Tag: 300-400

Synthesis and antiproliferative activity of C- and N-terminal analogues of culicinin D was written by Li, Freda F.;Stubbing, Louise A.;Kavianinia, Iman;Abbattista, Maria R.;Harris, Paul W. R.;Smaill, Jeff B.;Patterson, Adam V.;Brimble, Margaret A.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2020.Computed Properties of C21H21NO4 The following contents are mentioned in the article:

Culicinin D, a 10 amino acid peptaibol containing several unusual residues, has been shown to exhibit potent anticancer activity. Previous work in our group towards developing a structure-activity relationship (SAR) for this peptaibol has concentrated on replacement of the synthetically challenging AHMOD and AMD residues, resulting in the discovery of analogs with equivalent or better potency and simplified synthesis. The SAR of this peptaibol is extended in this work by investigating the effect of the N-terminal lipid tail and C-terminal amino alc., revealing the key contribution of each of these moieties on antiproliferative activity in a panel of breast and lung cancer cell lines. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Computed Properties of C21H21NO4).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N–H bond in an axial position, and the other in an equatorial position.Computed Properties of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthesis and antiproliferative activity of C- and N-terminal analogues of culicinin D was written by Li, Freda F.;Stubbing, Louise A.;Kavianinia, Iman;Abbattista, Maria R.;Harris, Paul W. R.;Smaill, Jeff B.;Patterson, Adam V.;Brimble, Margaret A.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2020.Name: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid The following contents are mentioned in the article:

Culicinin D, a 10 amino acid peptaibol containing several unusual residues, has been shown to exhibit potent anticancer activity. Previous work in our group towards developing a structure-activity relationship (SAR) for this peptaibol has concentrated on replacement of the synthetically challenging AHMOD and AMD residues, resulting in the discovery of analogs with equivalent or better potency and simplified synthesis. The SAR of this peptaibol is extended in this work by investigating the effect of the N-terminal lipid tail and C-terminal amino alc., revealing the key contribution of each of these moieties on antiproliferative activity in a panel of breast and lung cancer cell lines. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Name: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Name: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Design of short linear peptides that show hydrogen bonding constraints in water was written by Song, Ben-Ben;Kibler, Patrick;Malde, Alpeshkumar;Kodukula, Krishna;Galande, Amit K.. And the article was included in Journal of the American Chemical Society in 2010.Electric Literature of C21H21NO4 The following contents are mentioned in the article:

Using a combination of an aromatic amino acid, a homoserine side chain, and a D-amino acid, a series of linear tetrapeptides were designed that adopt an “Hse turn” in water. The conformation was stabilized by intramol. hydrogen bonds even in the presence of surrounding water mols. In particular, the peptide with sequence H-Abz-Homoser-Ser-D-Gln-NH₂ showed significant through-space interactions and its free energy of folding is estimated to be on the order of -4 kcal/mol. We report the design of the tetrapeptides using a novel mimicry approach and their characterization based on NMR spectroscopy and MD simulations. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Electric Literature of C21H21NO4).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Electric Literature of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Design of short linear peptides that show hydrogen bonding constraints in water was written by Song, Ben-Ben;Kibler, Patrick;Malde, Alpeshkumar;Kodukula, Krishna;Galande, Amit K.. And the article was included in Journal of the American Chemical Society in 2010.Reference of 86069-86-5 The following contents are mentioned in the article:

Using a combination of an aromatic amino acid, a homoserine side chain, and a D-amino acid, a series of linear tetrapeptides were designed that adopt an “Hse turn” in water. The conformation was stabilized by intramol. hydrogen bonds even in the presence of surrounding water mols. In particular, the peptide with sequence H-Abz-Homoser-Ser-D-Gln-NH₂ showed significant through-space interactions and its free energy of folding is estimated to be on the order of -4 kcal/mol. We report the design of the tetrapeptides using a novel mimicry approach and their characterization based on NMR spectroscopy and MD simulations. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Reference of 86069-86-5).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Reference of 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Creating Diverse Target-Binding Surfaces on FKBP12: Synthesis and Evaluation of a Rapamycin Analogue Library was written by Wu, Xiang-Hong;Wang, Li-Sheng;Han, Yao-Hua;Regan, Nicholas;Li, Pui-Kai;Villalona, Miguel A.;Hu, Xi-Che;Briesewitz, Roger;Pei, De-Hua. And the article was included in ACS Combinatorial Science in 2011.SDS of cas: 86069-86-5 The following contents are mentioned in the article:

Cyclopeptide analogs of rapamycin and FK506 (“rapalogs”) such as I, containing a common FKBP-binding moiety and variable effector domains, are prepared in a combinatorial library by solid-phase peptide synthesis. FKBP12 binds to most of the rapamycin analogs with high affinity (K_i values in the nanomolar to low micromolar range), creating a large repertoire of composite surfaces for potential recognition of macromol. targets such as proteins. For example, I binds to FKBP with an IC₅₀ value of 2±1 μM (IC₅₀ value±SD), as compared to 57±2 nM for rapamycin and 220±80 nM for FK 506. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5SDS of cas: 86069-86-5).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N–H bond in an axial position, and the other in an equatorial position.SDS of cas: 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Creating Diverse Target-Binding Surfaces on FKBP12: Synthesis and Evaluation of a Rapamycin Analogue Library was written by Wu, Xiang-Hong;Wang, Li-Sheng;Han, Yao-Hua;Regan, Nicholas;Li, Pui-Kai;Villalona, Miguel A.;Hu, Xi-Che;Briesewitz, Roger;Pei, De-Hua. And the article was included in ACS Combinatorial Science in 2011.Reference of 86069-86-5 The following contents are mentioned in the article:

Cyclopeptide analogs of rapamycin and FK506 (“rapalogs”) such as I, containing a common FKBP-binding moiety and variable effector domains, are prepared in a combinatorial library by solid-phase peptide synthesis. FKBP12 binds to most of the rapamycin analogs with high affinity (K_i values in the nanomolar to low micromolar range), creating a large repertoire of composite surfaces for potential recognition of macromol. targets such as proteins. For example, I binds to FKBP with an IC₅₀ value of 2±1 μM (IC₅₀ value±SD), as compared to 57±2 nM for rapamycin and 220±80 nM for FK 506. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Reference of 86069-86-5).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N–H bond in an axial position, and the other in an equatorial position.Reference of 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Microsporins A and B: new histone deacetylase inhibitors from the marine-derived fungus Microsporum cf. gypseum and the solid-phase synthesis of microsporin A was written by Gu, Wenxin;Cueto, Mercedes;Jensen, Paul R.;Fenical, William;Silverman, Richard B.. And the article was included in Tetrahedron in 2007.Formula: C21H21NO4 The following contents are mentioned in the article:

Two new cyclic peptides, microsporins A (I) and B, were isolated from culture extracts of the marine-derived fungus Microsporum cf. gypseum obtained from a sample of the bryozoan Bugula sp. collected in the U.S. Virgin Islands. The structures of the new compounds were determined by extensive interpretation of 2D NMR data and by chem. methods. Microsporins A and B are potent inhibitors of histone deacetylase and demonstrate cytotoxic activity against human colon adenocarcinoma (HCT-116), as well as against the National Cancer Institute 60 cancer cell panel. The total synthesis of microsporin A on solid-phase is also reported. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Formula: C21H21NO4).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Formula: C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Microsporins A and B: new histone deacetylase inhibitors from the marine-derived fungus Microsporum cf. gypseum and the solid-phase synthesis of microsporin A was written by Gu, Wenxin;Cueto, Mercedes;Jensen, Paul R.;Fenical, William;Silverman, Richard B.. And the article was included in Tetrahedron in 2007.Recommanded Product: 86069-86-5 The following contents are mentioned in the article:

Two new cyclic peptides, microsporins A (I) and B, were isolated from culture extracts of the marine-derived fungus Microsporum cf. gypseum obtained from a sample of the bryozoan Bugula sp. collected in the U.S. Virgin Islands. The structures of the new compounds were determined by extensive interpretation of 2D NMR data and by chem. methods. Microsporins A and B are potent inhibitors of histone deacetylase and demonstrate cytotoxic activity against human colon adenocarcinoma (HCT-116), as well as against the National Cancer Institute 60 cancer cell panel. The total synthesis of microsporin A on solid-phase is also reported. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Recommanded Product: 86069-86-5).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Recommanded Product: 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Targeting a novel KRAS binding site: Application of one-component stapling of small (5-6-mer) peptides was written by Fumagalli, Gabriele;Carbajo, Rodrigo J.;Nissink, J. Willem M.;Tart, Jonathan;Dou, Rongxuan;Thomas, Andrew P.;Spring, David R.. And the article was included in Journal of Medicinal Chemistry in 2021.SDS of cas: 86069-86-5 The following contents are mentioned in the article:

RAS proteins are central in the proliferation of many types of cancer, but a general approach toward the identification of pan-mutant RAS inhibitors has remained unresolved. In this work, we describe the application of a binding pharmacophore identified from anal. of known RAS binding peptides to the design of novel peptides. Using a chem. divergent approach, we generated a library of small stapled peptides from which we identified compounds with weak binding activity. Exploration of structure-activity relationships (SARs) and optimization of these early compounds led to low-micromolar binders of KRAS that block nucleotide exchange. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5SDS of cas: 86069-86-5).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.SDS of cas: 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Targeting a novel KRAS binding site: Application of one-component stapling of small (5-6-mer) peptides was written by Fumagalli, Gabriele;Carbajo, Rodrigo J.;Nissink, J. Willem M.;Tart, Jonathan;Dou, Rongxuan;Thomas, Andrew P.;Spring, David R.. And the article was included in Journal of Medicinal Chemistry in 2021.Electric Literature of C21H21NO4 The following contents are mentioned in the article:

RAS proteins are central in the proliferation of many types of cancer, but a general approach toward the identification of pan-mutant RAS inhibitors has remained unresolved. In this work, we describe the application of a binding pharmacophore identified from anal. of known RAS binding peptides to the design of novel peptides. Using a chem. divergent approach, we generated a library of small stapled peptides from which we identified compounds with weak binding activity. Exploration of structure-activity relationships (SARs) and optimization of these early compounds led to low-micromolar binders of KRAS that block nucleotide exchange. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Electric Literature of C21H21NO4).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Electric Literature of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem