Tag: M.W=150-200

An article Structure-Based Discovery of SD-36 as a Potent, Selective, and Efficacious PROTAC Degrader of STAT3 Protein WOS:000505633400021 published article about E3 UBIQUITIN LIGASE; 2 SH2 DOMAIN; SIGNAL TRANSDUCER; PEPTIDOMIMETIC INHIBITORS; SMALL MOLECULES; DESIGN; DEGRADATION; ACTIVATOR; OPTIMIZATION; VALIDATION in [Zhou, Haibin; Bai, Longchuan; Xu, Renqi; Zhao, Yujun; Chen, Jianyong; McEachern, Donna; Yang, Chao-Yie; Liu, Zhaomin; Wang, Mi; Liu, Liu; Yi, Han; Wang, Shaomeng] Univ Michigan, Rogel Canc Ctr, Ann Arbor, MI 48109 USA; [Zhou, Haibin; Bai, Longchuan; Xu, Renqi; Zhao, Yujun; Chen, Jianyong; McEachern, Donna; Yang, Chao-Yie; Liu, Zhaomin; Wang, Mi; Liu, Liu; Yi, Han; Wang, Shaomeng] Univ Michigan, Dept Internal Med, Ann Arbor, MI 48109 USA; [Wang, Shaomeng] Univ Michigan, Dept Pharmacol, Med Sch, Ann Arbor, MI 48109 USA; [Wang, Shaomeng] Univ Michigan, Coll Pharm, Med Chem, 428 Church St, Ann Arbor, MI 48109 USA; [Chinnaswamy, Krishnapriya; Meagher, Jennifer L.; Stuckey, Jeanne A.] Univ Michigan, Life Sci Inst, Ann Arbor, MI 48109 USA; [Wen, Bo; Dai, Lipeng; Kumar, Praveen; Sun, Duxin] Univ Michigan, Coll Pharm, Dept Pharmaceut Sci, 428 Church St, Ann Arbor, MI 48109 USA in 2019.0, Cited 43.0. Computed Properties of C13H13N. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9

Signal transducer and activator of transcription 3 (STAT3) is a transcription factor and an attractive therapeutic target for cancer and other human diseases. Despite 20 years of persistent research efforts, targeting STAT3 has been very challenging. We report herein the structure-based discovery of potent small-molecule STAT3 degraders based upon the proteolysis targeting chimera (PROTAC) concept. We first designed SI-109 as a potent, small-molecule inhibitor of the STAT3 SH2 domain. Employing ligands for cereblon/cullin 4A E3 ligase and SI-109, we obtained a series of potent PROTAC STAT3 degraders, exemplified by SD-36. SD-36 induces rapid STAT3 degradation at low nanomolar concentrations in cells and fails to degrade other STAT proteins. SD-36 achieves nanomolar cell growth inhibitory activity in leukemia and lymphoma cell lines with high levels of phosphorylated STAT3. A single dose of SD-36 results in complete STAT3 protein degradation in xenograft tumor tissue and normal mouse tissues. SD-36 achieves complete and long-lasting tumor regression in the Molm-16 xenograft tumor model at well-tolerated dose-schedules. SD-36 is a potent, selective, and efficacious STAT3 degrader.

Computed Properties of C13H13N. Welcome to talk about 91-00-9, If you have any questions, you can contact Zhou, HB; Bai, LC; Xu, RQ; Zhao, YJ; Chen, JY; McEachern, D; Chinnaswamy, K; Wen, B; Dai, LP; Kumar, P; Yang, CY; Liu, ZM; Wang, M; Liu, L; Meagher, JL; Yi, H; Sun, DX; Stuckey, JA; Wang, SM or send Email.

Reference:
Amide – Wikipedia,
,Amide – an overview | ScienceDirect Topics

Recently I am researching about NEDD8-ACTIVATING ENZYME-INHIBITOR; PROTEIN NEDDYLATION; IDENTIFICATION; PATHWAY; DEGRADATION; DISCOVERY; APOPTOSIS; LIGASES, Saw an article supported by the Chinese Minister of Science and Technology grant [2016YFA0501800]; National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [81872747, 21702061, 81625018, 81820108022]; Innovative Research Team of High-level Local Universities in Shanghai; National Special Fund for State Key Laboratory of Bioreactor Engineering [2060204]; National Key R&D Programof China [2017YFB0202600]; Innovation Program of Shanghai Municipal Education CommissionInnovation Program of Shanghai Municipal Education Commission [2019-01-07-00-10-E00056]; Program of Shanghai Academic/Technology Research Leader [18XD1403800]. Published in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER in ISSY-LES-MOULINEAUX ,Authors: Chen, X; Yang, X; Mao, F; Wei, JL; Xu, YX; Li, BL; Zhu, J; Ni, SS; Jia, LJ; Li, J. The CAS is 91-00-9. Through research, I have a further understanding and discovery of Diphenylmethanamine. Name: Diphenylmethanamine

Ubiquitin-like protein neddylation is overactivated in various human cancers and correlates with disease progression, and targeting this pathway represents a valuable therapeutic strategy. Our previous work disclosed an antihypertensive agent, candesartan cilexetic (CDC), serves as a novel neddylation inhibitor for suppressing tumor growth by targeting Nedd8-activating enzyme (NAE). In this study, 42 benzimidazole derivatives were designed and synthesized based on lead compound CDC to improve the neddylation inhibition and anticancer efficacy. Optimal benzimidazole-derived 35 displayed superior neddylation inhibition in enzyme assay compared to CDC (IC50 = 5.51 mu M vs 16.43 mu M), along with promising target inhibitory activity and killing selectivity in cancer cell. The results of cellular mechanism research combined with tumor growth suppression in human lung cancer cell A549 in vivo, accompanied with docking model, revealed that 35 has the potential to be developed as a promising neddylation inhibitor for anticancer therapy. (C) 2020 Elsevier Masson SAS. All rights reserved.

Welcome to talk about 91-00-9, If you have any questions, you can contact Chen, X; Yang, X; Mao, F; Wei, JL; Xu, YX; Li, BL; Zhu, J; Ni, SS; Jia, LJ; Li, J or send Email.. Name: Diphenylmethanamine

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Amide – Wikipedia,
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An article Enhancement of Benzothiazoles as Pteridine Reductase-1 Inhibitors for the Treatment of Trypanosomatidic Infections WOS:000466053900012 published article about DIHYDROFOLATE-REDUCTASE; THYMIDYLATE SYNTHASE; BINDING MODES; LEISHMANIA; IDENTIFICATION; ASSAY; DERIVATIVES; VALIDATION; SOLUBILITY; RESISTANCE in [Linciano, Pasquale; Luciani, Rosaria; Sesenna, Antony; Quotadamo, Antonio; Costantino, Luca; Costi, Maria Paola] Univ Modena & Reggio Emilia, Dipartimento Sci Vita, Via Campi 103, I-41125 Modena, Italy; [Pozzi, Cecilia; dello Iacono, Lucia; di Pisa, Flavio; Landi, Giacomo; Bonucci, Alessio; Mangani, Stefano] Univ Siena, Dipartimento Biotecnol Chim & Farm, Via Aldo Moro 2, I-53100 Siena, Italy; [Gul, Sheraz; Kuzikov, Maria; Ellinger, Bernhard; Witt, Gesa] Fraunhofer Inst Mol Biol & Appl Ecol Screening Po, D-22525 Hamburg, Germany; [Santarem, Nuno; Baptista, Catarina] Inst Mol & Cell Biol, P-4150180 Porto, Portugal; [Santarem, Nuno; Baptista, Catarina] Univ Porto, Inst Invest & Inovacao Saude, P-4150180 Porto, Portugal; [Franco, Caio; Moraes, Carolina B.] CNPEM, Lab Nacl Biociencias LNBio, BR-13083100 Campinas, SP, Brazil; [Mueller, Wolfgang; Wittig, Ulrike] HITS, Sci Databases & Visualizat Grp, D-69118 Heidelberg, Germany; [Wittig, Ulrike] HITS, Mol & Cellular Modeling Grp, D-69118 Heidelberg, Germany; [Franco, Caio; Moraes, Carolina B.] Univ Sao Paulo, Dept Microbiol, Inst Biomed Sci, BR-05508900 Sao Paulo, SP, Brazil in 2019.0, Cited 57.0. Name: Diphenylmethanamine. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9

2-Amino-benzo[d]thiazole was identified as a new scaffold for the development of improved pteridine reductase-1 (PTR1) inhibitors and anti-trypanosomatidic agents. Molecular docking and crystallography guided the design and synthesis of 42 new benzothiazoles. The compounds were assessed for Trypanosoma brucei and Leishmania major PTR1 inhibition and in vitro activity against T. brucei and amastigote Leishmania infantum. We identified several 2-amino-benzo[d]thiazoles with improved enzymatic activity (TbPTR1 IC50 = 0.35 mu M; LmPTR1 IC50 = 1.9 mu M) and low mu M antiparasitic activity against T. brucei. The ten most active compounds against TbPTR1 were able to potentiate the antiparasitic activity of methotrexate when evaluated in combination against T. brucei, with a potentiating index between 1.2 and 2.7. The compound library was profiled for early ADME toxicity, and 2-amino-N-benzylbenzo[d]thiazole-6-carboxamide (4c) was finally identified as a novel potent, safe, and selective anti-trypanocydal agent (EC50 = 7.0 mu M). Formulation of 4c with hydroxypropyl-beta-cyclodextrin yielded good oral bioavailability, encouraging progression to in vivo studies.

Welcome to talk about 91-00-9, If you have any questions, you can contact Linciano, P; Pozzi, C; dello Iacono, L; di Pisa, F; Landi, G; Bonucci, A; Gul, S; Kuzikov, M; Ellinger, B; Witt, G; Santarem, N; Baptista, C; Franco, C; Moraes, CB; Muller, W; Wittig, U; Luciani, R; Sesenna, A; Quotadamo, A; Ferrari, S; Pohner, I; Cordeiro-Da-Silva, A; Mangani, S; Costantino, L; Costi, MP or send Email.. Name: Diphenylmethanamine

Reference:
Amide – Wikipedia,
,Amide – an overview | ScienceDirect Topics

HPLC of Formula: C13H13N. Recently I am researching about SUFEX CLICK CHEMISTRY; NUCLEOPHILIC-SUBSTITUTION; N-ALKYLATION; SULFONAMIDES; ARYL; DISCOVERY; AMINES; ARYLATION; PEPTIDES; REAGENTS, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [21502241]; Natural Science Foundation of Guangdong ProvinceNational Natural Science Foundation of Guangdong Province [2016A030313290]. Published in WILEY-V C H VERLAG GMBH in WEINHEIM ,Authors: Wei, MJ; Liang, DC; Cao, XH; Luo, WJ; Ma, GJ; Liu, ZY; Li, L. The CAS is 91-00-9. Through research, I have a further understanding and discovery of Diphenylmethanamine

A broad-spectrum, catalytic method has been developed for the synthesis of sulfonamides and sulfamates. With the activation by the combination of a catalytic amount of 1-hydroxybenzotriazole (HOBt) and silicon additives, amidations of sulfonyl fluorides and fluorosulfates proceeded smoothly and excellent yields were generally obtained (87-99 %). Noticeably, this protocol is particularly efficient for sterically hindered substrates. Catalyst loading is generally low and only 0.02 mol % of catalyst is required for the multidecagram-scale synthesis of an amantadine derivative. In addition, the potential of this method in medicinal chemistry has been demonstrated by the synthesis of the marketed drug Fedratinib via a key intermediate sulfonyl fluoride 13. Since a large number of amines are commercially available, this route provides a facile entry to access Fedratinib analogues for biological screening.

HPLC of Formula: C13H13N. Welcome to talk about 91-00-9, If you have any questions, you can contact Wei, MJ; Liang, DC; Cao, XH; Luo, WJ; Ma, GJ; Liu, ZY; Li, L or send Email.

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Amide – Wikipedia,
,Amide – an overview | ScienceDirect Topics

In 2020.0 ORG PROCESS RES DEV published article about HYDROGEN; BROMIDES; OLEFINS; ARYL in [Kallemeyn, Jeffrey M.; Engstrom, Kenneth M.; Pelc, Matthew J.; Lukin, Kirill A.; Morrill, Westin H.; Wei, Haojuan; Towne, Timothy B.; Henle, Jeremy; Nere, Nandkishor K.; Welch, Dennie S.; Shekhar, Shashank; Ravn, Matthew M.; Zhao, Gang; Fickes, Michael G.; Cink, Russell D.] AbbVie Inc, Proc Res & Dev, N Chicago, IL 60064 USA; [Ding, Chen; Vinci, John C.; Marren, James] AbbVie Inc, Analyt Res & Dev, N Chicago, IL 60064 USA in 2020.0, Cited 35.0. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9. Recommanded Product: 91-00-9

Glecaprevir was identified as a potent hepatitis C virus (HCV) protease inhibitor, and a large-scale synthesis was required to support the late-stage clinical trials and subsequent commercial launch. The large-scale synthetic route to glecaprevir required the development of completely new synthetic approaches to the two key structural features: the 18-membered macrocycle 3 and the difluoromethyl-substituted cyclopropyl amino acid 4. In this first manuscript, we describe the route development for the macrocycle 3; the second manuscript will describe the development of a new synthetic route to the difluoromethyl-substituted cyclopropyl amino acid 4 and the final assembly of glecaprevir. The large-scale synthetic route to the macrocycle employed a unique intramolecular etherification reaction as the key step in the macrocycle synthesis, avoiding the scalability limitations of the ring-closing metathesis (RCM) reaction of the enabling route. The large-scale synthetic route to the macrocycle was successfully used to produce the amount of glecaprevir required to support the late-stage clinical development.

Recommanded Product: 91-00-9. About Diphenylmethanamine, If you have any questions, you can contact Kallemeyn, JM; Engstrom, KM; Pelc, MJ; Lukin, KA; Morrill, WH; Wei, HJ; Towne, TB; Henle, J; Nere, NK; Welch, DS; Shekhar, S; Ravn, MM; Zhao, G; Fickes, MG; Ding, C; Vinci, JC; Marren, J; Cink, RD or concate me.

Reference:
Amide – Wikipedia,
,Amide – an overview | ScienceDirect Topics

Safety of Diphenylmethanamine. Hatano, M; Nishio, K; Mochizuki, T; Nishikawa, K; Ishihara, K in [Hatano, Manabu; Nishio, Kosuke; Mochizuki, Takuya; Nishikawa, Keisuke; Ishihara, Kazuaki] Nagoya Univ, Grad Sch Engn, Chikusa Ku, Furo Cho, Nagoya, Aichi 4648603, Japan published Highly Active Chiral Dilithium(I) Binaphthyldisulfonate Catalysts for Enantio- and Chemoselective Strecker-Type Reactions in 2019.0, Cited 84.0. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9.

An enantioselective Strecker-type reaction of aldimines and ketimines was developed by using a chiral dilithium(I) binaphthyldisulfonate as a chiral acid-base cooperative catalyst. The present catalytic system features an extremely short reaction time (10 min to 4 h), unlike conventional catalytic systems. Along with the design of stronger chiral Li(I) Lewis acid catalysts, a highly reactive pentacoordinate silicate generated in situ could promote the reactions. In particular, instead of unstable N-Bn Strecker products, more stable N-CH2 (9-anthryl) and N-CH2 (1-naphthyl) Strecker products could be obtained in high yields with high enantioselectivities. By a switch of the present and previous catalyst systems, chemoselective cyanation to a ketoaldimine could be performed, respectively. Moreover, mechanistic investigations provided useful information regarding the active catalysts, catalytic cycles, and possible transition states.

Safety of Diphenylmethanamine. Welcome to talk about 91-00-9, If you have any questions, you can contact Hatano, M; Nishio, K; Mochizuki, T; Nishikawa, K; Ishihara, K or send Email.

Reference:
Amide – Wikipedia,
,Amide – an overview | ScienceDirect Topics

Recommanded Product: 91-00-9. Recently I am researching about H BOND-CLEAVAGE; N-C CLEAVAGE; SECONDARY AMIDES; CARBOXAMIDES; ACTIVATION, Saw an article supported by the National Research Foundation of Korea (NRF) – Korea Government (MSIT) [NRF-2021R1A2C1005169]. Published in ROYAL SOC CHEMISTRY in CAMBRIDGE ,Authors: Joseph, D; Park, MS; Lee, S. The CAS is 91-00-9. Through research, I have a further understanding and discovery of Diphenylmethanamine

N-Acyl lactam amides, such as benzoylpyrrolidin-2-one, benzoylpiperidin-2-one, and benzoylazepan-2-one reacted with amines in the presence of DTBP and TBAI to afford the transamidated products in good yields. The reactions were conducted under aqueous conditions and good functional group tolerance was achieved. Both aliphatic and aromatic primary amines displayed good activity under metal-free conditions. A radical reaction pathway is proposed.

Welcome to talk about 91-00-9, If you have any questions, you can contact Joseph, D; Park, MS; Lee, S or send Email.. Recommanded Product: 91-00-9

Reference:
Amide – Wikipedia,
,Amide – an overview | ScienceDirect Topics

Recently I am researching about SUCCINAMIC ACID; 1,4-DITHIINS; BINDING; ESTER, Saw an article supported by the Pakistan Science Foundation (PSF) through a research project entitled, Synthesis of Heterocyclic Organic Compounds for Drug Development [PSF/Res/SPCSIR/Chem(478)]. Published in UNIV KARACHI in KARACHI ,Authors: Ahme, S; Perveen, S; Khan, KM; Naz, F; Ali, RA; Ajaz, M; Shah, S. The CAS is 91-00-9. Through research, I have a further understanding and discovery of Diphenylmethanamine. HPLC of Formula: C13H13N

Sixteen derivatives of dithiin diisoimide 2a-2p have been synthesized and screened for antibacterial and antifungal activity. Compounds 2a-2g and 2i-2p are almost same or more active than gentamicine against Acinetobacter. Whereby compound 2,6-didodecyl-1H,5H-pyrrolo[3′,4′,5,6][1,4]dithiino[2,3-c]pyrrole-1,3,5,7(2H,6H)-tetrone (2d) having zone of inhibition 20 mm against Acinetobacter is the most potent among all these compounds and can be used as lead compound for the treatment of Acinetobacter infection.

HPLC of Formula: C13H13N. Welcome to talk about 91-00-9, If you have any questions, you can contact Ahme, S; Perveen, S; Khan, KM; Naz, F; Ali, RA; Ajaz, M; Shah, S or send Email.

Reference:
Amide – Wikipedia,
,Amide – an overview | ScienceDirect Topics

Recently I am researching about EFFICIENT RECYCLABLE CATALYST; DBN TETRAPHENYLBORATE SALTS; DIRECT AMIDATION; CARBOXYLIC-ACIDS; HIGHLY EFFICIENT; SILICA-GEL; ALCOHOLS; AMINES; PHENOLS; SOLVENT, Saw an article supported by the . Published in ROYAL SOC CHEMISTRY in CAMBRIDGE ,Authors: Ghosh, S; Purkait, A; Jana, CK. The CAS is 91-00-9. Through research, I have a further understanding and discovery of Diphenylmethanamine. Quality Control of Diphenylmethanamine

An operationally simple and general method for acetylation and acylation of a wide variety of substrates (amines, alcohols, phenols, thiols, and hydrazones) has been reported. Meldrum’s acid and its derivatives have been used as an air-stable, non-volatile, cost-effective, and easy to handle acetylating/acylating agent. Easily separable byproducts (CO2 and acetone) allowed the isolation of analytically pure acetylated products without the requirement of work-up and any chromatography.

Welcome to talk about 91-00-9, If you have any questions, you can contact Ghosh, S; Purkait, A; Jana, CK or send Email.. Quality Control of Diphenylmethanamine

Reference:
Amide – Wikipedia,
,Amide – an overview | ScienceDirect Topics

I found the field of Chemistry very interesting. Saw the article Development of a Large-Scale Route to Glecaprevir: Synthesis of the Macrocycle via Intramolecular Etherification published in 2020.0. Category: amides-buliding-blocks, Reprint Addresses Cink, RD (corresponding author), AbbVie Inc, Proc Res & Dev, N Chicago, IL 60064 USA.. The CAS is 91-00-9. Through research, I have a further understanding and discovery of Diphenylmethanamine

Glecaprevir was identified as a potent hepatitis C virus (HCV) protease inhibitor, and a large-scale synthesis was required to support the late-stage clinical trials and subsequent commercial launch. The large-scale synthetic route to glecaprevir required the development of completely new synthetic approaches to the two key structural features: the 18-membered macrocycle 3 and the difluoromethyl-substituted cyclopropyl amino acid 4. In this first manuscript, we describe the route development for the macrocycle 3; the second manuscript will describe the development of a new synthetic route to the difluoromethyl-substituted cyclopropyl amino acid 4 and the final assembly of glecaprevir. The large-scale synthetic route to the macrocycle employed a unique intramolecular etherification reaction as the key step in the macrocycle synthesis, avoiding the scalability limitations of the ring-closing metathesis (RCM) reaction of the enabling route. The large-scale synthetic route to the macrocycle was successfully used to produce the amount of glecaprevir required to support the late-stage clinical development.

Welcome to talk about 91-00-9, If you have any questions, you can contact Kallemeyn, JM; Engstrom, KM; Pelc, MJ; Lukin, KA; Morrill, WH; Wei, HJ; Towne, TB; Henle, J; Nere, NK; Welch, DS; Shekhar, S; Ravn, MM; Zhao, G; Fickes, MG; Ding, C; Vinci, JC; Marren, J; Cink, RD or send Email.. Category: amides-buliding-blocks

Reference:
Amide – Wikipedia,
,Amide – an overview | ScienceDirect Topics