The Absolute Best Science Experiment for C7H5NO3

Product Details of 99-61-6. Welcome to talk about 99-61-6, If you have any questions, you can contact Fekri, LZ; Zadeh, LH or send Email.

An article Synthesis, Characterization, and Evaluation of Antibacterial Activity of New Bis-Dapsone-Derived Dihydropyridines Using Fe3O4@SiO2-Pr@L-proline WOS:000644646500026 published article about MAGNETICALLY SEPARABLE CATALYST; COATED NIFE2O4 NANOPARTICLES; POT MULTICOMPONENT REACTIONS; POTENTIAL ANTITUMOR AGENTS; SOLVENT-FREE SYNTHESIS; EFFICIENT SYNTHESIS; HANTZSCH REACTION; HETEROGENEOUS CATALYST; REUSABLE CATALYST; DERIVATIVES in [Fekri, Leila Zare; Zadeh, Leila Hassan] Payame Noor Univ, Dept Chem, POB 19395-3697, Tehran, Iran in 2021, Cited 38. The Name is 3-Nitrobenzaldehyde. Through research, I have a further understanding and discovery of 99-61-6. Product Details of 99-61-6

Fe3O4@SiO2-Pr@L-proline magnetic nanoparticles were synthesized and their efficiency as nanocatalyst for the synthesis of new derivatives of bis dapsone derived dihydropyridines via one-pot three-component condensation reaction of various aromatic aldehydes, dimedone and dapsone in aqueous media was investigated. The products were characterized by H-1 NMR, C-13 NMR, FT-IR and CHNS analysis. These bis-drugs present high antibacterial activities against both gram-negative (Pseudomonas aeruginosa and Escherichia coli) and gram-positive (Micrococcus luteus and Bacillus subtilis) bacteria, which are in general more sensitive to compounds with halogen or hydroxyl functional groups.

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Reference:
Thiomorpholine – Wikipedia,
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The important role of C7H8N2O

HPLC of Formula: C7H8N2O. About 2-Aminobenzamide, If you have any questions, you can contact Vaidya, GN; Nagpure, M; Kumar, D or concate me.

HPLC of Formula: C7H8N2O. Authors Vaidya, GN; Nagpure, M; Kumar, D in AMER CHEMICAL SOC published article about in [Vaidya, Gargi Nikhil; Nagpure, Mithilesh; Kumar, Dinesh] Natl Inst Pharmaceut Educ & Res NIPER, Dept Med Chem, Gandhinagar 382355, Gujarat, India in 2021, Cited 72. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6

A borrowing carbonate-enabled allylic cross-amination reactions employing allylic alcohol were discovered via merging acyl/allyl C-O bonds activation under nickel catalysis. The key component of this protocol is the ability of nickel [Ni(II)-Ni(0)] to execute a relay process via the nucleophilic trapping of the generated acyl Ni complex, resulting from the acyl C-O bond cleavage of dialkyl carbonates, followed by selective allylic C-O bond activations (allylic C-O vs alkyl C-O vs acyl C-O) to yield pi-allyINi-complexes. The finding truly represents Ni-catalyzed green allylic amination reactions under additive(s)-free conditions with excellent chemo- (N vs O), regio- (linear vs branched), and stereoselectivity (E vs Z) with a wide range of fundamentally challenging N-heterocycles and allylic alcohols. The reaction is scalable, does not require harmful reaction media and a globe box, and is successfully applied to the scale-up synthesis of pharmaceuticals (cinnarizine, flunarizine, and naftifine) with promising yields.

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Reference:
Thiomorpholine – Wikipedia,
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In 2020 FRONT CHEM published article about DEPENDENT RNA-POLYMERASE; SOLUBILITY MEASUREMENT; BVDV INFECTION; PESTIVIRUS; AGENTS; REPLICATION; DISCOVERY; ACCURACY; DISEASE; TARGETS in [Fernandez, Gabriela A.; Fidalgo, Daniela M.; Adler, Natalia S.; Battini, Leandro; Bollini, Mariela] Ctr Invest Bionanociencias CIBION, Lab Quim Med, Consejo Nacl Invest Cient Tecn CONICET, Buenos Aires, DF, Argentina; [Castro, Eliana F.] Ctr Invest Ciencias Vet & Agro, Inst Virol & Innovac Tecnol, Inst Nacl Tecnol Agropecuaria, Consejo Nacl Invest Cient & Tecn CONICET, Buenos Aires, DF, Argentina; [Castro, Eliana F.; Espana de Marco, Maria J.] Univ Buenos Aires, Fac Farm & Bioquim, Dept Microbiol Inmunol Biotecnol & Genet, Buenos Aires, DF, Argentina; [Rosas, Rocio A.; Fabiani, Matias; Cavallaro, Lucia V.] Univ Buenos Aires, Inst Invest Bacteriol & Virol Mol IBaViM, Dept Microbiol Inmunol Biotecnol & Genet, Catedra Virol,Fac Farm & Bioquim, Buenos Aires, DF, Argentina; [Rosas, Rocio A.; Fabiani, Matias] Consejo Nacl Invest Cient & Tecn CONICET, Buenos Aires, DF, Argentina; [Bruno, Ana M.] Univ Buenos Aires, Fac Farm & Bioquim, Dept Quim Organ, Buenos Aires, DF, Argentina in 2020, Cited 54. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6. Recommanded Product: 88-68-6

Bovine viral diarrhea virus (BVDV) belongs to the Pestivirus genus (Flaviviridae). In spite of the availability of vaccines, the virus is still causing substantial financial losses to the livestock industry. In this context, the use of antiviral agents could be an alternative strategy to control and reduce viral infections. The viral RNA-dependent RNA polymerase (RdRp) is essential for the replication of the viral genome and constitutes an attractive target for the identification of antiviral compounds. In a previous work, we have identified potential molecules that dock into an allosteric binding pocket of BVDV RdRp via a structure-based virtual screening approach. One of them, N-(2-morpholinoethyl)-2-phenylquinazolin-4-amine [1, 50% effective concentration (EC50) = 9.7 +/- 0.5 mu M], was selected to perform different chemical modifications. Among 24 derivatives synthesized, eight of them showed considerable antiviral activity. Molecular modeling of the most active compounds showed that they bind to a pocket located in the fingers and thumb domains in BVDV RdRp, which is different from that identified for other non-nucleoside inhibitors (NNIs) such as thiosemicarbazone (TSC). We selected compound 2-[4-(2-phenylquinazolin-4-yl)piperazin-1-yl]ethanol (1.9; EC50 = 1.7 +/- 0.4 mu M) for further analysis. Compound 1.9 was found to inhibit the in vitro replication of TSC-resistant BVDV variants, which carry the N264D mutation in the RdRp. In addition, 1.9 presented adequate solubility in different media and a high-stability profile in murine and bovine plasma.

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Reference:
Thiomorpholine – Wikipedia,
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Chemistry Milestones Of 1-Phenylurea

Welcome to talk about 64-10-8, If you have any questions, you can contact Slachtova, V; Chasak, J; Brulikova, L or send Email.. Computed Properties of C7H8N2O

Computed Properties of C7H8N2O. Recently I am researching about BENZOXAZOLE DERIVATIVES; BIOLOGICAL EVALUATION; DIRECT AMINATION; DESIGN; ANTICANCER; CYANATION, Saw an article supported by the Ministry of Education, Youth and Sport of the Czech RepublicMinistry of Education, Youth & Sports – Czech Republic [IGA_PrF_2019_027, JG_2019_002]; Palacky University in Olomouc. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Slachtova, V; Chasak, J; Brulikova, L. The CAS is 64-10-8. Through research, I have a further understanding and discovery of 1-Phenylurea

This study reports two synthetic approaches leading to 2-aminobenzoxazoles and their N-substituted analogues. Our first synthetic strategy involves a reaction between various o-aminophenols and N-cyano-N-phenyl-p-toluenesulfonamide as a nonhazardous electrophilic cyanating agent in the presence of Lewis acid. The second synthetic approach uses the Smiles rearrangement upon activation of benzoxazole-2-thiol with chloroacetyl chloride. Both developed synthetic protocols are widely applicable, afford the desired aminobenzoxazoles in good to excellent yields, and use nontoxic and inexpensive starting material.

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Reference:
Thiomorpholine – Wikipedia,
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Why Are Children Getting Addicted To C7H8N2O

SDS of cas: 88-68-6. About 2-Aminobenzamide, If you have any questions, you can contact Moslin, R; Zhang, YL; Wrobleski, ST; Lin, SQ; Mertzman, M; Spergel, S; Tokarski, JS; Strnad, J; Gillooly, K; McIntyre, KW; Zupa-Fernandez, A; Cheng, LH; Sun, HD; Chaudhry, C; Huang, C; D’Arienzo, C; Heimrich, E; Yang, XX; Muckelbauer, JK; Chang, C; Tredup, J; Mulligan, D; Xie, DL; Aranibar, N; Chiney, M; Burke, JR; Lombardo, L; Carter, PH; Weinstein, DS or concate me.

An article Identification of N-Methyl Nicotinamide and N-Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2) WOS:000492801800005 published article about MONOCLONAL-ANTIBODY; POTENT; ACTIVATION; MODERATE; SIGNAL; ROLES; OPTIMIZATION; USTEKINUMAB; MOLECULES; DISCOVERY in [Moslin, Ryan; Zhang, Yanlei; Wrobleski, Stephen T.; Lin, Shuqun; Mertzman, Michael; Spergel, Steven; Lombardo, Louis; Carter, Percy H.; Weinstein, David S.] Bristol Myers Squibb Res & Dev, Immunosci Discovery Chem, POB 4000, Princeton, NJ 08543 USA; [Strnad, Joann; Gillooly, Kathleen; McIntyre, Kim W.; Zupa-Fernandez, Adriana; Cheng, Lihong; Heimrich, Elizabeth; Yang, Xiaoxia; Burke, James R.] Bristol Myers Squibb Res & Dev, Immunosci Discovery Biol, POB 4000, Princeton, NJ 08543 USA; [Tokarski, John S.; Muckelbauer, Jodi K.; Chang, ChiehYing; Tredup, Jeffrey; Mulligan, Dawn; Xie, Dianlin] Bristol Myers Squibb Res & Dev, Mol Struct & Design, Mol Discovery Technol, POB 4000, Princeton, NJ 08543 USA; [Sun, Huadong; Huang, Christine; D’Arienzo, Celia; Aranibar, Nelly; Chiney, Manoj] Bristol Myers Squibb Res & Dev, Lead Discovery & Optimizat, POB 4000, Princeton, NJ 08543 USA; [Chaudhry, Charu] Bristol Myers Squibb Res & Dev, Metab & Pharmacokinet Dept, Pharmaceut Candidate Optimizat, POB 4000, Princeton, NJ 08543 USA; [Weinstein, David S.] Vividion Therapeut Inc, Chem, 5820 Nancy Ridge Dr, San Diego, CA 92121 USA in 2019, Cited 53. SDS of cas: 88-68-6. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6

As a member of the Janus OAK) family of nonreceptor tyrosine kinases, TYK2 plays an important role in mediating the signaling of pro-inflammatory cytokines including IL-12, IL-23, and type 1 interferons. The nicotinamide 4, identified by a SPA-based high-throughput screen targeting the TYK2 pseudokinase domain, potently inhibits IL-23 and IFN alpha signaling in cellular assays. The described work details the optimization of this poorly selective hit (4) to potent and selective molecules such as 47 and 48. The discoveries described herein were critical to the eventual identification of the clinical TYK2 JH2 inhibitor (see following report in this issue). Compound 48 provided robust inhibition in a mouse IL-12-induced IFN gamma pharmacodynamic model as well as efficacy in an IL-23 and IL-12-dependent mouse colitis model. These results demonstrate the ability of TYK2 JH2 domain binders to provide a highly selective alternative to conventional TYK2 orthosteric inhibitors.

SDS of cas: 88-68-6. About 2-Aminobenzamide, If you have any questions, you can contact Moslin, R; Zhang, YL; Wrobleski, ST; Lin, SQ; Mertzman, M; Spergel, S; Tokarski, JS; Strnad, J; Gillooly, K; McIntyre, KW; Zupa-Fernandez, A; Cheng, LH; Sun, HD; Chaudhry, C; Huang, C; D’Arienzo, C; Heimrich, E; Yang, XX; Muckelbauer, JK; Chang, C; Tredup, J; Mulligan, D; Xie, DL; Aranibar, N; Chiney, M; Burke, JR; Lombardo, L; Carter, PH; Weinstein, DS or concate me.

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

 

What I Wish Everyone Knew About C7H5NO3

About 3-Nitrobenzaldehyde, If you have any questions, you can contact Demidov, MR; Dobrokvashina, AN; Osipov, DV; Osyanin, VA; Klimochkin, YN or concate me.. Product Details of 99-61-6

Product Details of 99-61-6. I found the field of Chemistry very interesting. Saw the article Three-component synthesis of 2-acyl-2,3-dihydro-4H-thiochromeno[4,3-b]furan-4-ones and their reductive rearrangement into 4H,5H-thiochromeno[4,3-b]pyran-5-ones published in 2021.0, Reprint Addresses Osyanin, VA (corresponding author), Samara State Tech Univ, 244 Molodogvardeyskaya St, Samara 443100, Russia.. The CAS is 99-61-6. Through research, I have a further understanding and discovery of 3-Nitrobenzaldehyde.

Three-component condensation of in situ generated pyridinium acyl methylides with aromatic aldehydes and 4-hydroxythiocoumarin led to a series of 2-acyl-2,3-dihydro-4H-thiochromeno[4,3-b]furan-4-ones. The reaction proceeds diastereoselectively with the formation of trans-isomers and represents a cascade process involving the Knoevenagel condensation, carbo-Michael reaction, and intramolecular nucleophilic substitution. The subsequent redox rearrangement of 2-acyl-2,3-dihydro-4H-thiochromeno[4,3-b]furan-4-ones by the action of Zn and ZrCl4 grants access to 4H,5H-thiochromeno[4,3-b]pyran-5-ones.

About 3-Nitrobenzaldehyde, If you have any questions, you can contact Demidov, MR; Dobrokvashina, AN; Osipov, DV; Osyanin, VA; Klimochkin, YN or concate me.. Product Details of 99-61-6

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

 

Final Thoughts on Chemistry for 119-61-9

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Stegner, PC; Eyselein, J; Ballmann, GM; Langer, J; Schmidt, J; Harder, S in [Stegner, Philipp C.; Eyselein, Jonathan; Ballmann, Gerd M.; Langer, Jens; Schmidt, Jochen; Harder, Sjoerd] Friedrich Alexander Univ Erlangen Nurnberg, Inorgan & Organometall Chem, Egerlandstr 1, D-91058 Erlangen, Germany published Calcium catalyzed enantioselective intramolecular alkene hydroamination with chiral C-2-symmetric bis-amide ligands in 2021.0, Cited 63.0. Safety of Benzophenone. The Name is Benzophenone. Through research, I have a further understanding and discovery of 119-61-9.

The chiral building block (R)-(+)-2,2 ‘-diamino-1,1 ‘-binaphthyl, (R)-BINAM, which is often used as backbone in privileged enantioselective catalysts, was converted to a series of N-substituted proligands (R)1-H-2 (R = CH(2)tBu, C(H)Ph-2, PPh2, dibenzosuberane, 8-quinoline). After double deprotonation with strong Mg or Ca bases, a series of alkaline earth (Ae) metal catalysts (R)1-Ae.(THF)(n) was obtained. Crystal structures of these C-2-symmetric catalysts have been analyzed by quadrant models which show that the ligands with C(H)Ph-2, dibenzosuberane and 8-quinoline substituents should give the best steric discrimination for the enantioselective intramolecular alkene hydroamination (IAH) of the aminoalkenes H2C = CHCH2CR ‘ 2CH2NH2 (CR ‘(2) = CPh2, CCy or CMe2). The dianionic (R)1(2-) ligand in (R)1-Ae center dot(THF)(n) functions as reagent that deprotonates the aminoalkene substrate, while the monoanionic ((R)1-H)(-) ligand formed in this reaction functions as a chiral spectator ligand that controls the enantioselectivity of the ring closure reaction. Depending on the substituent R in the BINAM ligand, full cyclization of aminoalkenes to chiral pyrrolidine products as fast as 5 minutes was observed. Product analysis furnished enantioselectivities up to 57% ee, which marks the highest enantioselectivity reported for Ca catalyzed IAH. Higher selectivities are impeded by double protonation of the (R)1(2-) ligand leading to complete loss of chiral information in the catalytically active species.

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Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

 

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Safety of Benzophenone. Bye, fridends, I hope you can learn more about C13H10O, If you have any questions, you can browse other blog as well. See you lster.

I found the field of Food Science & Technology very interesting. Saw the article Bioconversion by gut microbiota of predigested mango (Mangifera indica L) ‘Ataulfo’ peel polyphenols assessed in a dynamic (TIM-2) in vitro model of the human colon published in 2021.0. Safety of Benzophenone, Reprint Addresses Sayago-Ayerdi, SG (corresponding author), Tecnol Nacl Mexico, Inst Tecnol Tepic, Av Inst Tecnol 2595, Tepic 63175, Nayarit, Mexico.; Mateos, R (corresponding author), CSIC, Inst Food Sci Technol & Nutr ICTAN CSIC, Jose Antonio Novais 10, Madrid 28040, Spain.. The CAS is 119-61-9. Through research, I have a further understanding and discovery of Benzophenone

Gut microbiota bioconversion of polyphenols in predigested mango ‘Ataulfo’ peel was studied using a validated, dynamic in vitro human colon model (TIM-2) with faecal microbial inoculum. Dried peels were predigested with enzymatic treatment, followed by TIM-2 fermentation (72 h). Samples were taken at 0, 24, 48 and 72 h and analyzed by HPLC-QToF. Derivatives of hydroxyphenylpropionic, hydroxyphenylacetic and hydroxybenzoic acids, as well as, pyrogallol were the main polyphenols identified. These metabolites might derivate from flavonoid (flavanols and flavonols), gallate and gallotannin biotransformation. Despite the high content of ellagic acid in mango peel, low amounts were detected in TIM-2 samples due to transformation into urolythins A and C, mainly. Xanthone and benzophenone derivatives, specific to mango, remained after the colonic biotransformation, contrary to flavonoids, which completely disappeared. In conclusion, microbial-derived metabolites, such as xanthone and benzophenone derivatives, among others, are partially stable after colonic fermentation, and thus have the potential to contribute to mango peel bioactivity.

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Thiomorpholine – Wikipedia,
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Extended knowledge of 1-Phenylurea

Welcome to talk about 64-10-8, If you have any questions, you can contact Heriyanto; Pahlevani, F; Sahajwalla, V or send Email.. HPLC of Formula: C7H8N2O

HPLC of Formula: C7H8N2O. Authors Heriyanto; Pahlevani, F; Sahajwalla, V in ELSEVIER SCI LTD published article about in [Heriyanto; Pahlevani, Farshid; Sahajwalla, Veena] UNSW, Sch Mat Sci & Engn, Ctr Sustainable Mat Res & Technol SMaRT, Sydney, NSW 2052, Australia in 2019.0, Cited 24.0. The Name is 1-Phenylurea. Through research, I have a further understanding and discovery of 64-10-8

This study reports an innovative pathway for successfully synthesizing composite panels using various waste input. For this purpose, seven types of powder from waste or widely available filler i.e. Quartz off-cut, sand, waste seashell, dolomite, limestone aggregates, concrete waste and limestone dust were used. The study aims to assess the effectiveness and mechanical properties of the various waste powder in the production of powder-resin composites. The panels were then compared with the novel polymeric glass composite (PGC) in the previous study (Heriyanto et al., 2018). Following the same procedure in PGC, the filler was individually grounded to 64-108 mu m and chemically treated with amino silane coupling agent (CA). The powder filler (untreated or treated) is then mixed with the resin binder with a ratio of 80/20 respectively, followed by hot pressing the mixture at the pressure of 550 bar at 65 degrees C for 1 h. The final composite slab is then further cut for mechanical testing. It was found in the study that when CA was not added, surface roughness of the powder particles affected the flexural strength of the final panel significantly. High surface roughness particles such as in Quartz, sand and seashell adhere effectively with the resin binder which led to higher strength. On the contrary, other factors like smooth particle morphology in glass, dolomite and limestone as well as porous structure in concrete and clump of very fine powder in limestone dust degrade the strength of the final panels. With CA addition, adhesion between resin and powder filler were improved significantly. Flexural strength after the CA treatment was found to be much affected by particle characteristics. Silica-based panels i.e. quartz, sand and glass which consist of high strength and hardness of silica particles perform better compared to that of calcium carbonate-based panels. Compression strength, toughness, stiffness, scratch resistance, density and water absorption were also reported in this study. The properties of all the treated panels are found to be comparable, or if not, much better than natural stones. These new approaches of using waste filler in powder – resin based composites can be a new alternative to produce green materials that deliver economic and environmental benefits. (C) 2019 Elsevier Ltd. All rights reserved.

Welcome to talk about 64-10-8, If you have any questions, you can contact Heriyanto; Pahlevani, F; Sahajwalla, V or send Email.. HPLC of Formula: C7H8N2O

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

 

What unique challenges do researchers face in C7H8N2O

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Martini, G; Cardone, C; Vitiello, PP; Belli, V; Napolitano, S; Troiani, T; Ciardiello, D; Della Corte, CM; Morgillo, F; Matrone, N; Sforza, V; Papaccio, G; Desiderio, V; Paul, MC; Moreno-Viedma, V; Normanno, N; Rachiglio, AM; Tirino, V; Maiello, E; Latiano, TP; Rizzi, D; Signoriello, G; Sibilia, M; Ciardiello, F; Martinelli, E in [Martini, Giulia; Cardone, Claudia; Vitiello, Pietro Paolo; Belli, Valentina; Napolitano, Stefania; Troiani, Teresa; Ciardiello, Davide; Della Corte, Carminia Maria; Morgillo, Floriana; Matrone, Nunzia; Ciardiello, Fortunato; Martinelli, Erika] Univ Campania L Vanvitelli, Med Oncol, Dept Precis Med, Via Pansini 5, I-80131 Naples, Italy; [Sforza, Vincenzo] Fdn Pascale, IRCCS, Ist Nazl Tumori, Dept Clin Expt Thorac Oncol, Naples, Italy; [Papaccio, Gianpaolo; Desiderio, Vincenzo; Tirino, Virginia] Univ Campania Luigi Vanvitelli Napoli, Dept Expt Med, Naples, Italy; [Paul, Mariel C.; Moreno-Viedma, Veronica; Sibilia, Maria] Med Univ Vienna, Comprehens Canc Ctr, Dept Med 1, Inst Canc Res, Borschkegasse 8a, Vienna, Austria; [Normanno, Nicola; Rachiglio, Anna Maria] Fdn Pascale, IRCCS, Ist Nazl Tumori, Cell Biol & Biotherapy Unit, Naples, Italy; [Maiello, Evaristo; Latiano, Tiziana Pia; Rizzi, Daniele] Hosp Casa Sollievo Della Sofferenza San Giovanni, Med Oncol, San Giovanni Rotondo, Italy; [Signoriello, Giuseppe] Univ Campania L Vanvitelli, Biostat, Dipartimento Salute Mentale & Fis & Med Prevent, Naples, Italy published EPHA2 Is a Predictive Biomarker of Resistance and a Potential Therapeutic Target for Improving Antiepidermal Growth Factor Receptor Therapy in Colorectal Cancer in 2019.0, Cited 24.0. SDS of cas: 64-10-8. The Name is 1-Phenylurea. Through research, I have a further understanding and discovery of 64-10-8.

The EPHA2 tyrosine kinase receptor is implicated in tumor progression and targeted therapies resistance. We evaluated EPHA2 as a potential resistance marker to the antiepidermal growth factor receptor (EGFR) monoclonal antibody cetuximab in colorectal cancer. We studied activation of EPHA2 in a panel of human colorectal cancer cell lines sensitive or resistant to anti-EGFR drugs. The in vitro and in vivo effects of ALW-II-41-27 (an EPHA2 inhibitor) and/or cetuximab treatment were tested. Fonnalin-fixed paraffin-embedded tumor specimens from 82 RAS wild-type (WV) metastatic colorectal cancer patients treated with FOLFIRI + cetuximab as first-line therapy in the CAPRI-COIM trial were assessed for EPHA2 expression by immunohistochemistry and correlated with treatment efficacy. EPHA2 was differentially activated in colorectal cancer cell lines. Combined treatment with ALW-II-41-27 plus cetuximab reverted primary and acquired resistance to cetuximab, causing cell growth inhibition, inducing apoptosis and cell-cycle G1-G2 arrest. In tumor xenograft models, upon progression to cetuximab, ALW-II-41-27 addition significantly inhibited tumor growth. EPHA2 protein expression was detected in 55 of 82 tumor samples, frequently expressed in less-differentiated and left-sided tumors. High levels of EPHA2 significantly correlated with worse progression-free survival [8.6 months; confidence interval (CI) 95%, 6.4-10.8; vs. 12.3 months; CI 95%, 10.4-14,2; P = 0.03] and with increased progression rate (29% vs. 9%, P = 0.02). A specific EPHA2 inhibitor reverts in vitro and in vivo primary and acquired resistance to anti-ECFR therapy. EPHA2 levels are significantly associated with worse outcome in patients treated with FOLFIRI + cetuximab. These results highlight EPHA2 as a potential therapeutic target in metastatic colorectal cancer.

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Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem