Day: October 8, 2021

Recently I am researching about FEEDBACK ACTIVATION; DRUG-RESISTANCE; DERIVATIVES; BREAST, Saw an article supported by the Major science and technology projects of Guangxi Zhuang Autonomous Region [AA17204090]; Wenzhou science and technology project [Y20170280]; Medical Scientific Research Fund of Zhejiang Province [2019322308]; National Natural Science Funding of ChinaNational Natural Science Foundation of China (NSFC) [21762006]; Specific research project of Guangxi for research bases and talents [2017AD19029]. Published in WILEY in HOBOKEN ,Authors: Xu, LY; Qiu, SS; Yang, LH; Xu, HT; Liu, X; Fan, SQ; Cui, R; Fu, WT; Zhao, CG; Shen, LQ; Wang, LX; Huang, XY. The CAS is 99-93-4. Through research, I have a further understanding and discovery of 4′-Hydroxyacetophenone. Recommanded Product: 99-93-4

Lung cancer is a leading cause of cancer-related death worldwide. Cyanopyridines and aminocyanopyridines with carbon-nitrogen bonds have been proved to exert significant anticancer, antibacterial, and anti-inflammatory effects. In this study, we showed that aminocyanopyridine 3o and 3k displaying potent antitumor activity via inhibiting the signal transducer and activator of transcription 3 (STAT3) pathway. They blocked the constitutive STAT3 phosphorylation in a dose- and time-dependent manner and regulated the transcription of STAT3 target genes encoding apoptosis factors. Most importantly, 3o also inhibited interleukin-6-induced STAT3 activation and nuclear localization. Furthermore, 3o significantly inhibited the tumor growth of H460-derived xenografts. Taken together, these findings suggest that 3o and 3k are promising therapeutic drug candidates for lung cancer by inhibiting persistent STAT3 signaling.

About 4′-Hydroxyacetophenone, If you have any questions, you can contact Xu, LY; Qiu, SS; Yang, LH; Xu, HT; Liu, X; Fan, SQ; Cui, R; Fu, WT; Zhao, CG; Shen, LQ; Wang, LX; Huang, XY or concate me.. Recommanded Product: 99-93-4

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

Elbastawesy, MAI; Aly, AA; Ramadan, M; Elshaier, YAMM; Youssif, BGM; Brown, AB; Abuo-Rahma, GEDA in [Elbastawesy, Mohammed A., I; Ramadan, Mohamed] Al Azhar Univ, Fac Pharm, Dept Pharmaceut Organ Chem, Assiut 71524, Egypt; [Aly, Ashraf A.] Menia Univ, Fac Sci, Dept Chem, Al Minya 61519, Egypt; [Elshaier, Yaseen A. M. M.] Univ Sadat City, Fac Pharm, Dept Organ & Med Chem, Menoufia 32958, Egypt; [Youssif, Bahaa G. M.] Assiut Univ, Fac Pharm, Dept Pharmaceut Organ Chem, Assiut 71526, Egypt; [Brown, Alan B.] Florida Inst Technol, Program Chem, Melbourne, FL 32901 USA; [Abuo-Rahma, Gamal El-Din A.] Menia Univ, Fac Pharm, Dept Med Chem, Al Minya 61519, Egypt published Novel Pyrazoloquinolin-2-ones: Design, synthesis, docking studies, and biological evaluation as antiproliferative EGFR-TK inhibitors in 2019, Cited 50. Recommanded Product: 4-Hydroxyquinolin-2(1H)-one. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3.

Two new series of diethyl 2-[2-(substituted-2-oxo-1,2-dihydroquinolin-4-yl)hydrazono]-succinates 6a-g and 1-(2-oxo-1,2-dihydroquinolin-4-yl)-1H-pyrazoles 7a-f have been designed and synthesized. The structures of the synthesized compounds were proved by IR, mass, NMR (2D) spectra and elemental analyses. The target compounds were evaluated for their in vitro cytotoxic activity against 60 cancer cell lines according to NCI protocol. Consequently, seven compounds were further examined against the most sensitive cell lines, leukemia CCRFCEM, and MOLT-4. 5-Amino-1-(6-bromo-2-oxo-1,2-dihydroquinolin-4-yl)-1H-pyrazole-3,4-dicarbonitrile (7f) was the most active product, with IC50= 1.35 uM and 2.42 uM against MOLT-4 and CCRF-CEM, respectively. Also, it showed a remarkable inhibitory activity compared to erlotinib on the EGFR TK with IC50 = 247.14 nM and 208.42 nM, respectively. Cell cycle analysis of MOLT-4 cells treated with 7f showed cell cycle arrest at G2/M phase (supported by Caspases, BAX and Bcl-2 studies) with a significant pro-apoptotic activity as indicated by annexin V-FITC staining. Moreover, the docking study indicated that both the pyrazole moiety and the quinolin-2-one ring showed good fitting into EGFR (PDB code: 1M17). In order to interpret SAR of the designed compounds, and provide a basis for further optimization, molecular docking of the synthesized compounds to known EGFR inhibitors was performed. The study illustrated the effect of several factors on the compounds’ activity.

Recommanded Product: 4-Hydroxyquinolin-2(1H)-one. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Elbastawesy, MAI; Aly, AA; Ramadan, M; Elshaier, YAMM; Youssif, BGM; Brown, AB; Abuo-Rahma, GEDA 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

Recommanded Product: m-Methoxyphenol. Recently I am researching about ASYMMETRIC CATALYSIS; SALEN, Saw an article supported by the . Published in ROYAL SOC CHEMISTRY in CAMBRIDGE ,Authors: Lamb, KJ; Dowsett, MR; North, M; Parker, RR; Whitwood, AC. The CAS is 150-19-6. Through research, I have a further understanding and discovery of m-Methoxyphenol

The synthesis of novel tetrahydroquinoxalines by a metal induced one-electron reductive cyclisation of salophen ligands was found to occur when a salophen ligand was treated with chromium(ii) chloride or decamethylcobaltocene.

About m-Methoxyphenol, If you have any questions, you can contact Lamb, KJ; Dowsett, MR; North, M; Parker, RR; Whitwood, AC or concate me.. Recommanded Product: m-Methoxyphenol

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 Photochemical O-H Functionalization of Aryldiazoacetates with Phenols via Proton Transfer WOS:000574921100033 published article about INSERTION in [Empel, Claire; Jana, Sripati; Pei, Chao; Koenigs, Rene M.] Rhein Westfal TH Aachen, Inst Organ Chem, D-52074 Aachen, Germany; [Empel, Claire; Thanh Vinh Nguyen; Koenigs, Rene M.] Univ New South Waley, Sch Chem, Sydney, NSW 2052, Australia in 2020, Cited 44. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9. Recommanded Product: 98-17-9

In this work, we report a thorough investigation of the reaction of phenols with aryldiazoacetates. Mechanistic studies using different spectroscopic methods and theoretical calculations suggest a hydrogen bond between phenol and aryldiazoacetates, which can be modulated by the phenol acidity. The pK(A) of phenol and therefore the hydrogen bond plays an important role in a subsequent photoinduced proton transfer reaction to give the formal O-H functionalization product of phenols.

Recommanded Product: 98-17-9. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Empel, C; Jana, S; Pei, C; Nguyen, TV; Koenigs, RM 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

COA of Formula: C7H8O. Recently I am researching about CHLOROPHYLL-A DERIVATIVES; EXTRA RING; CHLORIN; ANTIOXIDANT; FRAGMENTS; GLYCOL, Saw an article supported by the . Published in MAIK NAUKA/INTERPERIODICA/SPRINGER in NEW YORK ,Authors: Tulaeva, LA; Gileva, NV; Belykh, DV. The CAS is 100-51-6. Through research, I have a further understanding and discovery of Benzyl Alcohol

The reaction of methyl pheophorbide a with various alcohols in toluene in the presence of dimethylaminopyridine as a base was investigated. Under these conditions, a chemoselective transesterification of the exocyclic ring proceeds without the use of an activating agent (N-methyl-2-chloropyridinium iodide) or a catalyst (molecular iodine).

COA of Formula: C7H8O. About Benzyl Alcohol, If you have any questions, you can contact Tulaeva, LA; Gileva, NV; Belykh, DV 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, synthesis and biological evaluation of fused naphthofuro[3,2-c]quinoline-6,7,12-triones and pyrano[3,2-c]quinoline-6,7,8,13-tetraones derivatives as ERK inhibitors with efficacy in BRAF-mutant melanoma WOS:000455479600032 published article about ACQUIRED-RESISTANCE; IN-VITRO; PROTEIN; DISCOVERY; DOCKING; PHOSPHORYLATION; ACTIVATION; PRODUCTS; QUINONES; BVD-523 in [Aly, Ashraf A.; El-Sheref, Essmat M.; Bakheet, Momtaz E. M.; Ibrahim, Mahmoud A. A.] Menia Univ, Fac Sci, Chem Dept, El Minia 61519, Egypt; [Mourad, Mai A. E.] Port Said Univ, Med Chem Dept, Fac Pharm, Port Said 42526, Egypt; [Kaoud, Tamer S.] Menia Univ, Fac Pharm, Dept Med Chem, El Minia 61519, Egypt; [Brase, Stefan] Karlsruhe Inst Technol, Inst Toxikol & Genet, Hermann von Helmholts Pl 1,Campus Nord, D-76344 Eggenstein Leopoldsha, Germany; [Brase, Stefan] Inst Toxikol & Genet, Hermann von Helmholts Pl 1,Campus Nord, D-76344 Eggenstein Leopoldsha, Germany; [Nieger, Martin] Univ Helsinki, Dept Chem, POB 55, Helsinki 00014, Finland; [Garvalov, Boyan K.] Mannhe Univ Heidelberg, Ctr Biomed & Med Technol Mannheim, Med Fac, D-68167 Mannheim, Germany; [Dalby, Kevin N.; Kaoud, Tamer S.] Univ Texas Austin, Div Chem Biol & Med Chem, Austin, TX 78712 USA in 2019, Cited 57. Recommanded Product: 4-Hydroxyquinolin-2(1H)-one. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3

Approximately 60% of human cancers exhibit enhanced activity of ERK1 and ERK2, reflecting their multiple roles in tumor initiation and progression. Acquired drug resistance, especially mechanisms associated with the reactivation of the MAPK (RAF/MEK/ERK) pathway represent a major challenge to current treatments of melanoma and several other cancers. Recently, targeting ERK has evolved as a potentially attractive strategy to overcome this resistance. Herein, we report the design and synthesis of novel series of fused naphthofuro[3,2-c] quinoline-6,7,12-triones 3a-f and pyrano[3,2-c]quinoline-6,7,8,13-tetraones 5a,b and 6, as potential ERK inhibitors. New inhibitors were synthesized and identified by different spectroscopic techniques and X-ray crystallography. They were evaluated for their ability to inhibit ERK1/2 in an in vitro radioactive kinase assay. 3b and 6 inhibited ERK1 with IC50s of 0.5 and 0.19 mu M, and inhibited ERK2 with IC50s of 0.6 and 0.16 mu M respectively. Kinetic mechanism studies revealed that the inhibitors are ATP-competitive inhibitors where 6 inhibited ERK2 with a K-i of 0.09 mu M. Six of the new inhibitors were tested for their in vitro anticancer activity against the NCI-60 panel of tumor cell lines. Compound 3b and 6 were the most potent against most of the human tumor cell lines tested. Moreover, 3b and 6 inhibited the proliferation of the BRAF mutant A375 melanoma cells with IC50s of 3.7 and 0.13 mu M, respectively. In addition, they suppressed anchorage-dependent colony formation. Treatment of the A375 cell line with 3b and 6 inhibited the phosphorylation of ERK substrates p-90RSK and ELK-1 and induced apoptosis in a dose dependent manner. Finally, a molecular docking study showed the potential binding mode of 3b and 6 within the ATP catalytic binding site of ERK2.

About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Aly, AA; El-Sheref, EM; Bakheet, MEM; Mourad, MAE; Brase, S; Ibrahim, MAA; Nieger, M; Garvalov, BK; Dalby, KN; Kaoud, TS or concate me.. Recommanded Product: 4-Hydroxyquinolin-2(1H)-one

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

Recommanded Product: Benzyl Alcohol. Abbasi, YA; Shahida, S; Ali, A; Khan, MH in [Abbasi, Y. A.] Univ Azad Jammu & Kashmir, Dept Chem, Muzaffarabad, AJK, Pakistan; [Abbasi, Y. A.; Ali, A.] Pakistan Inst Nucl Sci & Technol, Chem Div, PO Nilore, Islamabad, Pakistan; [Shahida, S.] Univ Poonch, Rawalakot, Azad Jammu & Ka, Pakistan; [Ali, A.; Khan, M. H.] Women Univ Azad Jammu & Kashmir Bagh, Bagh, Pakistan published Liquid-liquid extraction of mercury(II) from aqueous solution using furosemide in benzyl alcohol in 2019.0, Cited 42.0. The Name is Benzyl Alcohol. Through research, I have a further understanding and discovery of 100-51-6.

A simple, efficient and economical liquid-liquid extraction method has been developed for quantitative extraction of mercury(II) from aqueous buffer solution using furosemide in benzyl alcohol. The effect of various parameters and of various anions and cations on the extraction of mercury(II) was investigated. The separation factor of mercury was quite high in the presence of a number of transition and rare earth metals at pH 3.5. Among strippants, sodium thiosulphate was found most suitable, and the recovery of mercury was noted to be 98%. The stoichiometric composition of the extracted species was found to be [Hg(FS)(2)].

Recommanded Product: Benzyl Alcohol. About Benzyl Alcohol, If you have any questions, you can contact Abbasi, YA; Shahida, S; Ali, A; Khan, MH 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

Sigalapalli, DK; Pooladanda, V; Kadagathur, M; Guggilapu, SD; Uppu, JL; Godugu, C; Bathini, NB; Tangellamudi, ND in [Sigalapalli, Dilep Kumar; Kadagathur, Manasa; Guggilapu, Sravanthi Devi; Uppu, Jaya Lakshmi; Tangellamudi, Neelima D.] Natl Inst Pharmaceut Educ & Res NIPER, Dept Med Chem, Hyderabad 500037, Andhra Pradesh, India; [Bathini, Nagendra Babu] Indian Inst Chem Technol, CSIR, Fluoroagrochem, Hyderabad 500007, Andhra Pradesh, India; [Pooladanda, Venkatesh; Godugu, Chandraiah] Natl Inst Pharmaceut Educ & Res NIPER, Dept Regulatory Toxicol, Hyderabad 500037, Andhra Pradesh, India; [Guggilapu, Sravanthi Devi] NIDDK, NIH, Lab Bioorgan Chem, Bethesda, MD 20892 USA published Novel chromenyl-based 2-iminothiazolidin-4-one derivatives as tubulin polymerization inhibitors: Design, synthesis, biological evaluation and molecular modelling studies in 2021.0, Cited 52.0. Recommanded Product: 3,4-Dimethoxybenzaldehyde. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9.

Here-in, we present molecular design, chemical synthesis and evaluation of novel chromenyl-based 2-iminothiazolidin-4-one derivatives as tubulin polymerization inhibitors. The newly synthesized compounds were evaluated for their in vitro cytotoxicities against A549 (lung cancer), MDA-MB-231 and BT-471 (breast cancer), HepG2 (liver cancer) and HCT-116 (colon cancer) cell lines by MTT assay. Among the synthesized compounds, compound 12b showed excellent anticancer activity on MDA-MB-231 cell line with IC50 value of 0.95 +/- 1.88 mu M and was verified to be safe in normal human bronchial epithelial cells (Beas-2B). Apoptosis induced by the lead 12b was observed using morphological observations, AO/EB and DAPI staining procedures. Further, dose-dependent increase in the depolarization of mitochondrial membrane was also observed through JC-1 staining. Annexin V-FITC/PI assay confirmed that 12b induced early apoptosis. Additionally, cell cycle analysis indicated that the MDA-MB-231 cells were arrested at sub-G2/M phase and also inhibited tubulin polymerization with IC50 value of 3.54 +/- 0.2 mM. Molecular docking simulations were employed to identify the important binding modes responsible for the tubulin inhibitory activity, thus supporting their effective anticancer potential. (c) 2020 Published by Elsevier B.V.

Recommanded Product: 3,4-Dimethoxybenzaldehyde. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Sigalapalli, DK; Pooladanda, V; Kadagathur, M; Guggilapu, SD; Uppu, JL; Godugu, C; Bathini, NB; Tangellamudi, ND 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

Formula: C7H8O. In 2020.0 POLYM CHEM-UK published article about RING-OPENING POLYMERIZATION; CYCLIC OLEFIN; POLYMERS; COPOLYMERIZATION; CATALYSTS; EPOXIDES; PLASTICS; WASTE; ROUTE; ACID in [Xu, Yuechao; Sucu, Theona; Perry, Mitchell R.; Shaver, Michael P.] Univ Manchester, Sch Nat Sci, Dept Mat, Manchester M13 9PL, Lancs, England; [Shaver, Michael P.] Univ Manchester, Henry Royce Inst, Oxford Rd, Manchester M13 9PL, Lancs, England in 2020.0, Cited 35.0. The Name is Benzyl Alcohol. Through research, I have a further understanding and discovery of 100-51-6.

Alicyclic polymers with in-chain aliphatic rings promote improved thermal and optical performance due to backbone rigidity but remain limited in their functional diversity. In this paper we report the first polyester system with solely alicyclic ring connectivity, afforded through ring-opening of a bicyclic dioxane-4-one ring. Polymerisation of the accessibletransisomer is challenging, but affords a novel family of polymers and copolymers.

Formula: C7H8O. About Benzyl Alcohol, If you have any questions, you can contact Xu, YC; Sucu, T; Perry, MR; Shaver, MP 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

Application In Synthesis of 4-Hydroxyquinolin-2(1H)-one. In 2019 J AGR FOOD CHEM published article about MICROBIAL-PRODUCTION; SALICYLATE BIOSYNTHESIS; PURIFICATION; ENZYME in [Choo, Hye Jeong; Ahn, Joong-Hoon] Konkuk Univ, Bio Mol Informat Ctr, Dept Biosci & Biotechnol, Seoul 05029, South Korea in 2019, Cited 31. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3.

Intermediates in aromatic amino acid biosynthesis can serve as substrates for the synthesis of bioactive compounds. In this study we used two intermediates in the shikimate pathway of Escherichia coli, chorismate and anthranilate, to synthesize three bioactive compounds: 4-hydroxycoumarin (4-HC), 2,4-dihydroxyquinoline (DHQ), and 4-hydroxy-1-methyl-2(1H)-quinolone (NMQ). We introduced genes for the synthesis of salicylic acid from chorismate to supply the substrate for 4-HC and the gene encoding N-methyltransferase for the synthesis of N-methylanthranilate from anthranilate. Polyketide synthases and coenzyme (Co)A ligases were tested to determine the optimal combination of genes for the synthesis of each compound. We also tested several constructs and identified the best one for increasing levels of endogenous substrates for chorismate, anthranilate, and malonyl-CoA. With the use of these strategies, 255.4 mg/L 4-HC, 753.7 mg/L DHQ, and 17.5 mg/L NMQwere synthesized. This work provides a basis for the synthesis of diverse coumarin and quinoline derivatives with potential medical applications.

Application In Synthesis of 4-Hydroxyquinolin-2(1H)-one. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Choo, HJ; Ahn, JH 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