Month: October 2022

Amin, Mohammad A.; Camerino, Michelle A.; Mountford, Simon J.; Ma, Xiao; Manallack, David T.; Chalmers, David K.; Wills, Martin; Thompson, Philip E. published the artcile< (S)-(-)-Fluorenylethylchloroformate (FLEC); preparation using asymmetric transfer hydrogenation and application to the analysis and resolution of amines>, COA of Formula: C30H31ClN2O2RuS, the main research area is fluorenylethylchloroformate preparation hydrogenation.

An improved preparation of (S)-(-)-fluorenylethylchloroformate (FLEC) using an efficient asym. catalytic transfer hydrogenation as the key step was described. The application of FLEC as a chiral Fmoc equivalent for chiral resolution, with facile deprotection, of (S,S)/(S,R)-tetrahydroquinaldines I, and its capacity for inducing regioselective outcomes in nitration reactions were also demonstrated.

Tetrahedron published new progress about Chiral resolution. 1192620-83-9 belongs to class amides-buliding-blocks, and the molecular formula is C30H31ClN2O2RuS, COA of Formula: C30H31ClN2O2RuS.

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

Vu, Huu-Manh; Yong, Jia-Yuan; Chen, Fei-Wu; Li, Xu-Qin; Shi, Guo-Qing published the artcile< Rhodium-Catalyzed C(sp2)-H Amidation of Azine with Sulfonamides>, Quality Control of 6961-82-6, the main research area is regioselective rhodium catalyzed amidation azine sulfonamide.

Direct C-H amidation of azine with sulfonamide was developed for the first time. The reactions proceeded smoothly under benign conditions and gave the corresponding products with high selectivity. This approach shows high regioselectivity, wide substrate scope, and functional group tolerance. Addnl., this transformation can also be scaled up to the gram level. This strategy allows for the direct preparation of ortho-sulfonamide-substituted ketone products, thus providing a good complement to previous C-H amidation.

Journal of Organic Chemistry published new progress about Amidation. 6961-82-6 belongs to class amides-buliding-blocks, and the molecular formula is C6H6ClNO2S, Quality Control of 6961-82-6.

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

Li, Feng; Lu, Lei; Liu, Pengcheng published the artcile< Acceptorless Dehydrogenative Coupling of o-Aminobenzamides with the Activation of Methanol as a C1 Source for the Construction of Quinazolinones>, HPLC of Formula: 5004-88-6, the main research area is dehydrogenative coupling aminobenzamide methanol iridium catalyst; quinazolinone preparation dehydrogenative coupling aminobenzamide methanol iridium catalyst.

A strategy for the synthesis of quinazolinones I (R = H, 7-Me, 6-MeO, 8-F, etc.) via acceptorless coupling of o-aminobenzamides with methanol has been accomplished in the presence of the metal-ligand bifunctional catalyst [Cp*Ir(2,2′-bpyO)(H2O)]. Notably, this research exhibited the potential of transition-metal-catalyzed activation of methanol as a C1 source for the construction of heterocycles.

Organic Letters published new progress about Benzamides Role: RCT (Reactant), RACT (Reactant or Reagent) (o-aminobenzamides). 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, HPLC of Formula: 5004-88-6.

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

Nevidalova, Hana; Michalcova, Lenka; Glatz, Zdenek published the artcile< Applicability of capillary electrophoresis-frontal analysis for displacement studies: Effect of several drugs on L-tryptophan and lidocaine binding to human serum albumin>, Synthetic Route of 94-20-2, the main research area is tryptophan lidocaine human serum albumin binding constant capillary electrophoresis; drug protein binding screening; binding constant; binding sites; capillary electrophoresis-frontal analysis; drug competition; human serum albumin.

The effective concentration of a drug in the blood, i.e. the concentration of a free drug in the blood, is influenced by the strength of drug binding onto plasma proteins. Besides its efficacy, these interactions subsequently influence the liberation, absorption, distribution, metabolism, excretion, and toxicol. properties of the drug. It is important to not only determine the binding strength and stoichiometry, but also the binding site of a drug on the plasma protein mol., because the co-administration of drugs with the same binding site can affect the above-mentioned concentration and as a result the pharmacol. behavior of the drugs and lead to side effects caused by the change in free drug concentration, its toxicity. In this study, the binding characteristics of six drugs with human serum albumin, the most abundant protein in human plasma, were determined by capillary electrophoresis-frontal anal., and the obtained values of binding parameters were compared with the literature data. The effect of several drugs and site markers on the binding of L-tryptophan and lidocaine to human serum albumin was investigated in subsequent displacement studies which thus demonstrated the usability of capillary electrophoresis as an automated high-throughput screening method for drug-protein binding studies.

Journal of Separation Science published new progress about Capillary electrophoresis. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Synthetic Route of 94-20-2.

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

Raffa, Demetrio; Maggio, Benedetta; Raimondi, Maria Valeria; Cusimano, Maria Grazia; Amico, Giandomenico; Carollo, Anna; Conaldi, Pier Giulio; Bai, Ruoli; Hamel, Ernest; Daidone, Giuseppe published the artcile< 2-Cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity, and mechanism of action>, Formula: C9H12N2O3, the main research area is cinnamamido phenylpropiolamido phenylpropanamidobenzamide preparation anticancer; 2-(3-Phenylpropanamido)benzamides; 2-(3-Phenylpropiolamido)benzamides; 2-Cinnamamidobenzamides; Antiproliferative activity; Apoptosis; DYCGFIFOMKVDQP-UHFFFAOYSA-N; GAEWJVNXMYWFOT-FPYGCLRLSA-N; GLOIPBXNPXFMCD-CMDGGOBGSA-N; GTMVKWANDDSBPP-UHFFFAOYSA-N; GUWKFLZAMNTMFA-UHFFFAOYSA-N; IBBGALVVPWZGNP-JXMROGBWSA-N; IRYCZCAWVJZWKT-QPJJXVBHSA-N; JZURWIGFELHAQF-UHFFFAOYSA-N; LIWFXFAWCAUFBU-UHFFFAOYSA-N; LRIOFNWWMBLPSV-RMKNXTFCSA-N; MTEXNJMFEMIDJZ-CSKARUKUSA-N; MVXMFTXNNUIRAF-UHFFFAOYSA-N; MWHVYZNXRYFKFD-UHFFFAOYSA-N; OEHLQIRCXNADOK-JXMROGBWSA-N; PIQFLKOEQNXADK-QPJJXVBHSA-N; QUNOMTLXTSUWOB-CMDGGOBGSA-N; RHBJSXACCJTPRE-UHFFFAOYSA-N; USJUKEPNAZAKSG-UHFFFAOYSA-N; WMHHXKMPUMTPIJ-RMKNXTFCSA-N; WPPDXKZWCFUROB-UHFFFAOYSA-N; XMXNTDIXMAUMEJ-UHFFFAOYSA-N; ZLNSPXKNAWBJIG-ZHACJKMWSA-N; ZXBUZBGNIFHLGX-UHFFFAOYSA-N.

Several new benzamides were synthesized by stirring in pyridine the acid chlorides with the appropriate anthranilamide derivatives Some of the synthesized compounds were evaluated for their in vitro antiproliferative activity against a panel of 5 human cell lines (K562 human chronic myelogenous leukemia cells, MCF-7 breast cancer cells, HTC-116 and HT26 colon cancer cells and NCI H460 non-small cell lung cancer cells).

European Journal of Medicinal Chemistry published new progress about Acid chlorides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Formula: C9H12N2O3.

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

Ogawa, Nobuo; Yoshida, Toshihiko; Aratani, Takayuki; Koshinaka, Eiichi; Kato, Hideo; Ito, Yasuo published the artcile< Synthesis and histamine H2-antagonist activity of 4-quinazolinone derivatives>, Quality Control of 5004-88-6, the main research area is piperidinylmethylphenoxypropylaminoquinazolinone preparation antiulcer histamine antagonist; quinazolinone piperidinylmethylphenoxypropylamino preparation histamine antagonist; structure activity aminomethylphenoxyalkylaminoquinazolinone histamine antagonist.

With the aim of developing new antiulcer agents, a series of 4-quinazolinone derivatives e.g., I (R = piperidino, pyrrolidino, morpholino, R1 = H, OMe, R2 = H, Me; n = 2, 3, 4) was synthesized and tested for histamine H2-antagonist activity and gastric antisecretory activity. Thus, 2-alkylamino-, 2-alkylthio-, and 2-alkyl-4-quinazolinones were prepared by the condensation of alkylamines with 2-chloro- or 2-methylthio-4-quinazolinones, the condensation of alkyl bromides with 2-mercapto-4-quinazolinones, and the condensation of alkylcarboxylic acids with anthranilamides, resp. Several of the 4-quinazolinone derivatives showed potent H2-antagonist activity, and one of them, I (R = piperidino, R1 = R2 = H, n = 3), showed the most potent antisecretory activity. The structure-activity relationships are discussed.

Chemical & Pharmaceutical Bulletin published new progress about Histamine H2 receptor antagonists. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Quality Control of 5004-88-6.

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

Zhang, Qing; Zhou, Yue; Feng, Xingyu; Gao, Yuan; Huang, Chengzhi; Yao, Xueqing published the artcile< Low-dose orlistat promotes the therapeutic effect of oxaliplatin in colorectal cancer>, COA of Formula: C29H53NO5, the main research area is Apoptosis; Colorectal cancer; Low-dose Orlistat; Oxaliplatin; PDX models.

The failure of and resistance to oxaliplatin (OXA)-based chemotherapies may lead to poor prognosis in colorectal cancer (CRC) patients. It has been reported that orlistat (Orli) exhibits potent antitumor effects in several malignant tumors. Here, we identified that OXA in combination with low-dose Orli could sensitize CRC cells to OXA and induce marked synergistic apoptosis in vitro and in vivo. The potential synergistic effects were confirmed and quantified by in silico anal. Furthermore, we validated the synergistic anti-tumor effects in CRC PDX mice model. A qPCR array was performed to evaluate the changes in 85 apoptosis-related genes to elucidate the possible mol. mechanisms in combination-induced cytotoxicity. To conclude, the antitumor synergistic effects of OXA and Orli make them effective and promising candidates for cancer treatment.

Biomedicine & Pharmacotherapy published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, COA of Formula: C29H53NO5.

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

Appel, Rolf; Montenarh, Mathias published the artcile< Addition reaction of N,N-dialkylsulfamides, tertiary amines, and phosphines with fluorosulfonyl isocyanate>, Category: amides-buliding-blocks, the main research area is addition sulfamide fluorosulfonyl isocyanate; amine fluorosulfonyl isocyanate reaction; phosphine fluorosulfonyl isocyanate reaction; urea fluorosulfonyl sulfamoyl.

Addition of RSO2NH2 to FSO2NCO gave 72-98% RSO2NHCONHSO2F (R = Me2N, piperidino, morpholino, MeO), thermal decomposition of which gave 20-48% RSO2F (R = Me2N, piperidino, morpholino). The reaction of FSO2NCO with amines and phosphines gave 91-99% 1:1 adducts RR12E+CON-SO2F (RR12E = Et3N, pyridine, Me3P, PhEt2P, MePh2P, Ph3P).

Chemische Berichte published new progress about Addition reaction. 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Category: amides-buliding-blocks.

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

Nascimento, Jessica; Mariot, Camila; Vianna, Debora R. B.; Kliemann, Lucia M.; Chaves, Paula S.; Loda, Massimo; Buffon, Andreia; Beck, Ruy C. R.; Pilger, Diogo A. published the artcile< Fatty acid synthase as a potential new therapeutic target for cervical cancer>, Electric Literature of 96829-58-2, the main research area is .

Fatty acid synthase (FASN) is the rate-limiting enzyme for the de novo synthesis of fatty acids in the cytoplasm of tumor cells. Many tumor cells express high levels of FASN, and its expression is associated with a poorer prognosis. Cervical cancer is a major public health problem, representing the fourth most common cancer affecting women worldwide. To date, only a few in silico studies have correlated FASN expression with cervical cancer. This study aimed to investigate in vitro FASN expression in premalignant lesions and cervical cancer samples and the effects of a FASN inhibitor on cervical cancer cells. FASN expression was observed in all cervical cancer samples with increased expression at more advanced cervical cancer stages. The FASN inhibitor (orlistat) reduced the in vitro cell viability of cervical cancer cells (C-33A, ME-180, HeLa and SiHa) in a time-dependent manner and triggered apoptosis. FASN inhibitor also led to cell cycle arrest and autophagy. FASN may be a potential therapeutic target for cervical cancer, and medicinal chemists, pharmaceutical researchers and formulators should consider this fi nding in the development of new treatment approaches for this cancer type.

Anais da Academia Brasileira de Ciencias published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Electric Literature of 96829-58-2.

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

Barry, Jeremy A.; Groseclose, Mark Reid; Castellino, Stephen published the artcile< Quantification and assessment of detection capability in imaging mass spectrometry using a revised mimetic tissue model>, Related Products of 94-20-2, the main research area is liver kidney brain tissue distribution clozapine; LC–MS validation; detection capability; imaging MS; mimetic tissue model; quantification.

Aim: A revised method of preparing the mimetic tissue model for quant. imaging mass spectrometry (IMS) is evaluated. Concepts of assessing detection capability are adapted from other imaging or mass spectrometry (MS)-based technologies to improve upon the reliability of IMS quantification. Materials & methods: The mimetic tissue model is prepared by serially freezing spiked-tissue homogenates into a cylindrical mold to create a plug of tissue with a stepped concentration gradient of matrix-matched standards Weighted least squares (WLS) linear regression is applied due to the heteroscedastisity (change in variance with intensity) of most MS data. Results & conclusions: Imaging poses several caveats for quantification which are unique compared with other MS-based methods. Aspects of the design, construction, application, and evaluation of the matrix-matched standard curve for the mimetic tissue model are discussed. In addition, the criticality of the ion distribution in the design of a purposeful liquid chromatog. coupled to mass spectrometry (LC-MS) validation is reviewed.

Bioanalysis published new progress about Biopsy. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Related Products of 94-20-2.

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