Category: 50-84-0

Yao, Y; Kadam, RU; Lee, CCD; Woehl, JL; Wu, NC; Zhu, XY; Kitamura, S; Wilson, IA; Wolan, DW in [Yao, Yao; Woehl, Jordan L.; Kitamura, Seiya; Wolan, Dennis W.] Scripps Res Inst, Dept Mol Med, La Jolla, CA 92037 USA; [Kadam, Rameshwar U.; Lee, Chang-Chun David; Wu, Nicholas C.; Zhu, Xueyong; Wilson, Ian A.; Wolan, Dennis W.] Scripps Res Inst, Dept Integrat Struct & Computat Biol, La Jolla, CA 92037 USA; [Wilson, Ian A.] Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USA published An influenza A hemagglutinin small-molecule fusion inhibitor identified by a new high-throughput fluorescence polarization screen in 2020, Cited 45. Recommanded Product: 2,4-Dichlorobenzoic acid. The Name is 2,4-Dichlorobenzoic acid. Through research, I have a further understanding and discovery of 50-84-0.

Influenza hemagglutinin (HA) glycoprotein is the primary surface antigen targeted by the host immune response and a focus for development of novel vaccines, broadly neutralizing antibodies (bnAbs), and therapeutics. HA enables viral entry into host cells via receptor binding and membrane fusion and is a validated target for drug discovery. However, to date, only a very few bona fide small molecules have been reported against the HA. To identity new antiviral lead candidates against the highly conserved fusion machinery in the HA stem, we synthesized a fluorescence-polarization probe based on a recently described neutralizing cyclic peptide P7 derived from the complementarity-determining region loops of human bnAbs FI6v3 and CR9114 against the HA stem. We then designed a robust binding assay compatible with high-throughput screening to identify molecules with low micromolar to nanomolar affinity to influenza A group 1 HAs. Our simple, low-cost, and efficient in vitro assay was used to screen H1/Puerto Rico/8/1934 (H1/PR8) HA trimer against similar to 72,000 compounds. The crystal structure of H1/PR8 HA in complex with our best hit compound F0045(S) confirmed that it binds to pockets in the HA stem similar to bnAbs FI6v3 and CR9114, cyclic peptide P7, and small-molecule inhibitor JNJ4796. F0045 is enantioselective against a panel of group 1 HAs and F0045(S) exhibits in vitro neutralization activity against multiple H1N1 and H5N1 strains. Our assay, compound characterization, and small-molecule candidate should further stimulate the discovery and development of new compounds with unique chemical scaffolds and enhanced influenza antiviral capabilities.

Recommanded Product: 2,4-Dichlorobenzoic acid. About 2,4-Dichlorobenzoic acid, If you have any questions, you can contact Yao, Y; Kadam, RU; Lee, CCD; Woehl, JL; Wu, NC; Zhu, XY; Kitamura, S; Wilson, IA; Wolan, DW or concate me.

Reference:
Chloride – Wikipedia,
,Chlorides – an overview | ScienceDirect Topics

An article Practical and rapid construction of 2-pyridyl ketone library in continuous flow WOS:000588040300001 published article about ASYMMETRIC HYDROGENATION; NITRIC-ACID; CHEMISTRY; SYSTEM; GENERATION; CONVERSION; NITRATION; ARYL in [Sun, Maolin; Li, Jianchang; Liang, Chaoming; Shan, Chao; Shen, Xinyuan; Ma, Yueyue; Ye, Jinxing] East China Univ Sci & Technol, Minist Educ, Sch Pharm, Engn Res Ctr Pharmaceut Proc Chem, Shanghai 200237, Peoples R China; [Cheng, Ruihua] East China Univ Sci & Technol, Sch Chem Engn, Shanghai 200237, Peoples R China in 2021, Cited 59. The Name is 2,4-Dichlorobenzoic acid. Through research, I have a further understanding and discovery of 50-84-0. Application In Synthesis of 2,4-Dichlorobenzoic acid

2-Pyridyl ketones widely appear in bioactive molecules, natural products, and are employed as precursors of chiral 2-pyridine alky/aryl alcohols or 2-aminoalkyl pyridine ligands for asymmetric catalysis. Herein, a practical method for the rapid synthesis of 2-pyridyl ketone library in continuous flow is reported, in which the 2-lithiopyridine formed by Br/Li exchange reacts with commercially available esters to obtain 2-pyridyl ketones in a good yield at short reaction time. This protocol functions broadly on a variety of esters and has been applied to the synthesis of TGF-beta type 1 receptor inhibitor LY580276 intermediate in an environmentally friendly method. It is rapid, reliable, and cost-efficient to afford diverse kinds of 2-pyridyl ketones in the compound library.

Application In Synthesis of 2,4-Dichlorobenzoic acid. About 2,4-Dichlorobenzoic acid, If you have any questions, you can contact Sun, ML; Li, JC; Liang, CM; Shan, C; Shen, XY; Cheng, RH; Ma, YY; Ye, JX or concate me.

Reference:
Chloride – Wikipedia,
,Chlorides – an overview | ScienceDirect Topics

Chi, YH; Yeh, TK; Ke, YY; Lin, WH; Tsai, CH; Wang, WP; Chen, YT; Su, YC; Wang, PC; Chen, YF; Wu, ZW; Yeh, JY; Hung, MC; Wu, MH; Wang, JY; Chen, CP; Song, JS; Shih, C; Chen, CT; Chang, CP in [Chi, Ya-Hui; Yeh, Teng-Kuang; Ke, Yi-Yu; Lin, Wen-Hsing; Tsai, Chia-Hua; Wang, Wan-Ping; Chen, Yen-Ting; Su, Yu-Chieh; Wang, Pei-Chen; Chen, Yan-Fu; Wu, Zhong-Wei; Yeh, Jen-Yu; Hung, Ming-Chun; Wu, Mine-Hsine; Wang, Jing-Ya; Chen, Ching-Ping; Song, Jen-Shin; Shih, Chuan; Chen, Chiung-Tong; Chang, Chun-Ping] Natl Hlth Res Inst, Inst Biotechnol & Pharmaceut Res, Zhunan 35053, Taiwan; [Chi, Ya-Hui] China Med Univ, Grad Inst Biomed Sci, Taichung 40402, Taiwan; [Chang, Chun-Ping] Chung Yuan Christian Univ, Dept Chem, Taoyuan 320314, Taiwan published Discovery and Synthesis of a Pyrimidine-Based Aurora Kinase Inhibitor to Reduce Levels of MYC Oncoproteins in 2021, Cited 45. Quality Control of 2,4-Dichlorobenzoic acid. The Name is 2,4-Dichlorobenzoic acid. Through research, I have a further understanding and discovery of 50-84-0.

The A-type Aurora kinase is upregulated in many human cancers, and it stabilizes MYC-family oncoproteins, which have long been considered an undruggable target. Here, we describe the design and synthesis of a series of pyrimidine-based derivatives able to inhibit Aurora A kinase activity and reduce levels of cMYC and MYCN. Through structure-based drug design of a small molecule that induces the DFG-out conformation of Aurora A kinase, lead compound 13 was identified, which potently (IC50 < 200 nM) inhibited the proliferation of high-MYC expressing small-cell lung cancer (SCLC) cell lines. Pharmacokinetic optimization of 13 by prodrug strategies resulted in orally bioavailable 25, which demonstrated an 8-fold higher oral AUC (F = 62.3%). Pharmacodynamic studies of 25 showed it to effectively reduce cMYC protein levels, leading to >80% tumor regression of NCI-H446 SCLC xenograft tumors in mice. These results support the potential of 25 for the treatment of MYC-amplified cancers including SCLC.

About 2,4-Dichlorobenzoic acid, If you have any questions, you can contact Chi, YH; Yeh, TK; Ke, YY; Lin, WH; Tsai, CH; Wang, WP; Chen, YT; Su, YC; Wang, PC; Chen, YF; Wu, ZW; Yeh, JY; Hung, MC; Wu, MH; Wang, JY; Chen, CP; Song, JS; Shih, C; Chen, CT; Chang, CP or concate me.. Quality Control of 2,4-Dichlorobenzoic acid

Reference:
Chloride – Wikipedia,
,Chlorides – an overview | ScienceDirect Topics

An article Design, synthesis and biological evaluation of novel benzodioxole derivatives as COX inhibitors and cytotoxic agents WOS:000571118800001 published article about CYCLOOXYGENASE-2; ANALOGS; ANTICANCER; MECHANISMS; ENZYMES; SAFROLE in [Hawash, Mohammed; Jaradat, Nidal; Hameedi, Saba] An Najah Natl Univ, Fac Med & Hlth Sci, Dept Pharm, POB 7, Nablus 00970, Palestine; [Mousa, Ahmed] An Najah Natl Univ, Fac Med & Hlth Sci, Dept Biomed Sci, Nablus 00970, Palestine in 2020, Cited 37. The Name is 2,4-Dichlorobenzoic acid. Through research, I have a further understanding and discovery of 50-84-0. Recommanded Product: 2,4-Dichlorobenzoic acid

Non-steroidal anti-inflammatory drugs are among the most used drugs. They are competitive inhibitors of cyclooxygenase (COX). Twelve novel compounds (aryl acetate and aryl acetic acid groups) were synthesized in this work in order to identify which one was the most potent and which group was most selective towards COX1 and COX2 by using an in vitro COX inhibition assay kit. The cytotoxicity was evaluated for these compounds utilizing MTS assay against cervical carcinoma cells line (HeLa). The synthesized compounds were identified using FTIR, HRMS,H-1-NMR, and(13)C-NMR techniques. The results showed that the most potent compound against the COX1 enzyme was 4f with IC50 = 0.725 mu M. The compound 3b showed potent activity against both COX1 and COX2 with IC50 = 1.12 and 1.3 mu M, respectively, and its selectivity ratio (0.862) was found to be better than Ketoprofen (0.196). In contrast, compound 4d was the most selective with a COX1/COX2 ratio value of 1.809 in comparison with the Ketoprofen ratio. All compounds showed cytotoxic activity against the HeLa Cervical cancer cell line at a higher concentration ranges (0.219-1.94 mM), and the most cytotoxic compound was 3e with a CC(50)value of 219 mu M. This was tenfold more than its IC(50)values of 2.36 and 2.73 mu M against COX1 and COX2, respectively. In general, the synthesized library has moderate activity against both enzymes (i.e., COX1 and COX2) and ortho halogenated compounds were more potent than the meta ones.

Recommanded Product: 2,4-Dichlorobenzoic acid. About 2,4-Dichlorobenzoic acid, If you have any questions, you can contact Hawash, M; Jaradat, N; Hameedi, S; Mousa, A or concate me.

Reference:
Chloride – Wikipedia,
,Chlorides – an overview | ScienceDirect Topics

Authors Neshat, A; Osanlou, F; Kakavand, M; Mastrorilli, P; Schingaro, E; Mesto, E; Todisco, S in PERGAMON-ELSEVIER SCIENCE LTD published article about in [Neshat, Abdollah; Osanlou, Farzane; Kakavand, Meysam] Inst Adv Studies Basic Sci IASBS, Dept Chem, Zanjan 4513766731, Iran; [Mastrorilli, Piero; Todisco, Stefano] Politecn Bari, DICATECh Dept, Via Orabona 4, I-70125 Bari, Italy; [Schingaro, Emanuela; Mesto, Ernesto] Univ Aldo Moro Bari, Dipartimento Sci Terra & Geoambientali, Via Orabona 4, I-70125 Bari, Italy in 2021, Cited 49. COA of Formula: C7H4Cl2O2. The Name is 2,4-Dichlorobenzoic acid. Through research, I have a further understanding and discovery of 50-84-0

Four Schiff base manganese(III) complexes with derivatives of [(R,R)-N,N’-bis(salicy1idene)-1,2-cyclohexanediaminato)] including substituents on salicylaldehyde such as 3-methoxy, 3,5-di-tert-butyl and 3,5-chloro were synthesized and characterized using a combination of IR, UV-Vis, and HR ESI-MS techniques. The catalytic activity of these complexes was tested in the oxidation of 1-phenylethanol to acetophenone, revealing very good performances for all of the four manganese complexes. The catalytic reactions were carried out in the presence of tert-butyl hydroperoxide (TBHP) as oxidant and imidazole as co-catalyst. Complex Mn-4, bearing electron withdrawing [(R,R)-N,N’-bis(3,5-di-chloro-salicylidene)-1,2-cyclohexanediaminato)] ligand was found to be the most stable of the tested Mn(III) complexes and was selected for the oxidation of several primary and secondary alcohols. (C) 2020 Elsevier Ltd. All rights reserved.

COA of Formula: C7H4Cl2O2. About 2,4-Dichlorobenzoic acid, If you have any questions, you can contact Neshat, A; Osanlou, F; Kakavand, M; Mastrorilli, P; Schingaro, E; Mesto, E; Todisco, S or concate me.

Reference:
Chloride – Wikipedia,
,Chlorides – an overview | ScienceDirect Topics

An article Novel paeonol derivatives: Design, synthesis and anti-inflammatory activity in vitro and in vivo WOS:000526784800038 published article about NF-KAPPA-B; EXPRESSION; CELLS; INFLAMMATION; INHIBITOR; DISCOVERY; CYTOKINES; THERAPY; ANALOGS in [Hu, Yang Sheng; Han, Xu; Yu, Pei Jing; Jiao, Ming Ming; Liu, Xin Hua; Shi, Jing Bo] Anhui Med Univ, Sch Pharm, Hefei 230032, Peoples R China in 2020, Cited 32. Formula: C7H4Cl2O2. The Name is 2,4-Dichlorobenzoic acid. Through research, I have a further understanding and discovery of 50-84-0

Paeonol has been proved to have potential anti-inflammatory activity, but its clinical application is not extensive due to the poor anti-inflammatory activity (14.74% inhibitory activity at 20 mu M). In order to discover novel lead compound with high anti-inflammatory activity, series of paeonol derivatives were designed and synthesized, their anti-inflammatory activities were screened in vitro and in vivo. Structure-activity relationships (SARs) have been fully concluded, and finally (E)-N-(4-(2-acetyl-5-methoxyphenoxy)phenyl)-3-(3,4,5-trimet-hoxyphenyl) acrylamide (compound 1 la) was found to be the best active compound with low toxicity, which showed 96.32% inhibitory activity at 20 mu M and IC50 value of 6.96 mu M against LPS-induced over expression of nitric oxide (NO) in RAW 264.7 macrophages. Preliminary mechanism studies indicated that it could inhibit the expression of TLR4, resulting in inhibiting of NF-kappa B and MAPK pathways. Further studies have shown that compound 11a has obvious therapeutic effect against the adjuvant-induced rat arthritis model.

Formula: C7H4Cl2O2. About 2,4-Dichlorobenzoic acid, If you have any questions, you can contact Hu, YS; Han, X; Yu, PJ; Jiao, MM; Liu, XH; Shi, JB or concate me.

Reference:
Chloride – Wikipedia,
,Chlorides – an overview | ScienceDirect Topics

In 2021 SYNTHESIS-STUTTGART published article about METHYL KETONES; INTRAMOLECULAR CYCLIZATION; ELECTROPHILIC CYCLIZATION; MICHAEL ADDITION; ACCESS; STRATEGY; ANILINES; HYDROCHLORIDE; DERIVATIVES; INDOLES in [Zhou, Xiao-Yu; Chen, Xia] Liupanshui Normal Univ, Sch Chem & Mat Engn, Liupanshui 553004, Peoples R China in 2021, Cited 63. The Name is 2,4-Dichlorobenzoic acid. Through research, I have a further understanding and discovery of 50-84-0. Category: chlorides-buliding-blocks

Iodine-catalyzed oxidative C(sp(3))-H acyloxylation of acetone with carboxylic acids has been developed. The method employs iodide-as catalyst and sodium chlorite as oxidant. Substituted benzoic acids, naphthoic acids and heteroaromatic carboxylic acids can be used, and 2-oxopropyl carboxylates are obtained with good to excellent yields.

About 2,4-Dichlorobenzoic acid, If you have any questions, you can contact Zhou, XY; Chen, X or concate me.. Category: chlorides-buliding-blocks

Reference:
Chloride – Wikipedia,
,Chlorides – an overview | ScienceDirect Topics

An article New N-benzhydrylpiperazine/1,3,4-oxadiazoles conjugates inhibit the proliferation, migration, and induce apoptosis in HeLa cancer cells via oxidative stress-mediated mitochondrial pathway WOS:000458822400057 published article about IN-VITRO; BIOLOGICAL EVALUATION; ANTICANCER ACTIVITY; CERVICAL-CANCER; G2/M PHASE; DERIVATIVES; DISCOVERY; SYNTHASE; DOCKING; ARREST in [Khanam, Rashmin; Hejazi, Iram Iqbal; Athar, Fareeda] Jamia Millia Islamia, Ctr Interdisciplinary Res Basic Sci, New Delhi 110025, India; [Kumar, Raj; Meena, Ramovatar; Rajamani, Paulraj] Jawaharlal Nehru Univ, Sch Environm Sci, New Delhi, India; [Shahabuddin, Syed] Sunway Univ, RCNMET, Sch Sci & Technol, Selangor, Malaysia; [Yadav, Nitin] Indian Inst Technol, Dept Chem, New Delhi, India; [Bhat, Asif Iqbal] Cluster Univ, Dept Chem, Sri Pratap Coll, Srinagar, Jammu & Kashmir, India in 2019, Cited 43. Safety of 2,4-Dichlorobenzoic acid. The Name is 2,4-Dichlorobenzoic acid. Through research, I have a further understanding and discovery of 50-84-0

N-benzhydrylpiperazine and 1,3,4-oxadiazoles are pharmacologically active scaffolds which exhibits significant inhibitory growth effects against various cancer cells, however, antiproliferation effects and the underlying mechanism for inducing apoptosis for aforementioned scaffolds addressing HeLa cancer cells remains uncertain. In this study, N-benzhydrylpiperazine clubbed with 1,3,4-oxadiazoles (4a-4h) were synthesized, subsequently characterized using high resolution spectroscopic techniques and eventually evaluated for their antiproliferation potential by inducing apoptosis in HeLa cancer cells. The MTT assay screening results revealed that among all, compound 4d (N-benzhydryl-4-((5-(4-aminophenyl)-1,3,4-oxadiazol-2-yl)methyl)piperazine) in particular, exhibited IC (50) value of 28.13 +/- 0.21g/mL and significantly inhibited the proliferation of HeLa cancer cells in concentration-dependent manner. The in vitro anticancer assays for treated HeLa cells resulted in alterations in the cell morphology, reduction in colony formation, and inhibition of cell migration in concentration-dependent treatment. Furthermore, G2/M phase arrest, variations in the nuclear morphology, degradation of chromosomal DNA confirmed the ongoing apoptosis in treated HeLa cells. Increase in the expression of cytochrome C and caspase-3 confirmed the involvement of intrinsic mitochondrial pathway regulating the cell death. Also, elevation in reactive oxygen species level and loss of mitochondrial membrane potential signified that compound 4d induced apoptosis in HeLa cells by generating the oxidative stress. Therefore, compound 4d may act as a potent chemotherapeutic agent against human cervical cancer.

About 2,4-Dichlorobenzoic acid, If you have any questions, you can contact Khanam, R; Kumar, R; Hejazi, II; Shahabuddin, S; Meena, R; Rajamani, P; Yadav, N; Bhat, AI; Athar, F or concate me.. Safety of 2,4-Dichlorobenzoic acid

Reference:
Chloride – Wikipedia,
,Chlorides – an overview | ScienceDirect Topics

I found the field of Pharmacology & Pharmacy very interesting. Saw the article Discovery and Synthesis of a Pyrimidine-Based Aurora Kinase Inhibitor to Reduce Levels of MYC Oncoproteins published in 2021. Product Details of 50-84-0, Reprint Addresses Chi, YH; Chang, CP (corresponding author), Natl Hlth Res Inst, Inst Biotechnol & Pharmaceut Res, Zhunan 35053, Taiwan.; Chi, YH (corresponding author), China Med Univ, Grad Inst Biomed Sci, Taichung 40402, Taiwan.; Chang, CP (corresponding author), Chung Yuan Christian Univ, Dept Chem, Taoyuan 320314, Taiwan.. The CAS is 50-84-0. Through research, I have a further understanding and discovery of 2,4-Dichlorobenzoic acid

The A-type Aurora kinase is upregulated in many human cancers, and it stabilizes MYC-family oncoproteins, which have long been considered an undruggable target. Here, we describe the design and synthesis of a series of pyrimidine-based derivatives able to inhibit Aurora A kinase activity and reduce levels of cMYC and MYCN. Through structure-based drug design of a small molecule that induces the DFG-out conformation of Aurora A kinase, lead compound 13 was identified, which potently (IC50 < 200 nM) inhibited the proliferation of high-MYC expressing small-cell lung cancer (SCLC) cell lines. Pharmacokinetic optimization of 13 by prodrug strategies resulted in orally bioavailable 25, which demonstrated an 8-fold higher oral AUC (F = 62.3%). Pharmacodynamic studies of 25 showed it to effectively reduce cMYC protein levels, leading to >80% tumor regression of NCI-H446 SCLC xenograft tumors in mice. These results support the potential of 25 for the treatment of MYC-amplified cancers including SCLC.

About 2,4-Dichlorobenzoic acid, If you have any questions, you can contact Chi, YH; Yeh, TK; Ke, YY; Lin, WH; Tsai, CH; Wang, WP; Chen, YT; Su, YC; Wang, PC; Chen, YF; Wu, ZW; Yeh, JY; Hung, MC; Wu, MH; Wang, JY; Chen, CP; Song, JS; Shih, C; Chen, CT; Chang, CP or concate me.. Product Details of 50-84-0

Reference:
Chloride – Wikipedia,
,Chlorides – an overview | ScienceDirect Topics

An article Practical and rapid construction of 2-pyridyl ketone library in continuous flow WOS:000588040300001 published article about ASYMMETRIC HYDROGENATION; NITRIC-ACID; CHEMISTRY; SYSTEM; GENERATION; CONVERSION; NITRATION; ARYL in [Sun, Maolin; Li, Jianchang; Liang, Chaoming; Shan, Chao; Shen, Xinyuan; Ma, Yueyue; Ye, Jinxing] East China Univ Sci & Technol, Minist Educ, Sch Pharm, Engn Res Ctr Pharmaceut Proc Chem, Shanghai 200237, Peoples R China; [Cheng, Ruihua] East China Univ Sci & Technol, Sch Chem Engn, Shanghai 200237, Peoples R China in 2021, Cited 59. Computed Properties of C7H4Cl2O2. The Name is 2,4-Dichlorobenzoic acid. Through research, I have a further understanding and discovery of 50-84-0

2-Pyridyl ketones widely appear in bioactive molecules, natural products, and are employed as precursors of chiral 2-pyridine alky/aryl alcohols or 2-aminoalkyl pyridine ligands for asymmetric catalysis. Herein, a practical method for the rapid synthesis of 2-pyridyl ketone library in continuous flow is reported, in which the 2-lithiopyridine formed by Br/Li exchange reacts with commercially available esters to obtain 2-pyridyl ketones in a good yield at short reaction time. This protocol functions broadly on a variety of esters and has been applied to the synthesis of TGF-beta type 1 receptor inhibitor LY580276 intermediate in an environmentally friendly method. It is rapid, reliable, and cost-efficient to afford diverse kinds of 2-pyridyl ketones in the compound library.

Computed Properties of C7H4Cl2O2. About 2,4-Dichlorobenzoic acid, If you have any questions, you can contact Sun, ML; Li, JC; Liang, CM; Shan, C; Shen, XY; Cheng, RH; Ma, YY; Ye, JX or concate me.

Reference:
Chloride – Wikipedia,
,Chlorides – an overview | ScienceDirect Topics