Tag: 300-400

Soluble epoxide hydrolase pharmacological inhibition ameliorates experimental acute pancreatitis in mice was written by Bettaieb, Ahmed;Chahed, Samah;Bachaalany, Santana;Griffey, Stephen;Hammock, Bruce D.;Haj, Fawaz G.. And the article was included in Molecular Pharmacology in 2015.Name: 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea The following contents are mentioned in the article:

Acute pancreatitis (AP) is an inflammatory disease, and is one of the most common gastrointestinal disorders worldwide. Soluble epoxide hydrolase (sEH; encoded by Ephx2) deficiency and pharmacol. inhibition have beneficial effects in inflammatory diseases. Ephx2 whole-body deficiency mitigates exptl. AP in mice, but the suitability of sEH pharmacol. inhibition for treating AP remains to be determined We investigated the effects of sEH pharmacol. inhibition on caerulein- and arginine-induced AP using the selective sEH inhibitor 1-trifluoromethoxyphenyl-3-(1-propionylpiperidin-4-yl) urea (TPPU), which was administered before and after induction of pancreatitis. Serum amylase and lipase levels were lower in TPPU-treated mice compared with controls. In addition, circulating levels and pancreatic mRNA of the inflammatory cytokines tumor necrosis factor-伪, interleukin Il-1尾, and Il-6 were reduced in TPPU-treated mice. Moreover, sEH pharmacol. inhibition before and after induction of pancreatitis was associated with decreased caerulein- and arginine-induced nuclear factor-魏B inflammatory response, endoplasmic reticulum stress, and cell death. sEH pharmacol. inhibition before and after induction of pancreatitis mitigated caerulein- and arginine-induced AP. This work suggests that sEH pharmacol. inhibition may be of therapeutic value in acute pancreatitis. This study involved multiple reactions and reactants, such as 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7Name: 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea).

1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Name: 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Deletion of soluble epoxide hydrolase suppressed chronic kidney disease-related vascular calcification by restoring Sirtuin 3 expression was written by He, Wanbing;Huang, Jieping;Liu, Yang;Xie, Changming;Zhang, Kun;Zhu, Xinhong;Chen, Jie;Huang, Hui. And the article was included in Cell Death & Disease in 2021.Formula: C16H20F3N3O3 The following contents are mentioned in the article:

Vascular calcification is common in chronic kidney disease (CKD) and contributes to cardiovascular disease (CVD) without any effective therapies available up to date. The expression of soluble epoxide hydrolase (sEH) is different in patients with and without vascular calcification. The present study investigates the role of sEH as a potential mediator of vascular calcification in CKD. Both Ephx2-/- and wild-type (WT) mice fed with high adenine and phosphate (AP) diet were used to explore the vascular calcification in CKD. Compared with WT, deletion of sEH inhibited vascular calcification induced by AP. sEH deletion also abolished high phosphorus (Pi)-induced phenotypic transition of vascular smooth muscle cells (VSMCs) independent of its epoxyeicosatrienoic acids (EETs) hydrolysis. Further gene expression anal. identified the potential role of Sirtuin 3 (Sirt3) in the sEH-regulated VSMC calcification. Under high Pi treatment, sEH interacted with Sirt3, which might destabilize Sirt3 and accelerate the degradation of Sirt3. Deletion of sEH may preserve the expression of Sirt3, and thus maintain the mitochondrial ATP (ATP) synthesis and morphol., significantly suppressing VSMC calcification. Our data supported that sEH deletion inhibited vascular calcification and indicated a promising target of sEH inhibition in vascular calcification prevention. This study involved multiple reactions and reactants, such as 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7Formula: C16H20F3N3O3).

1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7) 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. 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.Formula: C16H20F3N3O3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

c[D-pro-Pro-D-pro-N-methyl-Ala] adopts a rigid conformation that serves as a scaffold to mimic reverse-turns was written by Arbor, Sage;Kao, Jeff;Wu, Yun;Marshall, Garland R.. And the article was included in Biopolymers in 2008.Name: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid The following contents are mentioned in the article:

Naturally occurring cyclic tetrapeptides (CTPs) such as tentoxin, ampicidin, HC-toxin, and trapoxin have a wide range of biol. activity and potential use ranging from herbicides to therapeutics for malaria and cancer. To elucidate scaffolds that have few low-energy conformations and could serve as semirigid reverse-turn mimetics, the flexibility of CTPs was determined computationally. Four analogs of cyclic tetraproline c[Pro-pro-Pro-pro] with alternating L– and D-prolines, namely cyclic peptides c[pro-Pro-pro-NMe-Ala], c[pip-Pro-pip-Pro], c[pro-Pip-pro-Pro], and c[Ala-Pro-pip-Pro] were synthesized and characterized by NOESY NMR. Both mol. mechanics and D. Functional Theory quantum calculations found these head-to-tail CTPs to be constrained to one or two relatively stable conformations. NMR structures, while not always yielding the same lowest energy conformation as expected by in silico predictions, confirmed only one or two highly populated solution conformations for all four peptides examined Cyclic peptide c[pro-Pro-pro-NMe-Ala] was shown to have a single all trans-amide bond conformation from both in silico predictions and NMR characterization, and to be a reverse-turn mimetic by overlapping four C伪-C尾 bonds with those for 鈭?.5% of reverse-turns in the Protein Data Bank PDB with a RMSD of 0.57 脜. 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. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Name: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

c[D-pro-Pro-D-pro-N-methyl-Ala] adopts a rigid conformation that serves as a scaffold to mimic reverse-turns was written by Arbor, Sage;Kao, Jeff;Wu, Yun;Marshall, Garland R.. And the article was included in Biopolymers in 2008.Recommanded Product: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid The following contents are mentioned in the article:

Naturally occurring cyclic tetrapeptides (CTPs) such as tentoxin, ampicidin, HC-toxin, and trapoxin have a wide range of biol. activity and potential use ranging from herbicides to therapeutics for malaria and cancer. To elucidate scaffolds that have few low-energy conformations and could serve as semirigid reverse-turn mimetics, the flexibility of CTPs was determined computationally. Four analogs of cyclic tetraproline c[Pro-pro-Pro-pro] with alternating L– and D-prolines, namely cyclic peptides c[pro-Pro-pro-NMe-Ala], c[pip-Pro-pip-Pro], c[pro-Pip-pro-Pro], and c[Ala-Pro-pip-Pro] were synthesized and characterized by NOESY NMR. Both mol. mechanics and D. Functional Theory quantum calculations found these head-to-tail CTPs to be constrained to one or two relatively stable conformations. NMR structures, while not always yielding the same lowest energy conformation as expected by in silico predictions, confirmed only one or two highly populated solution conformations for all four peptides examined Cyclic peptide c[pro-Pro-pro-NMe-Ala] was shown to have a single all trans-amide bond conformation from both in silico predictions and NMR characterization, and to be a reverse-turn mimetic by overlapping four C伪-C尾 bonds with those for 鈭?.5% of reverse-turns in the Protein Data Bank PDB with a RMSD of 0.57 脜. 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: (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 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.Recommanded Product: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthesis and Conformational Analysis of Efrapeptins was written by Weigelt, Sven;Huber, Thomas;Hofmann, Frank;Jost, Micha;Ritzefeld, Markus;Luy, Burkhard;Freudenberger, Christoph;Majer, Zsuzsanna;Vass, Elemer;Greie, Joerg-Christian;Panella, Lavinia;Kaptein, Bernard;Broxterman, Quirinus B.;Kessler, Horst;Altendorf, Karlheinz;Hollosi, Miklos;Sewald, Norbert. And the article was included in Chemistry – A European Journal in 2012.Reference of 86069-86-5 The following contents are mentioned in the article:

The efrapeptin family of peptide antibiotics produced by the fungus Tolypocladium niveum, and the neo-efrapeptins from the fungus Geotrichum candidum are inhibitors of F₁-ATPase with promising antitumor, antimalaria, and insecticidal activity. They are rich in C^伪-dialkyl amino acids (Aib, Iva, Acc) and contain one 尾-alanine and several pipecolic acid residues. The C-terminus bears an unusual heterocyclic cationic cap. The efrapeptins C-G and three analogs of efrapeptin C were synthesized using 伪-azido carboxylic acids as masked amino acid derivatives All compounds display inhibitory activity toward F₁-ATPase. The conformation in solution of the peptides was investigated with electronic CD spectroscopy, FT-IR spectroscopy, and VCD spectroscopy. All efrapeptins and most efrapeptin analogs were shown to adopt helical conformations in solution In the case of efrapeptin C, VCD spectra proved that a 3₁₀-helix prevails. In addition, efrapeptin C was conformationally studied in detail with NMR and mol. modeling. Besides NOE distance restraints, residual dipolar couplings (RDC) observed upon partial alignment with stretched PDMS gels were used for the conformational anal. and confirmed the 3₁₀-helical conformation. Safety: caution is advised with low-mol.-weight azido compounds 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 has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. 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.Reference of 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthesis and Conformational Analysis of Efrapeptins was written by Weigelt, Sven;Huber, Thomas;Hofmann, Frank;Jost, Micha;Ritzefeld, Markus;Luy, Burkhard;Freudenberger, Christoph;Majer, Zsuzsanna;Vass, Elemer;Greie, Joerg-Christian;Panella, Lavinia;Kaptein, Bernard;Broxterman, Quirinus B.;Kessler, Horst;Altendorf, Karlheinz;Hollosi, Miklos;Sewald, Norbert. And the article was included in Chemistry – A European Journal in 2012.Synthetic Route of C21H21NO4 The following contents are mentioned in the article:

The efrapeptin family of peptide antibiotics produced by the fungus Tolypocladium niveum, and the neo-efrapeptins from the fungus Geotrichum candidum are inhibitors of F₁-ATPase with promising antitumor, antimalaria, and insecticidal activity. They are rich in C^伪-dialkyl amino acids (Aib, Iva, Acc) and contain one 尾-alanine and several pipecolic acid residues. The C-terminus bears an unusual heterocyclic cationic cap. The efrapeptins C-G and three analogs of efrapeptin C were synthesized using 伪-azido carboxylic acids as masked amino acid derivatives All compounds display inhibitory activity toward F₁-ATPase. The conformation in solution of the peptides was investigated with electronic CD spectroscopy, FT-IR spectroscopy, and VCD spectroscopy. All efrapeptins and most efrapeptin analogs were shown to adopt helical conformations in solution In the case of efrapeptin C, VCD spectra proved that a 3₁₀-helix prevails. In addition, efrapeptin C was conformationally studied in detail with NMR and mol. modeling. Besides NOE distance restraints, residual dipolar couplings (RDC) observed upon partial alignment with stretched PDMS gels were used for the conformational anal. and confirmed the 3₁₀-helical conformation. Safety: caution is advised with low-mol.-weight azido compounds This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Synthetic Route 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. 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.Synthetic Route of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Investigation of the Binding Determinants of Phosphopeptides Targeted to the Src Homology 2 Domain of the Signal Transducer and Activator of Transcription 3. Development of a High-Affinity Peptide Inhibitor was written by Coleman, David R.;Ren, Zhiyong;Mandal, Pijus K.;Cameron, Arlin G.;Dyer, Garrett A.;Muranjan, Seema;Campbell, Martin;Chen, Xiaomin;McMurray, John S.. And the article was included in Journal of Medicinal Chemistry in 2005.COA of Formula: C21H21NO4 The following contents are mentioned in the article:

As part of their research on the design of Src homol. 2 (SH2) directed peptidomimetic inhibitors of Stat3, the authors, here, describe structure-activity relationship studies that provide information on the nature of peptide-protein interactions of a high-affinity phosphopeptide, Ac-Tyr(PO₃H₂)-Leu-Pro-Gln-Thr-Val-NH₂ (peptide 1), inhibitor of Stat3 dimerization and DNA binding. There is a hydrophobic surface on the SH2 domain that can accommodate lipophilic groups on the N-terminus. Of the amino acids tested, leucine provided the highest affinity at pY+1 and its main chain NH is involved with a hydrogen bond with Stat3, presumably Ser636. Cis-3,4-Methanoproline is optimal as a backbone constraint at pY+2. The side chain amide protons of Gln are required for high-affinity interactions. The C-terminal dipeptide, Thr-Val, can be replaced with groups ranging in size from Me to benzyl. The authors synthesized a phosphopeptide incorporating groups that provided increases in affinity at each position. Thus, Ph(CH₂)₂CO-Tyr(PO₃H₂)-Leu-cis-3,4-methanoPro-Gln-NHCH₂Ph was the highest affinity peptide, exhibiting an IC₅₀ of 125 nM vs. 290 nM for peptide 1 in a fluorescence polarization assay. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5COA of Formula: C21H21NO4).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. 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.COA of Formula: C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Investigation of the Binding Determinants of Phosphopeptides Targeted to the Src Homology 2 Domain of the Signal Transducer and Activator of Transcription 3. Development of a High-Affinity Peptide Inhibitor was written by Coleman, David R.;Ren, Zhiyong;Mandal, Pijus K.;Cameron, Arlin G.;Dyer, Garrett A.;Muranjan, Seema;Campbell, Martin;Chen, Xiaomin;McMurray, John S.. And the article was included in Journal of Medicinal Chemistry in 2005.Application In Synthesis of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid The following contents are mentioned in the article:

As part of their research on the design of Src homol. 2 (SH2) directed peptidomimetic inhibitors of Stat3, the authors, here, describe structure-activity relationship studies that provide information on the nature of peptide-protein interactions of a high-affinity phosphopeptide, Ac-Tyr(PO₃H₂)-Leu-Pro-Gln-Thr-Val-NH₂ (peptide 1), inhibitor of Stat3 dimerization and DNA binding. There is a hydrophobic surface on the SH2 domain that can accommodate lipophilic groups on the N-terminus. Of the amino acids tested, leucine provided the highest affinity at pY+1 and its main chain NH is involved with a hydrogen bond with Stat3, presumably Ser636. Cis-3,4-Methanoproline is optimal as a backbone constraint at pY+2. The side chain amide protons of Gln are required for high-affinity interactions. The C-terminal dipeptide, Thr-Val, can be replaced with groups ranging in size from Me to benzyl. The authors synthesized a phosphopeptide incorporating groups that provided increases in affinity at each position. Thus, Ph(CH₂)₂CO-Tyr(PO₃H₂)-Leu-cis-3,4-methanoPro-Gln-NHCH₂Ph was the highest affinity peptide, exhibiting an IC₅₀ of 125 nM vs. 290 nM for peptide 1 in a fluorescence polarization assay. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Application In Synthesis of (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 saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. 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.Application In Synthesis of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Solid-phase synthesis of libraries of ethynylated aminosteroid derivatives as potential antileukemic agents was written by Talbot, Amelie;Maltais, Rene;Kenmogne, Lucie Carolle;Roy, Jenny;Poirier, Donald. And the article was included in Steroids in 2016.Application In Synthesis of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid The following contents are mentioned in the article:

Steroids possessing an ethynyl group at position 17伪 (tertiary alcs.) are well known to be more stable than their non-ethynyl analogs (secondary alcs.). To facilitate the development of new drugs with better metabolic stability, we developed a new diethylsilyl acetylenic linker allowing us to rapidly synthesize libraries of ethynylated steroid derivatives using a solid-phase strategy. To illustrate its usefulness, this linker was used to expand the mol. diversity of a lead compound having a hydroxy acetylenic pattern and to potentially find new compounds with interesting cytotoxic activity against leukemia cell lines. Herein, we report the chem. synthesis and the characterization of three libraries of ethynylated aminosteroid derivatives using the diethylacetylenic linker. We discuss their antiproliferative activities obtained in 2 leukemia cell lines (HL-60 and Jurkat), which results provided new structure-activity relationships. We also identified a new promising aminosteroid derivative with an azetidine moiety, compound I, inhibiting 60% and 75% of HL-60 and Jurkat cell proliferation, resp., at 1 渭M. More generally, these results validate the use of a diethylsilyl acetylenic linker for researchers interested in generating libraries of alc. derivatives with better stability and drug profile. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Application In Synthesis of (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 metabolite of cadaverine, a polyamine found in the human intestine. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N鈥揌 bond in an axial position, and the other in an equatorial position.Application In Synthesis of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Solid-phase synthesis of libraries of ethynylated aminosteroid derivatives as potential antileukemic agents was written by Talbot, Amelie;Maltais, Rene;Kenmogne, Lucie Carolle;Roy, Jenny;Poirier, Donald. And the article was included in Steroids in 2016.Related Products of 86069-86-5 The following contents are mentioned in the article:

Steroids possessing an ethynyl group at position 17伪 (tertiary alcs.) are well known to be more stable than their non-ethynyl analogs (secondary alcs.). To facilitate the development of new drugs with better metabolic stability, we developed a new diethylsilyl acetylenic linker allowing us to rapidly synthesize libraries of ethynylated steroid derivatives using a solid-phase strategy. To illustrate its usefulness, this linker was used to expand the mol. diversity of a lead compound having a hydroxy acetylenic pattern and to potentially find new compounds with interesting cytotoxic activity against leukemia cell lines. Herein, we report the chem. synthesis and the characterization of three libraries of ethynylated aminosteroid derivatives using the diethylacetylenic linker. We discuss their antiproliferative activities obtained in 2 leukemia cell lines (HL-60 and Jurkat), which results provided new structure-activity relationships. We also identified a new promising aminosteroid derivative with an azetidine moiety, compound I, inhibiting 60% and 75% of HL-60 and Jurkat cell proliferation, resp., at 1 渭M. More generally, these results validate the use of a diethylsilyl acetylenic linker for researchers interested in generating libraries of alc. derivatives with better stability and drug profile. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Related Products 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. 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.Related Products of 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem