What kind of challenge would you like to see in a future of compound:4-Methoxybenzaldehyde

Recommanded Product: 123-11-5. Bye, fridends, I hope you can learn more about C8H8O2, If you have any questions, you can browse other blog as well. See you lster.

Recommanded Product: 123-11-5. Authors Rao, TN; Krishnarao, N; Ahmed, F; Alomar, SY; Albalawi, F; Mani, P; Aljaafari, A; Parvatamma, B; Arshi, N; Kumar, S in MDPI published article about in [Rao, Tentu Nageswara; Krishnarao, Nalla] Krishna Univ, Dept Chem, Machilipatnam 521001, Andhra Pradesh, India; [Ahmed, Faheem; Aljaafari, Abdullah; Kumar, Shalendra] King Faisal Univ, Dept Phys, Coll Sci, Al Hufuf 31982, Al Ahsa, Saudi Arabia; [Alomar, Suliman Yousef] King Saud Univ, Zool Dept, Coll Sci, Doping Res Chair, Riyadh 11451, Saudi Arabia; [Albalawi, Fadwa] King Saud Univ, Zool Dept, Coll Sci, Riyadh 11451, Saudi Arabia; [Mani, Panagal] Dept Biotechnol, Annai Coll Arts Sci, Kumbakonam 612503, Tamil Nadu, India; [Parvatamma, Botsa] GayathriPG Courses, Dept Organ Chem, Gotlam, Vizianagaram 530045, India; [Arshi, Nishat] King Faisal Univ, Dept Basic Sci, Preparatory Year Deanship, Al Hufuf, Al Ahsa, Saudi Arabia; [Kumar, Shalendra] Univ Petr & Energy Studies, Sch Engn, Dept Phys, Dehra Dun 248007, Uttarakhand, India in 2021, Cited 37. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5

A simple and highly efficient protocol for the synthesis of derivatives 7, 7-dimethyl-4-phenyl-2-thioxo-2, 3, 4, 6, 7, 8-hexahydro-1H-quinazoline-5-one from 5, 5-dimethyl cyclohexane-1, 3-dione (4a-4h) (dimedone) has been described. The aryl aldehydes were substituted with thiourea in the presence of synthesized zinc ferrite nanocatalyst, which increased the yield under reflux through condensation, followed by cyclization to give desired products. The other advantages are that it is eco-friendly and economically affordable for large-scale production. Structural validation and characterization of all the newly synthesized compounds were evaluated by spectral analysis (mass spectrometry, proton nuclear magnetic resonance ((HNMR)-H-1), and Carbon-13 nuclear magnetic resonance((CNMR)-C-13)spectroscopies. The structure of antibacterial and antifungal assays was performed with the newly synthesized compounds. The antimicrobial activity of title compounds possessing electron-withdrawing groups such as (4e-4h) (Cl, Br, and cyano group) exhibited more active potential than the electron-donating groups, C6H5,4-C6H4, 3-OC2H5-4OH-C6H3, etc., (4a-4d) containing moiety.

Recommanded Product: 123-11-5. Bye, fridends, I hope you can learn more about C8H8O2, 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

Brief introduction of Mequinol

Welcome to talk about 150-76-5, If you have any questions, you can contact Wander, DPA; van der Zanden, SY; Vriends, MBL; van Veen, BC; Vlaming, JGC; Bruyning, T; Hansen, T; van der Marel, GA; Overkleeft, HS; Neefjes, JJC; Codee, JDC or send Email.. HPLC of Formula: C7H8O2

In 2021.0 J ORG CHEM published article about OXOCARBENIUM IONS; DOXORUBICIN; ALKYNYLBENZOATES; DAUNORUBICIN; DAUNOSAMINE; DERIVATIVES; SUBSTITUENT in [Wander, Dennis P. A.; Vriends, Merijn B. L.; van Veen, Branca C.; Vlaming, Joey G. C.; Bruyning, Thomas; Hansen, Thomas; van der Marel, Gijsbert A.; Overkleeft, Herman S.; Codee, Jeroen D. C.] Leiden Univ, Leiden Inst Chem, NL-2333 CC Leiden, Netherlands; [van der Zanden, Sabina Y.; Neefjes, Jacques J. C.] Leiden Univ, ONCODE Inst, Med Ctr, NL-2333 ZC Leiden, Netherlands; [Hansen, Thomas] Vrije Univ Amsterdam, Amsterdam Ctr Multiscale Modeling ACMM, Amsterdam Inst Mol & Life Sci AIMSS, Dept Theoret Chem, NL-1081 HV Amsterdam, Netherlands in 2021.0, Cited 32.0. The Name is Mequinol. Through research, I have a further understanding and discovery of 150-76-5. HPLC of Formula: C7H8O2

Anthracyclines are effective drugs in the treatment of various cancers, but their use comes with severe side effects. The archetypal anthracycline drug, doxorubicin, displays two molecular modes of action: DNA double-strand break formation (through topoisomerase II alpha poisoning) and chromatin damage (via eviction of histones). These biological activities can be modulated and toxic side effects can be reduced by separating these two modes of action through alteration of the aminoglycoside moiety of doxorubicin. We herein report on the design, synthesis, and evaluation of a coherent set of configurational doxorubicin analogues featuring all possible stereoisomers of the 1,2-amino-alcohol characteristic for the doxorubicin 3-amino-2,3-dideoxyfucoside, each in nonsubstituted and N,N-dimethylated forms. The set of doxorubicin analogues was synthesized using appropriately protected 2,3,6-dideoxy-3-amino glycosyl donors, equipped with an alkynylbenzoate anomeric leaving group, and the doxorubicin aglycon acceptor. The majority of these glycosylations proceeded in a highly stereoselective manner to provide the desired axial alpha-linkage. We show that both stereochemistry of the 3-amine carbon and N-substitution state are critical for anthracycline cytotoxicity and generally improve cellular uptake. N,N-Dimethylepirubicin is identified as the most potent anthracycline that does not induce DNA damage while remaining cytotoxic.

Welcome to talk about 150-76-5, If you have any questions, you can contact Wander, DPA; van der Zanden, SY; Vriends, MBL; van Veen, BC; Vlaming, JGC; Bruyning, T; Hansen, T; van der Marel, GA; Overkleeft, HS; Neefjes, JJC; Codee, JDC or send Email.. HPLC of Formula: C7H8O2

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

Why do aromatic interactions matter of compound:150-76-5

Name: Mequinol. About Mequinol, If you have any questions, you can contact Jia, RF; Zhang, J; Bertagnin, C; Cherukupalli, S; Ai, W; Ding, X; Li, Z; Zhang, JW; Ju, H; Ma, XL; Loregian, A; Huang, B; Zhan, P; Liu, XY or concate me.

Name: Mequinol. Authors Jia, RF; Zhang, J; Bertagnin, C; Cherukupalli, S; Ai, W; Ding, X; Li, Z; Zhang, JW; Ju, H; Ma, XL; Loregian, A; Huang, B; Zhan, P; Liu, XY in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER published article about in [Jia, Ruifang; Cherukupalli, Srinivasulu; Ai, Wei; Ding, Xiao; Li, Zhuo; Zhang, Jiwei; Ju, Han; Zhan, Peng; Liu, Xinyong] Shandong Univ, Cheeloo Coll Med, Sch Pharmaceut Sci, Dept Med Chem,Key Lab Chem Biol,Minist Educ, 44 West Culture Rd, Jinan 250012, Shandong, Peoples R China; [Zhang, Jian] Shandong Univ, Hosp 2, Cheeloo Coll Med, Inst Med Sci, Jinan 250033, Shandong, Peoples R China; [Bertagnin, Chiara; Loregian, Arianna] Univ Padua, Dept Mol Med, Via Gabelli 63, I-35121 Padua, Italy; [Ma, Xiuli; Huang, Bing] Shandong Acad Agr Sci, Inst Poultry Sci, 1 Jiaoxiao Rd, Jinan 250023, Shandong, Peoples R China; [Zhan, Peng; Liu, Xinyong] China Belgium Collaborat Res Ctr Innovat Antivira, 44 West Culture Rd, Jinan 250012, Shandong, Peoples R China in 2021, Cited 41. The Name is Mequinol. Through research, I have a further understanding and discovery of 150-76-5

Encouraged by our earlier discovery of N1-selective inhibitors, the 150-cavity of influenza virus neuraminidases (NAs) could be further exploited to yield more potent oseltamivir derivatives. Herein, we report the design, synthesis and biological evaluation of a series of novel oseltamivir derivatives via the structural modifications at C-5-NH2 of oseltamivir targeting 150-cavity. Among them, compound 5c bearing 4-(3-methoxybenzyloxy)benzyl group exhibited the most potent activity, which was lower or modestly improved activities than oseltamivir carboxylate (OSC) against N1 (H1N1), N1 (H5N1) and N1 (H5N1-H274Y). Specifically, there was 30-fold loss of activity against the wild-type strain H1N1. However, 5c displayed 4.85-fold more potent activity than OSC against H5N1-H274Y NA. Also, 5c demonstrated low cytotoxicity in vitro and no acute toxicity in mice. Molecular docking studies provided insights into the high potency of 5c against N1 and N1-H274Y mutant NAs. Besides, the in silico prediction of physicochemical properties and CYP enzymatic inhibitory ability of representative compounds were conducted to evaluate their drug-like properties. (C) 2020 Elsevier Masson SAS. All rights reserved.

Name: Mequinol. About Mequinol, If you have any questions, you can contact Jia, RF; Zhang, J; Bertagnin, C; Cherukupalli, S; Ai, W; Ding, X; Li, Z; Zhang, JW; Ju, H; Ma, XL; Loregian, A; Huang, B; Zhan, P; Liu, XY 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

Extracurricular laboratory: Synthetic route of m-Methoxyphenol

Quality Control of m-Methoxyphenol. Welcome to talk about 150-19-6, If you have any questions, you can contact Costello, JP; Ferreira, EM or send Email.

Recently I am researching about HOMOPROPARGYLIC ALCOHOLS; ENOL-ETHERS; CYCLOISOMERIZATION; HYDROAMINATION; BOND; HYDROALKOXYLATION; CYCLIZATION; INDOLES; ACETALS; ROUTE, Saw an article supported by the National Institutes of Health (NIGMS)United States Department of Health & Human ServicesNational Institutes of Health (NIH) – USANIH National Institute of General Medical Sciences (NIGMS) [R01GM110560]; NIHUnited States Department of Health & Human ServicesNational Institutes of Health (NIH) – USA [S10RR028859]; NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCESUnited States Department of Health & Human ServicesNational Institutes of Health (NIH) – USANIH National Institute of General Medical Sciences (NIGMS) [R01GM110560] Funding Source: NIH RePORTER. Quality Control of m-Methoxyphenol. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Costello, JP; Ferreira, EM. The CAS is 150-19-6. Through research, I have a further understanding and discovery of m-Methoxyphenol

The steric and electronic drivers of regioselectivity in platinum -catalyzed intramolecular hydroalkoxylation are elucidated. A branch point is found that divides the process between 5-exo and 6-endo selective processes, and enol ethers can be accessed in good yields for both oxygen heterocycles. The main influence arises from an electronic effect, where the alkyne substituent induces a polarization of the alkyne that leads to preferential heteroatom attack at the more electron -deficient carbon. The electronic effects are studied in other contexts, including hydroacyloxylation and hydroamination, and similar trends in directionality are predominant although not uniformly observed.

Quality Control of m-Methoxyphenol. Welcome to talk about 150-19-6, If you have any questions, you can contact Costello, JP; Ferreira, EM 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

Extended knowledge of 123-11-5

SDS of cas: 123-11-5. Welcome to talk about 123-11-5, If you have any questions, you can contact Morita, S; Yoshimura, T; Matsuo, J or send Email.

SDS of cas: 123-11-5. Authors Morita, S; Yoshimura, T; Matsuo, J in ROYAL SOC CHEMISTRY published article about in [Morita, Shunya; Yoshimura, Tomoyuki; Matsuo, Jun-ichi] Kanazawa Univ, Div Pharmaceut Sci, Grad Sch Med Sci, Kakuma Machi, Kanazawa, Ishikawa 9201192, Japan in 2021.0, Cited 40.0. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5

Three-component reactions of nitroalkanes, acrylamides, and aldehydes by using a catalytic amount of KOH in DMSO gave beta ‘-hydroxy-gamma-nitro amides. Mechanistic studies suggested that the reactions proceeded by domino Michael/aldol reactions. The highly nucleophilic nature of transient amide enolates that were formed by Michael addition of nitronate anions to acrylamides in DMSO enabled the realization of catalytic intermolecular aldol reactions of amide enolates in the presence of acidic nitroalkanes.

SDS of cas: 123-11-5. Welcome to talk about 123-11-5, If you have any questions, you can contact Morita, S; Yoshimura, T; Matsuo, J 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

The important role of 80-59-1

HPLC of Formula: C5H8O2. Bye, fridends, I hope you can learn more about C5H8O2, If you have any questions, you can browse other blog as well. See you lster.

An article Palladium-Catalyzed Regioselective C-H Functionalization/Annulation Reaction of Amides and Allylbenzenes for the Synthesis of Isoquinolinones and Pyridinones WOS:000637001800031 published article about OXIDATIVE CYCLIZATION; DIRECTING GROUP; ALLYLATION; ACTIVATION; ANNULATION; ISOINDOLINONES; C(SP(3))-H; ARYLATION; ALKENES; OLEFINS in [Zhong, Rong; Xu, Yong; Wang, Yurong] Zhejiang Chinese Med Univ, Sch Pharmaceut Sci, Hangzhou 310053, Peoples R China; [Sun, Manman] Taizhou Univ, Adv Res Inst, Taizhou 318000, Peoples R China; [Sun, Manman] Taizhou Univ, Dept Chem, Taizhou 318000, Peoples R China in 2021, Cited 81. HPLC of Formula: C5H8O2. The Name is (E)-2-Methylbut-2-enoic acid. Through research, I have a further understanding and discovery of 80-59-1

A regioselective C-H functionalization/annulation reaction of N-sulfonyl amides and allylbenzenes through a palladium-catalyzed C(sp(2))-H allylation/aminopalladation/beta-H elimination/isomerization sequence has been reported. Various aryl and alkenyl carboxamides are found to be efficient substrates to construct isoquinolinones and pyridinones in up to 96% yield. Using ambient air as the terminal oxidant is another advantage regarding environmental friendliness and operational simplicity.

HPLC of Formula: C5H8O2. Bye, fridends, I hope you can learn more about C5H8O2, 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

Archives for Chemistry Experiments of Mequinol

HPLC of Formula: C7H8O2. About Mequinol, If you have any questions, you can contact Ou, GC; Wang, Q; Zhou, Q; Wang, XF or concate me.

HPLC of Formula: C7H8O2. Authors Ou, GC; Wang, Q; Zhou, Q; Wang, XF in MDPI published article about in [Ou, Guangchuan; Wang, Qiong; Zhou, Qiang] Hunan Univ Sci & Engn, Coll Chem & Bioengn, Yongzhou 425199, Hunan, Peoples R China; [Wang, Xiaofeng] Univ South China, Sch Chem & Chem Engn, Hengyang 421001, Hunan, Peoples R China in 2021.0, Cited 30.0. The Name is Mequinol. Through research, I have a further understanding and discovery of 150-76-5

Five host-guest trimesic-acid-based hydrogen-bonds framework compounds with different guests, namely [(TMA)(4)center dot(TMB)(3)] (1), [(TMA)(2)center dot(DMB)(1.5)] (2), [(TMA)(6)center dot(MP)] (3), [(TMA)center dot(EP)] (4) and [(TMA)center dot(PP)] (5) (TMA = trimesic acid, TMB = 1,3,5-trimethoxybenzene, DMB = 1,4-dimethoxybenzene, MP = 4-methoxyphenol, EP = 4-ethoxyphenol and PP = 4-propoxyphenol), were obtained through co-crystallization, and were characterized by elemental analysis, infrared spectroscopy analysis, and thermogravimetric analysis. The trimesic acid molecules comprise a hydrogen bonding six-membered cyclic host network that is found in a two-dimensional arrangement in compounds 1 and 2, and in a nine-fold interpenetrated three-dimensional structure in compound 3. In compounds 4 and 5, the trimesic acid and EP/PP molecules form a hydrogen-bonded six-membered cyclic network, resulting in a one-dimensional chain structure through O-H horizontal ellipsis O hydrogen bonds.

HPLC of Formula: C7H8O2. About Mequinol, If you have any questions, you can contact Ou, GC; Wang, Q; Zhou, Q; Wang, XF 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 update on the compound challenge: 4-Methoxybenzaldehyde

Recommanded Product: 4-Methoxybenzaldehyde. Welcome to talk about 123-11-5, If you have any questions, you can contact Nafie, MS; Mahgoub, S; Amer, AM or send Email.

Recently I am researching about 3-COMPONENT SYNTHESIS; QUINOLINE; DESIGN; DISCOVERY; HYBRIDS; SULFIDE; JAK2, Saw an article supported by the . Published in WILEY in HOBOKEN ,Authors: Nafie, MS; Mahgoub, S; Amer, AM. The CAS is 123-11-5. Through research, I have a further understanding and discovery of 4-Methoxybenzaldehyde. Recommanded Product: 4-Methoxybenzaldehyde

Quinoline derivatives are attracting considerable interest due to their biological importance. In this paper, several 2-amino-4-aryl-6-(quinolin-2-ylthio)pyridine-3,5-dicarbonitrile derivatives are synthesized by adopting a one-pot reaction of quinoline-2-thione, aromatic aldehydes, and malononitrile in the presence of sodium hydroxide in absolute ethanol. The structures of these newly synthesized compounds were determined using different spectroscopic techniques, including elemental analyses, IR,H-1 NMR, and MS. The synthesized derivatives were screened for their antimicrobial and cytotoxic activities. Compounds4a,4b,4d, and4eexhibited promising antimicrobial activity compared to antibacterial and antifungal standard drugs. Additionally,4f,4d, and4gshowed potent cytotoxic activity against both MCF-7 and A549 cells with IC(50)values (6.39-9.3 mu M). Our molecular docking results of compound4fprove good binding affinity toward the three tested proteins as Jak2/STATA3 inhibition and are in accordance with the RT-PCR mRNA expressions of the compound against MCF-7 cells which downregulated the Jak2 and STAT3 genes, and this may be the proposed mode of action for anti-breast cancer activity.

Recommanded Product: 4-Methoxybenzaldehyde. Welcome to talk about 123-11-5, If you have any questions, you can contact Nafie, MS; Mahgoub, S; Amer, AM 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

New explortion of m-Methoxyphenol

COA of Formula: C7H8O2. Welcome to talk about 150-19-6, If you have any questions, you can contact Schnell, SD; Hoff, LV; Panchagnula, A; Wurzenberger, MH; Klapotke, TM; Sieber, S; Linden, A; Gademann, K or send Email.

COA of Formula: C7H8O2. Schnell, SD; Hoff, LV; Panchagnula, A; Wurzenberger, MH; Klapotke, TM; Sieber, S; Linden, A; Gademann, K in [Schnell, Simon D.; Hoff, Lukas V.; Panchagnula, Advaita; Sieber, Simon; Linden, Anthony; Gademann, Karl] Univ Zurich, Winterthurerstr 190, CH-8057 Zurich, Switzerland; [Wurzenberger, Maximilian H.; Klapoetke, Thomas M.] Ludwig Maximilians Univ Munchen, Butenandtstr 5-13, D-81377 Munich, Germany published 3-Bromotetrazine: labelling of macromolecules via monosubstituted bifunctional s-tetrazines in 2020.0, Cited 52.0. The Name is m-Methoxyphenol. Through research, I have a further understanding and discovery of 150-19-6.

We report the synthesis and first characterisation of the novel chemical probe 3-bromotetrazine and establish its reactivity towards nucleophiles. This led to the synthesis of several novel classes of 3-monosubstituted s-tetrazines. A remarkable functional group selectivity is observed and is utilised to site-selectively functionalise different complex molecules. The stability of 3-bromotetrazine under the reaction conditions facilitated the development of a protocol for protein functionalisation, which enabled a minimal, bifunctional tetrazine unit as a bio-orthogonal handle for inverse electron demand Diels-Alder reactions. Additionally, a novel tetrazine-based chemical probe was developed and its application in the context of thiol-targeted natural product isolation and labelling of mammalian cells is demonstrated.

COA of Formula: C7H8O2. Welcome to talk about 150-19-6, If you have any questions, you can contact Schnell, SD; Hoff, LV; Panchagnula, A; Wurzenberger, MH; Klapotke, TM; Sieber, S; Linden, A; Gademann, K 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

Awesome and Easy Science Experiments about 86-95-3

Category: indole-building-block. Welcome to talk about 86-95-3, If you have any questions, you can contact Elbastawesy, MAI; Aly, AA; Ramadan, M; Elshaier, YAMM; Youssif, BGM; Brown, AB; Abuo-Rahma, GEDA or send Email.

Recently I am researching about FACTOR RECEPTOR KINASE; SUBSTITUTED QUINOLINONES; PYRAZOLE DERIVATIVES; POTENTIAL ANTICANCER; ERLOTINIB; CANCER; CRIZOTINIB; CHEMISTRY; ASSAY, Saw an article supported by the . Category: indole-building-block. Published in ACADEMIC PRESS INC ELSEVIER SCIENCE in SAN DIEGO ,Authors: Elbastawesy, MAI; Aly, AA; Ramadan, M; Elshaier, YAMM; Youssif, BGM; Brown, AB; Abuo-Rahma, GEDA. The CAS is 86-95-3. Through research, I have a further understanding and discovery of 4-Hydroxyquinolin-2(1H)-one

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.

Category: indole-building-block. Welcome to talk about 86-95-3, If you have any questions, you can contact Elbastawesy, MAI; Aly, AA; Ramadan, M; Elshaier, YAMM; Youssif, BGM; Brown, AB; Abuo-Rahma, GEDA 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