Fac Sci, Chem Dept, El Minia 61519, Egypt; [Brase, Stefan] Karlsruhe Inst Technol, Inst Biol & Chem Syst Funct Mol Syst IBCS FMS, Eggenstein Leopoldshafen, Germany in 2020, Cited 13. COA of Formula: C9H7NO2. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3

A novel series of 7,8-dichlorobenzofuro[3,2-c]quinoline-6,9,10(5H)-triones was obtained regioselectively in good yields. The products were formed by the reactions of the 4-hydroxy-2(1H)-quinolinones with 3,4,5,6-tetrachloro-1,2-benzoquinone in tetrahydrofuran as the solvent. Infrared, nuclear magnetic resonance (two-dimensional nuclear magnetic resonance), mass spectra and elemental analysis were used to elucidate the structures of new compounds.

COA of Formula: C9H7NO2. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Aly, AA; Hassan, AA; Mohamed, NK; Abd El-Haleem, LE; Brase, S or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Recently I am researching about PHOSPHORYLATION CASCADE; HYPERTENSION; COTRANSPORTER; MUTATIONS, Saw an article supported by the JSPS Core-to-Core Program, A. Advanced Research Networks; Japan Agency for Medical Research and Development (AMED)Japan Agency for Medical Research and Development (AMED) [JP20am0101098]. Published in PERGAMON-ELSEVIER SCIENCE LTD in OXFORD ,Authors: Fujii, S; Kikuchi, E; Watanabe, Y; Suzuyama, H; Ishigami-Yuasa, M; Mori, T; Isobe, K; Uchida, S; Kagechika, H. The CAS is 98-17-9. Through research, I have a further understanding and discovery of 3-(Trifluoromethyl)phenol. Recommanded Product: 3-(Trifluoromethyl)phenol

We report here structural development of N-(4-phenoxyphenyl)benzamide derivatives as novel SPAK (STE20/ SPS1-related proline/alanine-rich kinase) inhibitors. Abnormal activation of the signal cascade of with-no-lysine kinase (WNK) with OSR1 (oxidative stress-responsive kinase 1)/SPAK and NCC (NaCl cotransporter) results in characteristic salt-sensitive hypertension, and therefore inhibitors of the WNK-OSR1/SPAK-NCC cascade are candidates for antihypertensive drugs. Based on the structure of lead compound 2, we examined the SAR of N-(4-phenoxyphenyl)benzamide derivatives, and developed compound 20l as a potent SPAK inhibitor. Compounds 20l is a promising candidate for a new class of antihypertensive drugs.

Recommanded Product: 3-(Trifluoromethyl)phenol. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Fujii, S; Kikuchi, E; Watanabe, Y; Suzuyama, H; Ishigami-Yuasa, M; Mori, T; Isobe, K; Uchida, S; Kagechika, H or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

SDS of cas: 98-17-9. Gilles, P; Veryser, C; Vangrunderbeeck, S; Ceusters, S; Van Meervelt, L; De Borggraeve, WM in [Gilles, Philippe; Veryser, Cedrick; Vangrunderbeeck, Sarah; Ceusters, Sam; De Borggraeve, Wim M.] Katholieke Univ Leuven, Dept Chem, Mol Design & Synth, Celestijnenlaan 200F,Box 2404, B-3001 Leuven, Belgium; [Van Meervelt, Luc] Katholieke Univ Leuven, Dept Chem, Biochem Mol & Struct Biol, Celestijnenlaan 200F,Box 2404, B-3001 Leuven, Belgium published Synthesis of N-Acyl Sulfamates from Fluorosulfates and Amides in 2019, Cited 34. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9.

A novel synthetic strategy toward N-acyl sulfamates was developed. Interestingly, fluorosulfates, a new emerging class of electrophiles, were used to construct the sulfamate core. This precludes handling of chlorosulfonyl isocyanate and sulfamoyl chloride. In combination with amides, a wide and diverse set of N-acyl sulfamates was synthesized, including functionalized bioactive compounds. Furthermore, initial results showed that this method is also amenable to access N-thioacyl sulfamates.

About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Gilles, P; Veryser, C; Vangrunderbeeck, S; Ceusters, S; Van Meervelt, L; De Borggraeve, WM or concate me.. SDS of cas: 98-17-9

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles