451472-23-4Relevant academic research and scientific papers
Enantioselective Comlexation with a Conformationally Homogeneous C2 Podand Ionophore
Iimori, Takamasa,Erickson, Shawn D.,Rheingold, Arnold L.,Still, W. Clark
, p. 6947 - 6950 (1989)
The podand tetraether 1b has been prepared from (+)-diethyl tartarate.This ionophore is expected to have only one significantly populated conformation.It binds a variety of chiral organic ammonium cations with enantioselectivities corresponding to 34-42pe
COPOLYMERS OF FORMULA (I) AND USES
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Paragraph 0119-0121, (2017/04/11)
Disclosed is a copolymer of following formula (I): in which:—x is an integer between 10 and 250, preferably between 40 and 120, —y is an integer between 4 and 100, preferably between 10 and 100, preferably between 19 and 60, —z is an integer between 0 and
Development of diacyltetrol lipids as activators for the C1 domain of protein kinase C
Mamidi, Narsimha,Gorai, Sukhamoy,Mukherjee, Rakesh,Manna, Debasis
experimental part, p. 1275 - 1285 (2012/06/04)
The protein kinase C (PKC) family of serine/threonine kinases is an attractive drug target for the treatment of cancer and other diseases. Diacylglycerol (DAG), phorbol esters and others act as ligands for the C1 domain of PKC isoforms. Inspection of the crystal structure of the PKCδ C1b subdomain in complex with phorbol-13-O-acetate shows that one carbonyl group and two hydroxyl groups play pivotal roles in recognition of the C1 domain. To understand the importance of two hydroxyl groups of phorbol esters in PKC binding and to develop effective PKC activators, we synthesized DAG like diacyltetrols (DATs) and studied binding affinities with C1b subdomains of PKCδ and PKC. DATs, with the stereochemistry of natural DAGs at the sn-2 position, were synthesized from (+)-diethyl l-tartrate in four to seven steps as single isomers. The calculated EC50 values for the short and long chain DATs varied in the range of 3-6 μM. Furthermore, the fluorescence anisotropy values of the proteins were increased in the presence of DATs in a similar manner to that of DAGs. Molecular docking of DATs (1b-4b) with PKCδ C1b showed that the DATs form hydrogen bonds with the polar residues and backbone of the protein, at the same binding site, as that of DAG and phorbol esters. Our findings reveal that DATs represent an attractive group of C1 domain ligands that can be used as research tools or further structurally modified for potential drug development.
Synthesis and spectroscopic correlation of the diastereoisomers of 2,3-dihydroxy-2,6,8-trimethyldeca-(4Z,6E)-dienoic acid: implications for the structures of papuamides A-D and mirabamides A-D
Ramamoorthy, Gurusankar,Acevedo, Cristina M.,Alvira, Edgardo,Lipton, Mark A.
experimental part, p. 2546 - 2554 (2009/04/11)
All 4 diastereomeric possibilities for the 2,3-dihydroxy-2,6,8-trimethyldeca-(4Z,6E)-dienoic acid (Dhtda) residue, found in the cyclic depsipeptide natural products papuamides A-D and mirabamides A-D, were stereoselectively synthesized using a Z-selective
Enantioselective complexation of organic ammonium ions by simple tetracyclic podand ionophores
Wang, Xuebao,Erickson, Shawn D.,Iimori, Takamasa,Clark Still
, p. 4128 - 4137 (2007/10/02)
A series of enantiomerically pure, C2-symmetric tetracyclic podands are synthesized and studied. These host molecules have methyl substitution, which allows only a few low-energy conformations, and they form well-defined complexes with chiral a
