Tag: M.W=150-200

Safety of 4-Hydroxyquinolin-2(1H)-one. Authors Chheda, PR; Kummer, DA; Nishimura, RT; McClure, KJ; Venkatesan, H in AMER CHEMICAL SOC published article about in [Kummer, David A.] Lundbeck La Jolla Res Ctr Inc, San Diego, CA 92121 USA; [Chheda, Pratik R.; Nishimura, Rachel T.; McClure, Kelly J.; Venkatesan, Hariharan] Janssen Res & Dev, Discovery Chem, San Diego, CA 92121 USA in 2021, Cited 63. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3

A one-pot, Hantzsch ester-mediated Knoevenagel condensation-reduction reaction has been developed for alkylation of a wide range of substituted 2,4-quinoline diols and 2,4-pyridine diols with aldehydes. The process is operationally simple to perform, scalable, and provides highly useful C-3 alkylated quinoline and pyridine diols in yields of 58-92%. The alkylation products can be converted to 2,4-dihaloquinoline and pyridine substrates for further functionalization.

Safety of 4-Hydroxyquinolin-2(1H)-one. Bye, fridends, I hope you can learn more about C9H7NO2, If you have any questions, you can browse other blog as well. See you lster.

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

Krapf, MK; Gallus, J; Spindler, A; Wiese, M in [Krapf, Michael K.; Gallus, Jennifer; Spindler, Anna; Wiese, Michael] Univ Bonn, Inst Pharmaceut, Immenburg 4, D-53121 Bonn, Germany published Synthesis and biological evaluation of quinazoline derivatives – A SAR study of novel inhibitors of ABCG2 in 2019, Cited 51. Recommanded Product: 98-17-9. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9.

Multidrug resistance (MDR) is a major obstacle for effective chemotherapeutic treatment of cancer frequently leading to failure of the therapy. MDR is often associated with the overexpression of ABC transport proteins like ABCB1 or ABCG2 which efflux harmful substances out of cells at the cost of ATP hydrolysis. One way to overcome MDR is to apply potent inhibitors of ABC transporters to restore the sensitivity of the cells toward cytostatic agents. This study focusses on the synthesis and evaluation of novel 2,4-disubstituted quinazoline derivatives regarding the structure-activity-relationship (SAR), their ability to reverse MDR and their mode of interaction with ABCG2. Hence, the inhibitory potency and selectivity toward ABCG2 was determined. Moreover, the intrinsic cytotoxicity and the reversal of MDR were investigated. Interaction type studies with the substrate Hoechst 33342 and conformational analyses of ABCG2 with 5D3 monoclonal antibody were performed for a better understanding of the underlying mechanisms. In our study we could further enhance the inhibitory effect against ABCG2 (compound 31, IC50: 55 nM) and identify the structural features that are crucial for inhibitory potency, the impact on transport activity and binding to the protein. (C) 2018 Elsevier Masson SAS. All rights reserved,

Welcome to talk about 98-17-9, If you have any questions, you can contact Krapf, MK; Gallus, J; Spindler, A; Wiese, M or send Email.. Recommanded Product: 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

In 2020 BEILSTEIN J ORG CHEM published article about 2,4-DIHYDROXYQUINOLINE; DERIVATIVES; QUINOLINE; ANALOGS in [Li, Dandan; Oku, Naoya; Igarashi, Yasuhiro] Toyama Prefectural Univ, Biotechnol Res Ctr, 5180 Kurokawa, Imizu, Toyama 9390398, Japan; [Li, Dandan; Oku, Naoya; Igarashi, Yasuhiro] Toyama Prefectural Univ, Dept Biotechnol, 5180 Kurokawa, Imizu, Toyama 9390398, Japan; [Shinozaki, Yukiko] Toyama Coll, Natl Inst Technol, 13 Hongo Machi, Toyama, Toyama 9398630, Japan; [Kurokawa, Yoichi] Fukui Prefectural Univ, Dept Biosci & Biotechnol, Eiheiji Cho, Fukui, Japan in 2020, Cited 45. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3. Quality Control of 4-Hydroxyquinolin-2(1H)-one

4-Hydroxy-3-methyl-2(1H)-quinolone (1), a molecule known for a long time and recently discovered from a Brassicaceae plant Isatis tinctoria without providing sufficient evidence to support the structure, was isolated from a fermentation extract of Burkholderia sp. 3Y-MMP isolated from a soil by a Zn2+ enrichment culture. Detailed spectroscopic analyses by MS and NMR, combined with C-13 chemical shift comparison with literature values of the related compounds and a synthetic preparation of 1, allowed its first full NMR characterization and identification of 2-quinolone but not 2-quinolinol (2) as the preferred tautomer for this heterocyclic system. While the metal-chelating activity was negligible, compound 1 at 10 mu M, a concentration lower than that in liquid production cultures, quenched hydroxy radical-induced chemiluminescence emitted by luminol by 86%. Because some Burkholderia species are pathogenic to plants and animals, the above result suggests that 1 is a potential antioxidant to counteract reactive oxygen species-based immune response in the host organisms.

Welcome to talk about 86-95-3, If you have any questions, you can contact Li, DD; Oku, N; Shinozaki, Y; Kurokawa, Y; Igarashi, Y or send Email.. Quality Control of 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

Name: 3,4-Dimethoxybenzaldehyde. Authors Abosalim, HM; Nael, MA; El-Moselhy, TF in WILEY-V C H VERLAG GMBH published article about in [Abosalim, Heba M.; Nael, Manal A.; El-Moselhy, Tarek F.] Tanta Univ, Fac Pharm, Dept Pharmaceut Chem, Tanta 31527, Egypt in 2021.0, Cited 31.0. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9

Twenty derivatives of chalcones were synthesized and their anticancer activities were estimated against both breast and liver cancer besides two human normal cell lines. Out of our candidates, there were five compounds 3 b, 3 d, 3 h, 7 and 10 b that revealed a broad superlative antitumor activity against both HepG2 and MCF7 cell lines. Surprisingly, 3 h showed the most powerful anticancer activity (GI(50)=5.43 +/- 0.170 mu M for MCF7 and GI(50)=1.80 +/- 0.50 mu M for HepG2) and displayed the most effective inhibition activity on tubulin with IC50=4.51 +/- 0.13 mu M. 3 h exerted low toxicity toward both normal human, Hs371.T and AML12, cell lines. 3 h revealed arrest of cell cycle at G2/M and induced apoptosis compared to control cells. Docking study of all newly derivatives was achieved to decide the preeminent binding mode. Generally, the outcome of the docking study showed that 3 h had better binding mode.

Welcome to talk about 120-14-9, If you have any questions, you can contact Abosalim, HM; Nael, MA; El-Moselhy, TF or send Email.. Name: 3,4-Dimethoxybenzaldehyde

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 ACTIVATION; RHODIUM; AIR; FUNCTIONALIZATION; DERIVATIVES; BONDS, Saw an article supported by the National NSF of ChinaNational Natural Science Foundation of China (NSFC) [21432005, 21672154, 21871193]; Comprehensive Training Platform of Specialized Laboratory, College of Chemistry, Sichuan University. SDS of cas: 98-17-9. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Zhang, LQ; Wang, YB; Shi, Y; Wu, YM; Lan, JB; Ma, WX; You, JS. The CAS is 98-17-9. Through research, I have a further understanding and discovery of 3-(Trifluoromethyl)phenol

An urgent yet challenging task is to overcome the limitations in substrate scope and regio- and chemoselectivity in the oxidative couplings between two arenes for the construction of unsymmetrical 2,2′-difunctional biaryls with diverse application requirements. In this work, a co-oxidant-free Rh(I)/Zn(NTf2)(2)/air catalytic system has been developed for dual chelation-assisted oxidative C-H/C-H cross-couplings between two anilines, between two phenols, and between phenols and anilines, which enables rapid assembly of rich libraries of 2,2′-bianilines, 2,2′-biphenols, and 2′-aminobiphenyl-2-ols. This protocol features air as the sole oxidant, complete regioselectivity, high chemoselectivity, low molar ratio of substrates (even 1:1), convenient operation, and scale-up synthesis. The established catalytic system is tolerant of the substrates having both electron-donating and electron-withdrawing substituents at different positions of the aryl ring. This work further discloses that the chemoselectivity of cross-coupling over homocoupling mainly relies on a suitable combination of two directing groups (i.e., a pair of strongly and weakly coordinating directing groups) rather than the electronically distinct properties between two substrates, which provides an inspiration for designing the matching directing group pair for the dual chelation-assisted oxidative Ar-H/Ar-H cross-couplings. Thus, this strategy allows the highly chemoselective cross-coupling between electronically similar coupling partners, which represents a challenging task in the oxidative Ar-H/Ar-H cross-coupling reactions.

SDS of cas: 98-17-9. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Zhang, LQ; Wang, YB; Shi, Y; Wu, YM; Lan, JB; Ma, WX; You, JS 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

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. HPLC 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.

HPLC of Formula: C9H10O3. Welcome to talk about 120-14-9, If you have any questions, you can contact Chen, L; Lin, ZY; Zhang, XF; Tan, LS; Zhang, M; Li, YB or send Email.

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. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3. Formula: C9H7NO2

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.

Bye, fridends, I hope you can learn more about C9H7NO2, If you have any questions, you can browse other blog as well. See you lster.. Formula: C9H7NO2

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 Kulkarni, MR; Lad, NP; Khedkar, VM; Gaikwad, ND in WILEY published article about in [Kulkarni, Mahesh R.; Lad, Nitin P.; Gaikwad, Nitin D.] KRT Arts BH Commerce & AM Sci Coll, Dept Chem, Organ Chem Res Ctr, Gangapur Rd, Nasik 422002, India; [Khedkar, Vijay M.] Vishwakarma Univ, Sch Pharm, Pune, Maharashtra, India in 2021.0, Cited 22.0. Application In Synthesis of 3,4-Dimethoxybenzaldehyde. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9

With the aim of expanding the scope of SAR on piperlongumine (PL), a naturally occurring anticancer molecule, we have designed a novel hybrid molecule bearing 3,4-dihydroisoquinolin-1(2H)-one and trans-cinnamic acids. The structure, based on hybridization strategy, is used for hybridization of naturally occurring scaffolds. We have synthesized 14 hybrid molecules by coupling 3,4-dihydroisoquinolin-1(2H)-one core with cinnamic acids using the mix anhydride approach. The newly synthesized inhibitors were evaluated for cell viability against breast cancer MCF-7 and cervical cancer HeLa cell lines. Furthermore, the active compounds were screened for their potential in breast cancer MDA-MB-231, cervical cancer C33A cell lines, prostate cancer DU-145, PC-3, and normal VERO cells. From the series, compound 10g was seen to inhibit MCF-7 cell growth significantly with GI(50) < 0.1 mu M along with growth inhibition in MDA-MB-231 (GI(50) = 20 mu M) and C33A (GI(50) = 3.2 mu M). While the inhibitor 10i inhibits MCF-7 breast cancer cell growth GI(50) = 3.42 mu M along with inhibition of cell growth in MDA-MB-231 (GI(50) = 30 mu M), HeLa (GI(50) = 7.67 mu M), C33A (GI(50) = 13 mu M), DU-145 (GI(50) = 6.45 mu M), PC-3 (GI(50) = 8.68 mu M), and VERO (GI(50) = 2.93 mu M), respectively. Furthermore, molecular docking study demonstrated these compounds could bind tightly to the colchicine domain of tubulin through a network of favorable steric and electrostatic interactions and thus act as a tubulin polymerization inhibitor. Welcome to talk about 120-14-9, If you have any questions, you can contact Kulkarni, MR; Lad, NP; Khedkar, VM; Gaikwad, ND or send Email.. Application In Synthesis of 3,4-Dimethoxybenzaldehyde

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 Zhang, XY; Dou, PH; Lu, WY; You, Y; Zhao, JQ; Wang, ZH; Yuan, WC in ROYAL SOC CHEMISTRY published article about in [Zhang, Xia-Yan; Dou, Pei-Hao; Lu, Wen-Ya; You, Yong; Zhao, Jian-Qiang; Wang, Zhen-Hua; Yuan, Wei-Cheng] Chengdu Univ, Inst Adv Study, Chengdu 610106, Peoples R China; [Zhang, Xia-Yan; Dou, Pei-Hao; Lu, Wen-Ya] Chinese Acad Sci, Chengdu Inst Organ Chem, Natl Engn Res Ctr Chiral Drugs, Chengdu 610041, Peoples R China; [Zhang, Xia-Yan; Dou, Pei-Hao; Lu, Wen-Ya] Univ Chinese Acad Sci, Beijing 100049, Peoples R China in 2021.0, Cited 38.0. Product Details of 120-14-9. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9

By taking advantage of benzylidene succinimides as a new class of 3C synthons, a highly diastereo- and enantioselective tandem Mannich reaction/transamidation has been established by reacting them with cyclic trifluoromethyl N-acyl ketimines. Using a Cinchona alkaloid-derived squaramide as the catalyst, the tandem reaction proceeded smoothly under mild conditions and afforded a range of F3C-containing chiral polycyclic dihydroquinazolinones with excellent results (up to 99% yield, all cases >20 : 1 dr, up to 99% ee).

Product Details of 120-14-9. Welcome to talk about 120-14-9, If you have any questions, you can contact Zhang, XY; Dou, PH; Lu, WY; You, Y; Zhao, JQ; Wang, ZH; Yuan, WC or send Email.

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 2021.0 EUR J ORG CHEM published article about STEREOSELECTIVE-SYNTHESIS; CRAFTS CYCLIZATION; NATURAL-PRODUCTS; EPICALYXIN-F; SCH 900229; DERIVATIVES; SCAFFOLDS; TETRAHYDROPYRANS; CONSTRUCTION; HETEROCYCLES in [Satteyyanaidu, Vallabhareddy; Chandrashekhar, Rapelli; Reddy, B. V. Subba] CSIR, Indian Inst Chem Technol, Fluoro & Agrochem, Hyderabad 500007, India; [Satteyyanaidu, Vallabhareddy; Chandrashekhar, Rapelli; Reddy, B. V. Subba] Acad Sci & Innovat Res AcSIR, New Delhi 110025, India; [Lalli, Claudia] Univ Rennes, CNRS, ISCR UMR 6226, F-35000 Rennes, France in 2021.0, Cited 53.0. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9. COA of Formula: C9H10O3

We propose the synthesis of biologically relevant hexahydro-1H-pyrano[3,4-c]chromenes, via a tandem Prins/Friedels-Crafts process, catalyzed by BF3.Et2O, starting from (E)- and (Z)-5-phenoxypent-3-en-1-ol. The diastereoselectivity of the process is controlled by the geometry of the homoallylic alcohol. We also point out that the Prins product can be obtained in high yields and good diastereoselectivity when the reaction is promoted by AlCl3 as Lewis acid in the presence of an external nucleophile.

COA of Formula: C9H10O3. 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:
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