- Synthesis of tris-tertiary amine CycloTriVeratrilene (TACTV) derivatives as water soluble pre-organized three aromatic ring containing molecular scaffolds for the construction of protein mimics
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The synthesis of water soluble highly pre-organized Tris-tertiary Amine CycloTriVeratrilene (TACTV) derivatives was developed. A semi-orthogonally protected derivative allowed one pot sequential introduction of different peptide loops toward the molecular construction of synthetic antibody protein mimics.
- Longin, Ond?ej,van de Langemheen, Helmus,Gannon, Susan,Ward, David,Liskamp, Rob M.J.
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- Bifunctional Fluoroalcohol Catalysts Enabled Sustainable Synthesis of Poly(amino acid)s?
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A series of novel bifunctional single-molecule hydrogen-bonding organocatalysts based on fluorinated tertiary alcohol were synthesized to mediate the metal-free polymerization of α-amino acid N-carboxyanhydride (NCA) monomer. Through the screening of catalysts, the polymerization catalyzed by the preferred bifunctional fluoroalcohol catalyst proceeded in a fast and controlled manner, affording high molecular weight polypeptide up to 35.2 × 104 Da with relatively narrow molecular weight distribution (? 1.20). A phenomenon of self-accelerating effect of polymerization induced by α-helical structure of polypeptides was observed, and a possible polymerization pathway has been discussed.
- He, Wenjing,Tao, Youhua
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- Design, synthesis and biological evaluation of novel 4-alkynyl-quinoline derivatives as PI3K/mTOR dual inhibitors
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Abstract A novel series of 4-alkynyl-quinoline derivatives were designed, synthesized and biologically evaluated for their PI3Kα inhibitory activities and anti-proliferative effects against two cancer cell lines PC-3 and HCT-116. Most of them showed potent PI3Kα inhibitory activities with IC50 values at low nanomolar level and good to excellent anti-proliferative effects against both cell lines. Among them, compound 15d, the most potent one, was selected for further biological evaluation. As a result, 15d displayed strong inhibitory activity against other class I PI3K isoforms (PI3Kβ, PI3Kγ and PI3Kδ) and mTOR with an acceptable kinase selectivity profile. Moreover, the western blot assay indicated that the phosphorylation of Akt, another downstream effector of PI3K, can be remarkably suppressed by 15d at cellular level. All these experimental results suggested that 15d is a potent PI3K/mTOR dual inhibitor and could serve as a promising lead compound for the development of anticancer agents.
- Lv, Xiaoqing,Ying, Huazhou,Ma, Xiaodong,Qiu, Ni,Wu, Peng,Yang, Bo,Hu, Yongzhou
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- Synthesis and preliminary evaluation steroidal antiestrogen-geldanamycin conjugates
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Three novel steroidal antiestrogen-geldanamycin conjugates were prepared using a convergent strategy. The antiestrogenic component utilized the 11β-(4-functionalized-oxyphenyl) estradiol scaffold, while the geldanamycin component was derived by replacement of the 17-methoxy group with an appropriately functionalized amine. Ligation was achieved in high yield using azide alkyne cyclization reactions. Evaluation of the products against two breast cancer cell lines indicated that the conjugates retained significant antiproliferative activity.
- Adam Hendricks,Hanson, Robert N.,Amolins, Michael,Mihelcic, John M.,Blagg, Brian S.
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supporting information
p. 3635 - 3639
(2013/07/19)
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- Clickosomes - Using triazole-linked phospholipid connectors to fuse vesicles
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Two complementary artificial diether phospholipids were synthesized that can undergo a Cu(i)-catalyzed Huisgen-Sharpless click reaction. The resulting lipid can bridge the membranes of large unilamellar vesicles and cause their aggregation and ultimately their fusion.
- Loosli, Frederic,Doval, David Alonso,Grassi, David,Zaffalon, Pierre-Leonard,Favarger, France,Zumbuehl, Andreas
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supporting information; experimental part
p. 1604 - 1606
(2012/03/11)
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- Modifications of C-2 on the pyrroloquinoline template aimed at the development of potent herpesvirus antivirals with improved aqueous solubility
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A series of C-2 pyrroloquinoline analogs designed to improve aqueous solubility were examined for herpesvirus polymerase and antiviral activity. Several analogs were identified that maintained the antiviral activity of the previous development candidate against HCMV, HSV-1 and VZV, but with significantly improved aqueous solubility.
- Nieman, James A.,Nair, Sajiv K.,Heasley, Steven E.,Schultz, Brenda L.,Zerth, Herbert M.,Nugent, Richard A.,Chen, Ke,Stephanski, Kevin J.,Hopkins, Todd A.,Knechtel, Mary L.,Oien, Nancee L.,Wieber, Janet L.,Wathen, Michael W.
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supporting information; experimental part
p. 3039 - 3042
(2010/07/03)
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- STEROIDAL ANTI-HORMONE HYBRIDS
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Disclosed are novel compounds and compositions for inhibition of androgen and estrogen receptor signaling, methods for inhibiting androgen signaling, methods for inhibiting estrogen signaling, methods for inhibiting the interaction between a co-regulatory protein and an androgen or estrogen receptor, and methods for treating cancer.
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Page/Page column 73
(2010/08/08)
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- BIFUNCTIONAL HETEROCYCLIC COMPOUNDS AND METHODS OF MAKING AND USING SAME
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The invention provides a family of bifunctional heterocyclic compounds useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. The invention also provides methods of making the bifunctional hetercyclic compounds, and methods of using such compounds as anti-infective, anti-proliferative agents, anti-inflammatory, and/or prokinetic agents.
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Page/Page column 215; 216
(2010/02/06)
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- Nickel-catalyzed heterocycle construction with stereoselective exocyclic alkene introduction
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A series of monocyclic and bicyclic heterocycles with exocyclic alkenes were constructed in a stereoselective fashion by an organozinc/Ni(COD)2 - mediated cyclization of alkynyl enones. Both reductive and alkylative cyclization manifolds were accessible depending on the ligand and organozinc structure. Alkylative cyclizations were generally more efficient than reductive cyclizations, particularly with cyclic substrates.
- Montgomery, John,Chevliakov, Maxim V.,Brielmann, Harry L.
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p. 16449 - 16462
(2007/10/03)
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