What kind of challenge would you like to see in a future of compound:2,5-Dimethoxybenzaldehyde

About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Gao, CZ; Dong, W; Cui, ZW; Yuan, Q; Hu, XM; Wu, QM; Han, XL; Xu, Y; Min, ZL or concate me.. Product Details of 93-02-7

Product Details of 93-02-7. Recently I am researching about ALZHEIMERS-DISEASE; BUTYRYLCHOLINESTERASE INHIBITORS; POLY(ADP-RIBOSE) POLYMERASE-1; POTENT; ACETYLCHOLINESTERASE; DERIVATIVES; DISCOVERY; THERAPY; CANCER; CHALCONE, Saw an article supported by the . Published in TAYLOR & FRANCIS LTD in ABINGDON ,Authors: Gao, CZ; Dong, W; Cui, ZW; Yuan, Q; Hu, XM; Wu, QM; Han, XL; Xu, Y; Min, ZL. The CAS is 93-02-7. Through research, I have a further understanding and discovery of 2,5-Dimethoxybenzaldehyde

A series of new Olaparib derivatives was designed and synthesized, and their inhibitory activities against poly (ADP-ribose) polymerases-1 (PARP-1) enzyme and cancer cell line MDA-MB-436 in vitro were evaluated. The results showed that compound 5l exhibited the most potent inhibitory effects on PARP-1 enzyme (16.10 +/- 1.25 nM) and MDA-MB-436 cancer cell (11.62 +/- 2.15 mu M), which was close to that of Olaparib. As a PARP-1 inhibitor had been reported to be viable to neuroprotection, in order to search for new multitarget-directed ligands (MTDLs) for the treatment of Alzheimer’s disease (AD), the inhibitory activities of the synthesized compounds against the enzymes AChE (from electric eel) and BChE (from equine serum) were also tested. Compound 5l displayed moderate BChE inhibitory activity (9.16 +/- 0.91 mu M) which was stronger than neostigmine (12.01 +/- 0.45 mu M) and exhibited selectivity for BChE over AChE to some degree. Molecular docking studies indicated that 5l could bind simultaneously to the catalytic active of PARP-1, but it could not interact well with huBChE. For pursuit of PARP-1 and BChE dual-targeted inhibitors against AD, small and flexible non-polar groups introduced to the compound seemed to be conducive to improving its inhibitory potency on huBChE, while keeping phthalazine-1-one moiety unchanged which was mainly responsible for PARP-1 inhibitory activity. Our research gave a clue to search for new agents based on AChE and PARP-1 dual-inhibited activities to treat Alzheimer’s disease.

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Computed Properties of C9H10O3. About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Halder, S or concate me.

Computed Properties of C9H10O3. Recently I am researching about ONE-POT SYNTHESIS; SOLID-PHASE SYNTHESIS; 2-SUBSTITUTED BENZIMIDAZOLES; EFFICIENT METHOD; SOLVENT; WATER; BENZOXAZOLES; DERIVATIVES; ACID; 2-ARYLBENZIMIDAZOLES, Saw an article supported by the . Published in ORIENTAL SCIENTIFIC PUBL CO in BHOPAL ,Authors: Halder, S. The CAS is 93-02-7. Through research, I have a further understanding and discovery of 2,5-Dimethoxybenzaldehyde

Various substituted benzimidazoles have been successfully synthesized in aqueous medium by developing VO(acac)(2)-Cu(OTf)(2) catalytic system. A green synthetic protocol has been created in presence of water and cetyltrimethyl ammonium bromide (CTAB) system in an organic solvent free condition. This chemoselective cyclocondensation cumoxidation process occurred in aqueous media. In this suitable method easily synthesized 2-Substituted benzimidazoles with good yields and no 1,2-disubstituted by-products were noticed. Excellent yields, environmentally benign and mild reaction condition, easy purification of the desired products are the main attractive features of this newly devised method. [GRAPHICS]

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Reference:
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Chemistry Milestones Of 2,5-Dimethoxybenzaldehyde

About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Kumar, M; Joshi, G; Arora, S; Singh, T; Biswas, S; Sharma, N; Bhat, ZR; Tikoo, K; Singh, S; Kumar, R or concate me.. Safety of 2,5-Dimethoxybenzaldehyde

Safety of 2,5-Dimethoxybenzaldehyde. Authors Kumar, M; Joshi, G; Arora, S; Singh, T; Biswas, S; Sharma, N; Bhat, ZR; Tikoo, K; Singh, S; Kumar, R in MDPI published article about in [Kumar, Manvendra; Joshi, Gaurav; Arora, Sahil; Biswas, Sajal; Kumar, Raj] Cent Univ Punjab, Sch Hlth Sci, Dept Pharmaceut Sci & Nat Prod, Lab Drug Design & Synth, Bathinda 151401, Punjab, India; [Joshi, Gaurav] Graph Era Hill Univ, Sch Pharm, Dehra Dun 248171, Uttarakhand, India; [Singh, Tashvinder; Singh, Sandeep] Cent Univ Punjab, Dept Human Genet & Mol Med, Bathinda 151401, Punjab, India; [Sharma, Nisha; Bhat, Zahid Rafiq; Tikoo, Kulbhushan] Natl Inst Pharmaceut Educ & Res, Dept Pharmacol & Toxicol, Sas Nagar 160062, Punjab, India in 2021.0, Cited 33.0. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7

A series of 30 non-covalent imidazo[1,2-a]quinoxaline-based inhibitors of epidermal growth factor receptor (EGFR) were designed and synthesized. EGFR inhibitory assessment (against wild type) data of compounds revealed 6b, 7h, 7j, 9a and 9c as potent EGFR(WT) inhibitors with IC50 values of 211.22, 222.21, 193.18, 223.32 and 221.53 nM, respectively, which were comparable to erlotinib (221.03 nM), a positive control. Furthermore, compounds exhibited excellent antiproliferative activity when tested against cancer cell lines harboring EGFR(WT); A549, a non-small cell lung cancer (NSCLC), HCT-116 (colon), MDA-MB-231 (breast) and gefitinib-resistant NSCLC cell line H1975 harboring EGFR(L858R/T790M). In particular, compound 6b demonstrated significant inhibitory potential against gefitinib-resistant H1975 cells (IC50 = 3.65 mu M) as compared to gefitinib (IC50 > 20 mu M). Moreover, molecular docking disclosed the binding mode of the 6b to the domain of EGFR (wild type and mutant type), indicating the basis of inhibition. Furthermore, its effects on redox modulation, mitochondrial membrane potential, cell cycle analysis and cell death mode in A549 lung cancer cells were also reported.

About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Kumar, M; Joshi, G; Arora, S; Singh, T; Biswas, S; Sharma, N; Bhat, ZR; Tikoo, K; Singh, S; Kumar, R or concate me.. Safety of 2,5-Dimethoxybenzaldehyde

Reference:
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Brief introduction of C9H10O3

HPLC of Formula: C9H10O3. About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Mohammadi-Khanaposhtani, M; Yahyavi, H; Barzegaric, E; Imanparast, S; Heravi, MM; Faramarzi, MA; Foroumadi, A; Adibi, H; Larijani, B; Mandavi, M or concate me.

Mohammadi-Khanaposhtani, M; Yahyavi, H; Barzegaric, E; Imanparast, S; Heravi, MM; Faramarzi, MA; Foroumadi, A; Adibi, H; Larijani, B; Mandavi, M in [Mohammadi-Khanaposhtani, Maryam] Babol Univ Med Sci, Cellular & Mol Biol Res Ctr, Hlth Res Inst, Babol, Iran; [Yahyavi, Hoda; Heravi, Majid M.] Alzahra Univ, Fac Chem & Phys, Dept Chem, Tehran, Iran; [Barzegaric, Ebrahim] Kermanshah Univ Med Sci, Med Biol Res Ctr, Kermanshah, Iran; [Imanparast, Somaye; Faramarzi, Mohammad Ali] Univ Tehran Med Sci, Dept Pharmaceut Biotechnol, Fac Pharm, Tehran, Iran; [Imanparast, Somaye; Faramarzi, Mohammad Ali] Univ Tehran Med Sci, Biotechnol Res Ctr, Tehran, Iran; [Foroumadi, Alireza] Univ Tehran Med Sci, Fac Pharm, Dept Med Chem, Tehran, Iran; [Foroumadi, Alireza] Univ Tehran Med Sci, Pharmaceut Sci Res Ctr, Tehran, Iran; [Adibi, Hossein; Larijani, Bagher; Mandavi, Mohammad] Univ Tehran Med Sci, Endocrinol & Metab Res Ctr, Endocrinol & Metab Clin Sci Inst, Tehran, Iran published New Biscoumarin Derivatives as Potent alpha-Glucosidase Inhibitors: Synthesis, Biological Evaluation, Kinetic Analysis, and Docking Study in 2020.0, Cited 26.0. HPLC of Formula: C9H10O3. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7.

A new series of biscoumarin derivatives3a-nwere synthesized and evaluated for their alpha-glucosidase inhibitory activities. The reaction of the 4-aminocoumarin with benzaldehyde derivatives led to the formation of the title compounds in good yields. All the synthesized compounds showed potent alpha-glucosidase inhibitory activity with IC(50)ranging from 20.0 +/- 0.7 to180.1 +/- 0.8 mu M, in comparison with acarbose as the standard drug (IC50= 750.0 1.5 mu M). Among the synthesized compounds, 3,3′-(p-tolylmethylene)bis(4-amino-2H-chromen-2-one)3cwas found to be the most active compound with an IC(50)value of 20.0 +/- 0.7 mu M. Kinetic study exhibited that compound3cwas a competitive inhibitor against alpha-glucosidase (K-i= 22.4 mu M). In silico docking study for the most potent compound3cwas also performed.

HPLC of Formula: C9H10O3. About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Mohammadi-Khanaposhtani, M; Yahyavi, H; Barzegaric, E; Imanparast, S; Heravi, MM; Faramarzi, MA; Foroumadi, A; Adibi, H; Larijani, B; Mandavi, M or concate me.

Reference:
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COA of Formula: C9H10O3. About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Gein, VL; Buldakova, EA; Dmitriev, MV or concate me.

COA of Formula: C9H10O3. Authors Gein, VL; Buldakova, EA; Dmitriev, MV in MAIK NAUKA/INTERPERIODICA/SPRINGER published article about in [Gein, V. L.; Buldakova, E. A.] Perm State Pharmaceut Acad, Perm, Russia; [Dmitriev, M., V] Perm State Natl Res Univ, Perm, Russia in 2019.0, Cited 11.0. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7

Three-component reaction of methyl 4-aryl-2,4-dioxobutanoates with aromatic aldehyde and 2-aminoacetonitrile sulfate in glacial acetic acid in the presence of anhydrous sodium acetate afforded previously unknown (3-aroyl-2-aryl-4-hydroxy-5-oxo-2,5-dihydro-1H-pyrrol-1-yl)acetonitriles. The reaction involved intermediate formation of Schiff base, followed by Michael-type addition of the dioxo ester to the C=N bond and cyclization of the addition product, methyl 3-aroyl-4-aryl-4-(cyanomethylamino)-2-oxobutanoate. The cyclization product reacted with hydrazine hydrate at the aroyl carbonyl group to give the corresponding hydrazone which was converted in 1,4-dioxane to the cyclic form, [3,4-diaryl-6a-hydroxy-6-oxo-3a,4,6,6a-tetrahydropyrrolo[3,4-c]pyrazol-5(1H)-yl]acetonitrile, without elimination of the second water molecule. When the reaction of (3-aroyl-2-aryl-4-hydroxy-5-oxo-2,5-dihydro-1H-pyrrol-1-yl)acetomtriles with hydrazine hydrate was carried out in boiling acetic acid, [3,4-diaryl-6-oxo-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]acetonitriles were obtained as a result of dehydration of initially formed [3,4-diaryl-6a-hydroxy-6-oxo-3a,4,6,6a-tetrahydropyrrolo[3,4-c]pyrazol-5(1H)-yl]acetonitriles as shown by special experiment. The structures of [6a-hydroxy-6-oxo-3,4-diphenyl-3a,4,6,6a-tetrahydropyrrolo[3,4-c]pyrazol-5(1H)-yl]acetonitrile and [4-(4-methoxyphenyl)-6-oxo-3-phenyl-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]acetonitrile were determined by X-ray analysis.

COA of Formula: C9H10O3. About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Gein, VL; Buldakova, EA; Dmitriev, MV or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Never Underestimate The Influence Of 2,5-Dimethoxybenzaldehyde

Product Details of 93-02-7. About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Gouhar, RS; Haneen, DSA; El-Hallouty, SM or concate me.

I found the field of Chemistry very interesting. Saw the article Synthesis and Anticancer Evaluation of Some Novel Quinazolin-4(3H)-one Derivatives published in 2019.0. Product Details of 93-02-7, Reprint Addresses Gouhar, RS (corresponding author), Natl Res Ctr, Therapeut Chem Dept, PO 12622, Giza, Egypt.. The CAS is 93-02-7. Through research, I have a further understanding and discovery of 2,5-Dimethoxybenzaldehyde

A new series of quinazolinone derivatives bearing pyridine, pyrimidine, pyrazole, or pyran moieties were synthesized for the purpose of anticancer cell line evaluation. Synthesis of these derivatives was achieved by the reaction of the ketone 2 with the appropriate aldehydes in the presence of either ethylcyanoacetate or malononitrile and ammonium acetate in one-pot reaction. Chalcones 6 reacted also with hydrazine hydrate to give the corresponding pyrazolines 7 and reacted with urea or thiourea to give the 2-oxopyrimidines or the 2-thioxopyrimidines 8, respectively. Evaluation of some representative examples of the newly synthesized compounds against cancer cell lines showed promising activity as anticancer agents.

Product Details of 93-02-7. About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Gouhar, RS; Haneen, DSA; El-Hallouty, SM or concate me.

Reference:
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Why do aromatic interactions matter of compound:C9H10O3

Safety of 2,5-Dimethoxybenzaldehyde. About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Hue, BTB; Nguyen, PH; De, TQ; Hieu, MV; Jo, E; Tuan, NV; Thoa, TT; Anh, L; Son, NH; Thanh, DLD; Dupont-Rouzeyrol, M; Grailhe, R; Windisch, MP or concate me.

In 2020 CHEMMEDCHEM published article about CATALYZED SYNTHESIS; SIRTUIN INHIBITORS; IN-VITRO; ELECTROLUMINESCENCE; TRANSMISSION; ENTRY in [Hue, Bui Thi Buu; De, Tran Quang; Van Hieu, Mai; Van Tuan, Nguyen; Anh, Le Duc; Son, Nguyen Hoang; Duc Thanh, Danh La] Can Tho Univ, Coll Nat Sci, Dept Chem, Campus 2,3-2 St, Can Tho City, Vietnam; [Nguyen, Phuong Hong; Jo, Eunji; Thoa, Than Thi; Windisch, Marc P.] Inst Pasteur Korea, Appl Mol Virol Lab, Discovery Biol Div, Seongnam 13488, South Korea; [Nguyen, Phuong Hong; Windisch, Marc P.] Univ Sci & Technol, Div Biomed Sci & Technol, Daejeon 34141, South Korea; [Dupont-Rouzeyrol, Myrielle] Inst Pasteur Nouvelle Caledonie, URE Dengue & Arboviruses, Noumea 98800, New Caledonia; [Grailhe, Regis] Inst Pasteur Korea, Technol Dev Platform, Seongnam 13488, South Korea in 2020, Cited 42. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7. Safety of 2,5-Dimethoxybenzaldehyde

We have synthesized 50 benzimidazole (BMZ) derivatives with 1,2-phenylenediamines and aromatic aldehydes under mild oxidation conditions by using inexpensive, nontoxic inorganic salt sodium metabisulfite in a one-pot condensation reaction and screened their ability to interfere with Zika virus (ZIKV) infection utilizing a cell-based phenotypic assay. Seven BMZs inhibited an African ZIKV strain with a selectivity index (SI=CC50/EC50) of 9-37. Structure-activity relationship analysis demonstrated that substitution at the C-2, N-1, and C-5 positions of the BMZ ring were important for anti-ZIKV activity. The hybrid structure of BMZ and naphthalene rings was a structural feature responsible for the high anti-ZIKV activity. Importantly, BMZs inhibited ZIKV in human neural stem cells, a physiologically relevant system considering the severe congenital anomalies, like microcephaly, caused by ZIKV infection. Compound 39 displayed the highest antiviral efficacy against the African ZIKV strain in Huh-7 (SI>37) and neural stem cells (SI=12). Compound 35 possessed the highest activity in Vero cells (SI=115). Together, our data indicate that BMZs derivatives have to be considered for the development of ZIKV therapeutic interventions.

Safety of 2,5-Dimethoxybenzaldehyde. About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Hue, BTB; Nguyen, PH; De, TQ; Hieu, MV; Jo, E; Tuan, NV; Thoa, TT; Anh, L; Son, NH; Thanh, DLD; Dupont-Rouzeyrol, M; Grailhe, R; Windisch, MP or concate me.

Reference:
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Final Thoughts on Chemistry for 2,5-Dimethoxybenzaldehyde

About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Temperini, A; Ballarotto, M; Siciliano, C or concate me.. COA of Formula: C9H10O3

Temperini, A; Ballarotto, M; Siciliano, C in [Temperini, Andrea; Ballarotto, Marco] Univ Perugia, Dipartimento Sci Farmaceut, Consorzio CINMPIS, Via Liceo 1, I-06123 Perugia, Italy; [Siciliano, Carlo] Univ Calabria, Dipartimento Farm & Sci Salute & Nutr, Edificio Polifunz, I-87030 Cosenza, Italy published Chemoselective and metal-free reduction of alpha,beta-unsaturated ketones byin situproduced benzeneselenol fromO-(tert-butyl) Se-phenyl selenocarbonate in 2020.0, Cited 59.0. COA of Formula: C9H10O3. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7.

The carbon-carbon double bond of arylidene acetones and chalcones can be selectively reduced with benzeneselenol generatedin situby reactingO-(tert-butyl) Se-phenyl selenocarbonate with hydrochloric acid in ethanol. This mild, metal-free and experimentally simple reduction procedure displays considerable functional-group compatibility, products are obtained in good to excellent yields, and the use of toxic Se/CO mixture and NaSeH, or the smelly and air-sensitive benzeneselenol, is avoided.

About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Temperini, A; Ballarotto, M; Siciliano, C or concate me.. COA of Formula: C9H10O3

Reference:
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,Isothiazole – ScienceDirect.com

Extended knowledge of C9H10O3

About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Znidar, D; O’Kearney-McMullan, A; Munday, R; Wiles, C; Poechlauer, P; Schmoelzer, C; Dallinger, D; Kappe, CO or concate me.. COA of Formula: C9H10O3

Znidar, D; O’Kearney-McMullan, A; Munday, R; Wiles, C; Poechlauer, P; Schmoelzer, C; Dallinger, D; Kappe, CO in [Znidar, Desiree; Dallinger, Doris; Kappe, C. Oliver] Res Ctr Pharmaceut Engn GmbH RCPE, Ctr Continuous Flow Synth & Proc CCFLOW, Inffeldgasse 13, A-8010 Graz, Austria; [Znidar, Desiree; Dallinger, Doris; Kappe, C. Oliver] Karl Franzens Univ Graz, NAWI Graz, Inst Chem, Heinrichstr 28, A-8010 Graz, Austria; [O’Kearney-McMullan, Anne; Munday, Rachel] AstraZeneca, Silk Rd Business Pk, Macclesfield SK10 2NA, Cheshire, England; [Wiles, Charlotte] Chemtrix BV, Galvaniweg 8A, NL-6101 XH Echt, Netherlands; [Poechlauer, Peter; Schmoelzer, Christoph] Patheon Austria GmbH & Co KG, Sankt Peter Str 25, A-4020 Linz, Austria published Scalable Wolff-Kishner Reductions in Extreme Process Windows Using a Silicon Carbide Flow Reactor in 2019.0, Cited 45.0. COA of Formula: C9H10O3. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7.

A safe and scalable continuous flow strategy for Wolff-Kishner reductions that employs methanol as the solvent has been developed. The use of low-cost hydrazine as the reducing agent in combination with a caustic base provides an atom-efficient, environmentally friendly method for the deoxygenation of aldehydes and ketones to alkanes. Because of the required harsh and corrosive reaction conditions (200 degrees C, 50 bar), reactor materials such as stainless steel, glass, or any type of polymer have compatibility problems, rendering this process problematic on a production scale. The use of corrosion-resistant silicon carbide (SiC) as the reactor material opens up the possibility of performing Wolff-Kishner reductions on scale with a considerably improved safety profile. Methanol as the solvent significantly simplifies the workup procedure compared with the generally employed high-boiling solvents such as diethylene glycol. The continuous flow protocol was applied to a number of substrates and provided the desired products in good to high yields with space-time yields of up to 152 g L(-1)h(-1). In addition, a pharmaceutically valuable active pharmaceutical ingredient precursor was synthesized by employing this high-temperature/pressure Wolff-Kishner protocol.

About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Znidar, D; O’Kearney-McMullan, A; Munday, R; Wiles, C; Poechlauer, P; Schmoelzer, C; Dallinger, D; Kappe, CO or concate me.. COA of Formula: C9H10O3

Reference:
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What advice would you give a new faculty member or graduate student interested in a career 93-02-7

Category: isothiazole. About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Abdel-Mohsen, HT; Abd El-Meguid, EA; El Kerdawy, AM; Mahmoud, AEE; Ali, MM or concate me.

Recently I am researching about PROTEIN-KINASE INHIBITORS; DRUG-RESISTANCE; RECEPTOR 2; GROWTH; BENZOTHIAZOLES; ANGIOGENESIS; DISCOVERY; VEGFR-2; POTENT; MECHANISMS, Saw an article supported by the . Published in WILEY-V C H VERLAG GMBH in WEINHEIM ,Authors: Abdel-Mohsen, HT; Abd El-Meguid, EA; El Kerdawy, AM; Mahmoud, AEE; Ali, MM. The CAS is 93-02-7. Through research, I have a further understanding and discovery of 2,5-Dimethoxybenzaldehyde. Category: isothiazole

A novel series of 2-arylbenzothiazoles 9, 10, and 12 were designed and synthesized as VEGFR-2/FGFR-1/PDGFR-beta multiangiokinase inhibitors targeting breast cancer. Structural elongation of the known 2-phenylbenzothiazole scaffold (type I protein kinase inhibitor [PKI]), was carried out to afford series of type II PKIs 9, 10, and 12. Compounds 9d, 9f, 9i, and 9k exhibited potent multikinase inhibitory activity with IC50 values of 0.19, 0.18, 0.17, and 0.13 mu M, respectively, against VEGFR-2; IC50 values of 0.28, 0.37, 0.19, and 0.27 mu M, respectively, against FGFR-1; and IC50 values of 0.07, 0.04, 0.08, and 0.14 mu M, respectively, against PDGFR-beta. Moreover, the synthesized benzothiazoles demonstrated promising cytotoxic activity against the MCF-7 cell line. The most potent benzothiazoles 9d and 9i exhibited IC50 values of 7.83 and 6.58 mu M, respectively, on the MCF-7 cell line in comparison to sorafenib (III), which showed IC50 = 4.33 mu M. Additionally, 9d and 9i showed VEGFR-2 inhibitory activity in MCF-7 cells of 81% and 83% when compared with sorafenib (III), which showed 88% inhibition. Molecular docking of the designed compounds in the VEGFR-2 and FGFR-1 active sites showed the accommodation of the 2-phenylbenzothiazole moiety, as reported, in the hinge region of the receptor tyrosine kinase (RTK)-binding site, while the amide moiety is involved in hydrogen bond interactions with the key amino acids in the gate area; this in turn directs the aryl group to the hydrophobic allosteric back pocket of the RTKs in a type II-like binding mode. The synthesized benzothiazoles showed satisfactory ADME properties for further optimization in drug discovery.

Category: isothiazole. About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Abdel-Mohsen, HT; Abd El-Meguid, EA; El Kerdawy, AM; Mahmoud, AEE; Ali, MM or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com