- Synthesis, characterization and biological activity of copper(II) complexes with ligands derived from β-amino acids
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Two copper(II) complexes with ligands derived from β-amino acids, 2-(1-aminocyclohexyl)acetic acid L1 and 2-(1-amino-4-(tert-butyl)cyclohexyl)acetic acid L2, were synthesized and characterized by microanalysis, infrared, UV–Vis and EPR spectra. The spectr
- Bukonji?, Andriana M.,Tomovi?, Du?an Lj.,Stankovi?, Ana S.,Jevti?, Verica V.,Ratkovi?, Zoran R.,Bogojeski, Jovana V.,Milovanovi?, Jelena Z.,?or?evi?, Dragana B.,Arsenijevi?, Aleksandar N.,Milovanovi?, Marija Z.,Poto?ňák, Ivan,Trifunovi?, Sre?ko R.,Radi?, Gordana P.
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- C11/C9 Helical Folding in αβ Hybrid Peptides Containing 1-Amino-cyclohexane acetic acid (β3, 3-Ac6c)
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The present study describes the solid-state conformation of αβ hybrid peptides, Boc-Leu-β3, 3-Ac6c-OH, P1; Boc-Leu-β3, 3-Ac6c-Leu-β3, 3-Ac6c-OMe, P2; and Boc-Leu-β3, 3-Ac6c-Leu-β3, 3-Ac6c-Leu-OMe, P3. The dipeptide P1 adopts extended conformations, whereas tetrapeptide P2 and pentapeptide P3 favor a helical conformation stabilized by mixed types of C11/C9 intramolecular hydrogen bonds. In peptide P3, the amino group of β3, 3-Ac6c(2) and β3, 3-Ac6c(4) residues occupies axial orientation, whereas in P2 it occupies axial and equatorial orientations for residues β3, 3-Ac6c(2) and β3, 3-Ac6c(4), respectively. The self-assembly of P3 forms channels filled with solvent molecules that present interesting patterns.
- Wani, Naiem Ahmad,Raghothama, Srinivasarao,Singh, Umesh Prasad,Rai, Rajkishor
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- CYCLIN-DEPENDENT KINASE INHIBITING COMPOUNDS FOR THE TREATMENT OF MEDICAL DISORDERS
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This invention is in the area of cell cycle inhibiting compounds for the treatment of disorders involving abnormal cellular proliferation, and include selective CDK2 inhibitors for medical therapy and their pharmaceutically acceptable salts and compositions.
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Page/Page column 172; 192
(2021/11/26)
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- Inhibition of Invasion in Pancreatic Cancer Cells by Conjugate of EPA with β3,3-Pip-OH via PI3K/Akt/NF-kB Pathway
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The present work describes the anti-invasive effect of conjugate BC06, a novel conjugate of EPA, (2E,4E)-4-(benzo[d][1,3]dioxol-5-ylmethylene) hex-2-enoic acid with β,β-disubstituted-β-amino acid, β3,3-Pip-OH (2-(4-aminopiperidin-4-yl)acetic acid), in human pancreatic carcinoma. The conjugate BC06 inhibited invasion and migration of PANC-1 cells in wound healing, matrigel invasion, and gelatin degradation assays. Apart from suppressing PI3K/Akt/NF-kB signaling, which is involved in the up-regulation of matrix metalloproteinases, our study also demonstrated that dose-dependent treatment of BC06 results in the upregulation of TIMP-1 and E-cadherin expression. Further, BC06 was found to be inhibiting the metastatic ability of PANC-1 cells by reducing MMP-2 and MMP-9 expression. These findings suggest that EPA conjugate with β3,3-Pip-OH, BC06, may be used as an anti-invasive agent against human pancreatic carcinoma.
- Amin, Hina,Wani, Naiem Ahmad,Farooq, Saleem,Nayak, Debasis,Chakraborty, Souneek,Shankar, Sudha,Rasool, Reyaz Ur,Koul, Surinder,Goswami, Anindya,Rai, Rajkishor
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supporting information
p. 1071 - 1074
(2015/10/20)
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- Competitive formation of β-amino acids, propenoic, and ylidenemalonic acids by the Rodionov reaction from malonic acid, aldehydes, and ammonium acetate in alcoholic medium
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The Rodionov reaction of 49 available aliphatic and aromatic aldehydes with malonic acid and ammonium acetate in alcoholic medium, resulting in formation of β-amino acids, propenoic, and ylidenemalonic acids, was studied. Certain regioselectivity regularities of the reaction were revealed. Among the variety of ketones studied, cyclohexanone is the only whose reaction yields a β-amino acid. Unusual dehydrofluorination of 6-chloro-2-fluorocinnamic acid under the Rodionov reaction was discovered. 2005 Pleiades Publishing, Inc.
- Lebedev,Lebedeva,Sheludyakov,Kovaleva,Ustinova,Kozhevnikov
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p. 1113 - 1124
(2007/10/03)
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- β-Aminopenicillins, salts and esters
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β-Aminopenicillins, Salts and Esters are described having a wide spectrum of activity against Gram-positive and Gram-negative organisms. The β-aminopenicillins are derivatives of 6-amino-penicillanic acid and the procedure for preparing the β-aminopenicillins is set forth. β-aminopenicillins are characterized by having in the 6-position side chain a cycloalkyl ring of 5 - 7 carbon atoms particularly cyclopentyl, cyclohexyl or cycloheptyl.
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