M.W=150-200 | - Page 129 of 152 - Indole Building Blocks

The important role of 3-(Trifluoromethyl)phenol

Application In Synthesis of 3-(Trifluoromethyl)phenol. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Dai, H; Huang, ML; Qian, JQ; Liu, J; Meng, C; Li, YY; Ming, GX; Zhang, T; Wang, SL; Shi, YJ; Yao, Y; Ge, SS; Zhang, YN; Ling, Y or concate me.

An article Excellent antitumor and antimetastatic activities based on novel coumarin/pyrazole oxime hybrids WOS:000461402400039 published article about BIOLOGICAL EVALUATION; COUMARIN DERIVATIVES; MOLECULAR DOCKING; ANTICANCER ACTIVITY; PYRAZOLE; DESIGN; APOPTOSIS; POTENT; AGENTS; METASTASIS in [Dai, Hong; Huang, Meiling; Wang, Senling; Shi, Yujun; Yao, Yong; Ge, Shushan; Ling, Yong] Nantong Univ, Coll Chem & Chem Engn, Nantong 226019, Peoples R China; [Dai, Hong; Huang, Meiling; Qian, Jianqiang; Liu, Ji; Meng, Chi; Li, Yangyang; Ming, Guxu; Zhang, Ting; Ge, Shushan; Zhang, Yanan; Ling, Yong] Nantong Univ, Sch Pharm, Nantong 226001, Peoples R China; [Qian, Jianqiang; Liu, Ji; Meng, Chi; Li, Yangyang; Ming, Guxu; Zhang, Ting; Zhang, Yanan; Ling, Yong] Nantong Univ, Jiangsu Prov Key Lab Inflammat & Mol Drug Target, Nantong 226001, Peoples R China in 2019, Cited 49. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9. Application In Synthesis of 3-(Trifluoromethyl)phenol

A series of hybrids 10a-v based on coumarin/pyrazole oxime have been synthesized, and exhibit good to excellent antitumor activities. Compound 10n has shown remarkable anticancer effect on SMMC-7721 cells (IC50 = 2.08 mu M), which is considerably lower than 5-FU (IC50 = 37.8 mu M) and similar to ADM (IC50 = 2.67 mu M), with little effect on normal hepatic cells LO2. Notably, the suppression experiments of metastatic activities reveal that 10n also displays significant anti-metastasis effects through inhibiting cell migration and invasion in highly metastatic SMMC-7721 cell line, and dose-dependently reverses TGF-beta 1-induced epithelial-mesenchymal transition (EMT) procedure better than ADM. Finally, 10n also possesses low acute toxicity and potent tumor growth inhibitory property against SMMC-7721 cell lines in vivo. Our findings suggest that novel coumarin/pyrazole oxime hybrids are promising therapeutic agent candidates for further research. (C) 2019 Elsevier Masson SAS. All rights reserved.

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

How did you first get involved in researching 120-14-9

Name: 3,4-Dimethoxybenzaldehyde. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Fan, TY; Yang, YX; Zeng, QX; Wang, XL; Wei, W; Guo, XX; Zhao, LP; Song, DQ; Wang, YX; Wang, L; Hong, B or concate me.

Name: 3,4-Dimethoxybenzaldehyde. In 2021 BIOORG CHEM published article about HETEROZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA; HIGH CARDIOVASCULAR RISK; LDL; DEGRADATION; INHIBITION; EVOLOCUMAB; EXPRESSION; EFFICACY; THERAPY; SAFETY in [Fan, Tian-Yun; Yang, Yu-Xin; Zeng, Qing-Xuan; Wang, Xue-Lei; Wei, Wei; Guo, Xi-Xi; Zhao, Li-Ping; Song, Dan-Qing; Wang, Yan-Xiang; Wang, Li; Hong, Bin] Chinese Acad Med Sci & Peking Union Med Coll, Inst Med Biotechnol, Beijing 10050, Peoples R China in 2021, Cited 31. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9.

Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a secreted protein and its deficiency markedly enhanced the survival rate of patient with cardiovascular diseases (CVDs). Forty berberine (BBR) derivatives were synthesized and evaluated for their activities on down-regulating the transcription of PCSK9 in HepG2 cells, taking BBR as the lead. Structure-activity relationship (SAR) analysis revealed that 2,3-dimethoxy moiety might be beneficial for activity. Among them, 9k displayed the most potent activity with IC50 value of 9.5 +/- 0.5 mu M, better than that of BBR. Also, it significantly decreased PCSK9 protein level at cellular level, as well as in the liver and serum of mice in vivo. Furthermore, 9k markedly increased LDLR expression and LDL-C clearance via downregulating PCSK9 protein. The mechanism of action of 9k is targeting HNF1 alpha and/or Sp1 cluster modulation upstream of PCSK9, a different one from BBR. Therefore, 9k might have the potential to be a novel PCSK9 transcriptional inhibitor for the treatment of atherosclerosis, worthy for further investigation.

Discovery of 120-14-9

Formula: C9H10O3. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Shahari, MSB; Junaid, A; Tiekink, ERT; Dolzhenko, AV or concate me.

Authors Shahari, MSB; Junaid, A; Tiekink, ERT; Dolzhenko, AV in GEORG THIEME VERLAG KG published article about in [Shahari, Muhammad Syafiq Bin; Dolzhenko, Anton, V] Monash Univ Malaysia, Sch Pharm, Jalan Lagoon Selatan, Bandar Sunway 47500, Selangor Darul, Malaysia; [Junaid, Ahmad] Purdue Univ, Dept Med Chem & Mol Pharmacol, W Lafayette, IN 47907 USA; [Tiekink, Edward R. T.] Sunway Univ, Res Ctr Crystalline Mat, Sch Med & Life Sci, 5 Jalan Univ, Bandar Sunway 47500, Selangor Darul, Malaysia; [Dolzhenko, Anton, V] Curtin Univ, Fac Hlth Sci, Sch Pharm & Biomed Sci, Curtin Hlth Innovat Res Inst, GPO Box U1987, Perth, WA 6845, Australia in 2021.0, Cited 47.0. Formula: C9H10O3. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9

A new method for the fast synthesis of diverse 4-aryl-6-cycloamino-1,3,5-triazin-2-amines was developed. The synthesis is performed under microwave irradiation in a one-pot manner from cyanoguanidine, aromatic aldehydes, and cyclic amines. Their three-component reaction in the presence of hydrochloric acid produced dihydrotriazines, which were then converted (without isolation) into the targeted compounds via aromatic dehydrogenation in the presence of alkali. The reaction tolerated various aromatic aldehydes (including heterocyclic) and cyclic amities. Crystal structures of two representative 4-aryl-6-morpholino-1,3,5-triazin-2-amines were established by X-ray crystallography. The results of preliminary biological screening identified potent antileukemic activity for 6-[3,4-dihydroisoquinolin-2(1H)-yl]-4- phenyl-1,3,5-triazin-2-amine.

Formula: C9H10O3. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Shahari, MSB; Junaid, A; Tiekink, ERT; Dolzhenko, AV or concate me.

What Kind of Chemistry Facts Are We Going to Learn About 98-17-9

Formula: C7H5F3O. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Manganaro, R; Zonsics, B; Bauer, L; Lopez, ML; Donselaar, T; Zwaagstra, M; Saporito, F; Ferla, S; Strating, JRPM; Coutard, B; Hurdiss, DL; van Kuppeveld, FJM; Brancale, A or concate me.

An article Synthesis and antiviral effect of novel fluoxetine analogues as enterovirus 2C inhibitors WOS:000540343900005 published article about POLIOVIRUS; REPLICATION; PROTEIN; ATPASE; CLASSICS; MOTIF in [Manganaro, Roberto; Zonsics, Birgit; Lopez, Moira Lorenzo; Saporito, Fabiana; Ferla, Salvatore; Brancale, Andrea] Cardiff Univ, Sch Pharm & Pharmaceut Sci, King Edward VII Ave, Cardiff CF10 3NB, Wales; [Bauer, Lisa; Donselaar, Tim; Zwaagstra, Marleen; Strating, Jeroen R. P. M.; Hurdiss, Daniel L.; van Kuppeveld, Frank J. M.] Univ Utrecht, Fac Vet Med, Dept Infect Dis & Immunol, Virol Div, NL-3584 CL Utrecht, Netherlands; [Coutard, Bruno] UVE Aix Marseille Univ, Inserm 1207, IHU Mediterranee Infect, Unite Virus Emergents,IRD 190, Marseille, France; [Coutard, Bruno] Aix Marseille Univ, CNRS, AFMB UMR 7257, Marseille, France in 2020, Cited 24. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9. Formula: C7H5F3O

Enteroviruses (EV) are a group of positive-strand RNA ( + RNA) viruses that include many important human pathogens (e.g. poliovirus, coxsackievirus, echovirus, numbered enteroviruses and rhinoviruses). Fluoxetine was identified in drug repurposing screens as potent inhibitor of enterovirus B and enterovirus D replication. In this paper we are reporting the synthesis and the antiviral effect of a series of fluoxetine analogues. The results obtained offer a preliminary insight into the structure-activity relationship of its chemical scaffold and confirm the importance of the chiral configuration. We identified a racemic fluoxetine analogue, 2b, which showed a similar antiviral activity compared to (S)-fluoxetine. Investigating the stereochemistry of 2b revealed that the Senantiomer exerts potent antiviral activity and increased the antiviral spectrum compared to the racemic mixture of 2b. In line with the observed antiviral effect, the Senantiomer displayed a dose-dependent shift in the melting temperature in thermal shift assays, indicative for direct binding to the recombinant 2C protein.

How did you first get involved in researching 3,4-Dimethoxybenzaldehyde

About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Saffarian, H; Karimi, F; Yarie, M; Zolfigol, MA or concate me.. HPLC of Formula: C9H10O3

In 2021 J MOL STRUCT published article about DERIVATIVES in [Saffarian, Haniyeh; Karimi, Fatemeh; Yarie, Meysam; Zolfigol, Mohammad Ali] Bu Ali Sina Univ, Fac Chem, Dept Organ Chem, Hamadan, Hamadan, Iran in 2021, Cited 81. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9. HPLC of Formula: C9H10O3

Fe3O4@SiO2@(CH2)(3)-urea-quinoline sulfonic acid chloride, as a novel and efficient nanomagnetic catalyst bearing urea linkers, was designed, synthesized and then fully characterized by using various techniques. To investigate the catalytic activity of the described catalyst, it was used for the synthesis of coumarin containing 1,4-dihydropyridines (DHPs), through a condensation reaction of aromatic aldehydes, 4-hydroxycoumarin, and ammonium acetate under solvent-free conditions. This procedure includes important aspects like simple procedure, simplicity of product isolation using water, decreasing the temperature of reaction, disuse of solvent, high to excellent yields, environmentally benign reaction conditions and short reaction times. Also, the presented catalyst was recycled and reused for at least five times with only a negligible decrease in its catalytic activity. The applied catalyst has both acidic and H-bond donor-acceptor sites so that it can use as a dual role catalytic system. (C) 2020 Elsevier B.V. All rights reserved.

About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Saffarian, H; Karimi, F; Yarie, M; Zolfigol, MA or concate me.. HPLC of Formula: C9H10O3

Downstream Synthetic Route Of 4-Hydroxyquinolin-2(1H)-one

HPLC of Formula: C9H7NO2. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Marjani, AP; Khalafy, J; Farajollahi, A or concate me.

In 2019 J HETEROCYCLIC CHEM published article about TETRAPROPYLAMMONIUM BROMIDE; BIOLOGICAL EVALUATION; DERIVATIVES; CATALYST; WATER in [Marjani, Ahmad Poursattar; Khalafy, Jabbar; Farajollahi, Ayda] Urmia Univ, Dept Organ Chem, Fac Chem, Orumiyeh, Iran in 2019, Cited 41. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3. HPLC of Formula: C9H7NO2

In this research, in order to synthesize a series of ethyl 2-amino-4-benzoyl-5-oxo-5,6-dihydro-4H-pyrano[3,2-c]quinoline-3-carboxylates, a green and an efficient method is proposed through one-pot three-component reaction of substituted arylglyoxals, ethyl cyanoacetate, and 4-hydroxyquinolin-2(1H)-one in the presence of terapropylammonium bromide as a catalyst in good yields. All synthesized new substances were characterized by FTIR, H-1-NMR, and C-13-NMR spectral data and elemental analysis.

HPLC of Formula: C9H7NO2. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Marjani, AP; Khalafy, J; Farajollahi, A or concate me.

Get Up to Speed Quickly on Emerging Topics:86-95-3

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.. COA of Formula: C9H7NO2

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. COA of 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.

A new application about98-17-9

Safety of 3-(Trifluoromethyl)phenol. 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.

An article Synthesis of N-Acyl Sulfamates from Fluorosulfates and Amides WOS:000456632800058 published article about SIDEROPHORE BIOSYNTHESIS; NUCLEOSIDE ANTIBIOTICS; ARYL FLUOROSULFONATES; MECHANISM; FLUORIDE; ACYLTRANSFERASE; TUBERCULOSIS; ASCAMYCIN; PHENOLS; TARGET 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 in 2019, Cited 34. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9. Safety of 3-(Trifluoromethyl)phenol

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.

Machine Learning in Chemistry about 4-Hydroxyquinolin-2(1H)-one

Computed Properties of C9H7NO2. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Block, TM; Young, JAT; Javanbakht, H; Sofia, MJ; Zhou, TL or concate me.

An article Host RNA quality control as a hepatitis B antiviral target WOS:000657774400001 published article about NONCANONICAL POLY(A) POLYMERASE; POLYADENYLATION SIGNAL; MOLECULAR-BIOLOGY; STEM-LOOP; VIRUS; DEGRADATION; EXOSOME; TRAMP; DECAY; TRANSCRIPTS in [Block, Timothy M.; Zhou, Tianlun] Baruch S Blumberg Inst, Doylestown, PA 18902 USA; [Young, John A. T.] F Hoffmann La Roche Ltd, Roche Innovat Ctr Basel, Roche Pharma Res & Early Dev, Basel, Switzerland; [Javanbakht, Hassan] SQZ Biotechnol, 200 Arsenal Yards Blvd,Suite 210, Watertown, MA 02472 USA; [Sofia, Michael J.] Arbutus Biopharma Inc, 701 Vet Circle, Warminster, PA 18974 USA in 2021, Cited 69. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3. Computed Properties of C9H7NO2

Inhibition of the host RNA polyadenylating polymerases, PAPD5 and PAPD7 (PAPD5/7), with dihydroquinolizinone, a small orally available, molecule, results in a rapid and selective degradation of hepatitis B virus (HBV) RNA, and hence reduction in the amounts of viral gene products. DHQ, is a first in class investigational agent and could represent an entirely new category of HBV antivirals. PAPD5 and PAPD7 are noncanonical, cell specified, polyadenylating polymerases, also called terminal nucleotidyl transferases 4B and 4A (TENT4B/A), respectively. They are involved in the degradation of poor-quality cell transcripts, mostly noncoding RNAs and in the maturation of a sub-set of transcripts. They also appear to play a role in shielding some mRNA from degradation. The results of studies with DHQ, along with other recent findings, provide evidence that repression of the PAPD5/7 arm of the cell RNA quality control pathway, causes a profound (multifold) reduction rather than increase, in the amount of HBV pre-genomic, pre-core and HBsAg mRNA levels in tissue culture and animal models, as well. In this review we will briefly discuss the need for new HBV therapeutics and provide background about HBV transcription. We also discuss cellular degradation of host transcripts, as it relates to a new family of anti-HBV drugs that interfere with these processes. Finally, since HBV mRNA maturation appears to be selectively sensitive to PAPD5/7 inhibition in hepatocytes, we discuss the possibility of targeting host RNA quality control as an antiviral strategy.

Computed Properties of C9H7NO2. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Block, TM; Young, JAT; Javanbakht, H; Sofia, MJ; Zhou, TL or concate me.

An update on the compound challenge: 3,4-Dimethoxybenzaldehyde

Name: 3,4-Dimethoxybenzaldehyde. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Kostopoulou, I; Tzani, A; Polyzos, NI; Karadendrou, MA; Kritsi, E; Pontiki, E; Liargkova, T; Hadjipavlou-Litina, D; Zoumpoulakis, P; Detsi, A or concate me.

An article Exploring the 2 ‘-Hydroxy-Chalcone Framework for the Development of Dual Antioxidant and Soybean Lipoxygenase Inhibitory Agents WOS:000650694300001 published article about OXIDATIVE STRESS; CHALCONES in [Kostopoulou, Ioanna; Tzani, Andromachi; Polyzos, Nestor-Ioannis; Karadendrou, Maria-Anna; Detsi, Anastasia] Natl Tech Univ Athens, Sch Chem Engn, Dept Chem Sci, Lab Organ Chem, Heroon Polytechniou 9,Zografou Campus, Athens 15780, Greece; [Kritsi, Eftichia; Zoumpoulakis, Panagiotis] Natl Hellen Res Fdn, Inst Chem Biol, 48 Vas Constantinou Ave, Athens 11635, Greece; [Kritsi, Eftichia; Zoumpoulakis, Panagiotis] Univ West Attica, Dept Food Sci & Technol, Ag Spyridonos 12243, Egaleo, Greece; [Pontiki, Eleni; Liargkova, Thalia; Hadjipavlou-Litina, Dimitra] Aristotle Univ Thessaloniki, Sch Pharm, Lab Pharmaceut Chem, Fac Hlth Sci, Thessaloniki 54124, Greece in 2021.0, Cited 78.0. Name: 3,4-Dimethoxybenzaldehyde. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9

2 ‘-hydroxy-chalcones are naturally occurring compounds with a wide array of bioactivity. In an effort to delineate the structural features that favor antioxidant and lipoxygenase (LOX) inhibitory activity, the design, synthesis, and bioactivity profile of a series of 2 ‘-hydroxy-chalcones bearing diverse substituents on rings A and B, are presented. Among all the synthesized derivatives, chalcone 4b, bearing two hydroxyl substituents on ring B, was found to possess the best combined activity (82.4% DPPH radical scavenging ability, 82.3% inhibition of lipid peroxidation, and satisfactory LOX inhibition value (IC50 = 70 mu M). Chalcone 3c, possessing a methoxymethylene substituent on ring A, and three methoxy groups on ring B, exhibited the most promising LOX inhibitory activity (IC50 = 45 mu M). A combination of in silico techniques were utilized in an effort to explore the crucial binding characteristics of the most active compound 3c and its analogue 3b, to LOX. A common H-bond interaction pattern, orienting the hydroxyl and carbonyl groups of the aromatic ring A towards Asp768 and Asn128, respectively, was observed. Regarding the analogue 3c, the bulky (-OMOM) group does not seem to participate in a direct binding, but it induces an orientation capable to form H-bonds between the methoxy groups of the aromatic ring B with Trp130 and Gly247.