Synthesis of the lactone of 2-carboxy-4-hydroxy-7-methoxy-1, 2, 3, 4-tetrahydrophenanthrone

Starting from 6-methoxynaphthaldehyde-2, 2-carboxy-7-methoxy-1, 2, 3, 4-tetrahydrophenanthrone-4 was prepared. Sodium borohydride reduction of the keto-acid followed by chromic acid oxidation yielded the lactone of 2-carboxy-4-hydroxy-7-methoxy-1, 2, 3, 4-tetrahydrophenanthrone. Alkylation of the lactone of 2-carboxy-4-hydroxy-6-methoxytetralone was not promising.

Synthesis of cyclohexylideneacetaldehyde 2-, 3- and 4-methylcyclohexylideneacetaldehyde

Cyclohexanone and 2-, 3- and 4-methylcyclohexanones have been condensed with acetylene to give the respective 1-ethinylcyclohexanola. The 1-ethinylcyclohexanols were hydrogenated to the respective 1-vinyl- and 1-ethylcyclohexanols. The 1-vinylcyclohexanols have been treated with phosphorus tribromide to give the corresponding rearranged β-cyclohexylidenethyl bromides which have been converted to the pyridinium salts. The latter were treated with p-nitrosodimethylaniline and alkali (Krohnke's method) to give the corresponding nitrones which were hydrolyzed to the corresponding aldehydes. The 1-ethinyl-, 1-vinyl- and 1-ethylcyclohexanols prepared were subjected to pharmacological tests.

1-[2,4,6-Trimethyl-3,5-bis(4-oxopiperidin ylmethyl) benzyl ]piperidin- 4-one

In the structure of the title compound, C27H39N3O3, each of the (4-oxopiperidin-1-yl)methyl residues adopts a flattened chair conformation (with the N and carbonyl groups being oriented to either,side of the central C-4 plane) and they occupy positions approximatelym orthogonal to the central benzene ring [C-benzene-C-C-methylene-N torsion angles 103.4 (2), -104.4 (3) and 71.9 (3)degrees]; further, two of these residues are oriented to one side of the central benzene ring with the third to the other side. In the crystal packing, supramolecular layers in the ab plane are sustained by C-H center dotcenter dot center dot O interactions.

N-[4-Chloro-2-(2-chlorobenzoyl)phenyl]acetamide

In the title compound, C15H11Cl2NO2, the dihedral angle between the two benzene rings is 74.83 (5)degrees. The N-bound and terminal benzene rings are inclined at dihedral angles of 4.09 (10) and 78.38 (9) degrees, respectively, to the mean plane through the acetamide group.Intramolecular C-H center dot center dot center dot O and N-H center dot center dot center dot O hydrogen bonds both generate S(6) rings.

Methyl 1-methyl-1H-1,2,3-triazole-4-carboxylate

The title molecule, C5H7N3O2, has an almost planar conformation, with a maximum deviation of 0.043 (3) angstrom, except for the methyl H atoms. In the crystal structure, intermolecular C-H center dot center dot center dot O hydrogen bonds link the molecules into layers parallel to the bc plane. Intermolecular pi-pi stacking interactions [centroid-centroid distances = 3.685 (2) and 3.697 (2) angstrom] are observed between the parallel triazole rings.

Crystal And Molecular-Structure Of 8-Acetoxy-6-(2,4-Dimethoxy-5-Bromophenyl)-3-Methyl-Tricyclo[5,2,1,03,8 ]Decan-2-One

The crystal and molecular structure has been determined by the heavy-atom method and refined by the least-squares procedure to R= 8"3 % for 2033 photographically observed reflexions. The compound crystallizes in the space group P]" with two molecules in a unit cell of dimensions a = 11"68 + 0-02, b = 12"91 +0"02, c= 10"43+0"02/~, e= 114"7+ 1, fl=90-2+ 1 and 7,= 118.3+ 1 °. The unit cell also contains one molecule of the solvent, benzene. The 'cage' part of the molecule exhibits a large number of elongated bonds and strained internal valency angles. The bridgehead angle in the bicyclic heptane ring system is 89 °. The acetate group at C(16) and the methyl group at C(15) are cis to each other.

Role and function of nonmuscle alpha-actinin-1 and -4 in regulating distinct subcategories of actin stress fibers in mammalian cells

Actin stress fibers are dynamic structures in the cytoskeleton, which respond to mechanical stimuli and affect cell motility, adhesion and invasion of cancer cells. In nonmuscle cells, stress fibers have been subcategorized to three distinct stress fiber types: dorsal and ventral stress fibers and transverse arcs. These stress fibers are dissimilar in their subcellular localization, connection to substratum as well as in their dynamics and assembly mechanisms. Still uncharacterized is how they differ in their function and molecular composition. Here, I have studied involvement of nonmuscle alpha-actinin-1 and -4 in regulating distinct stress fibers as well as their localization and function in human U2OS osteosarcoma cells. Except for the correlation of upregulation of alpha-actinin-4 in invasive cancer types very little is known about whether these two actinins are redundant or have specific roles. The availability of highly specific alpha-actinin-1 antibody generated in the lab, revealed localization of alpha-actinin-1 along all three categories of stress fibers while alphaactinin-4 was detected at cell edge, distal ends of stress fibers as well as perinuclear regions. Strikingly, by utilizing RNAi-mediated gene silencing of alpha-actinin-1 resulted in specific loss of dorsal stress fibers and relocalization of alpha-actinin-4 to remaining transverse arcs and ventral stress fibers. Unexpectedly, aberrant migration was not detected in cells lacking alpha-actinin-1 even though focal adhesions were significantly smaller and fewer. Whereas, silencing of alpha-actinin-4 noticeably affected overall cell migration. In summary, as part of my master thesis study I have been able to demonstrate distinct localization and functional patterns for both alpha-actinin-1 and -4. I have identified alpha-actinin-1 to be a selective dorsal stress fiber crosslinking protein as well as to be required for focal adhesion maturation, while alpha-actinin-4 was demonstrated to be fundamental for cell migration.

Mandelic Acid 4-Hydroxylase - New Inducible Enzyme From Pseudomonas-Convexa

A soluble fraction of catalyzed the hydroxylation of mandelic acid to -hydroxymandelic acid. The enzyme had a pH optimum of 5.4 and showed an absolute requirement for Fe2+, tetrahydropteridine, NADPH. -Hydroxymandelate, the product of the enzyme reaction was identified by paper chromatography, thin layer chromatography, UV and IR-spectra

1,3,6-Trimethylpyrano[4,3-b]pyrrol-4(1H)-one

All the non-H atoms of the title compound, C10H11NO2, are almost coplanar [maximum deviation = 0.040 (3) angstrom]. The crystal structure is stabilized by C-H center dot center dot center dot O hydrogen bonds.

2-Chloro-8-methyl-3-[(pyrimidin-4-yloxy)methyl]quinoline

In the title compound, C15H12ClN3O, the quinoline ring system is essentially planar, with a maximum deviation of 0.017 (1) angstrom. The crystal packing is stabilized by pi-pi stacking interactions between the quinoline rings of adjacent molecule, with a centroid-centroid distance of 3.5913 (8) angstrom. Aweak C-H center dot center dot center dot pi contact is also observed between molecules.

5-(4-Chlorophenyl)-3-(2,4-dimethylthiazol-5-yl)-1,2,4-triazolo[3,4-a]isoquinoline

In the title molecule, C21H15ClN4S, the triazoloisoquinoline ring system is approximately planar, with an r.m.s. deviation of 0.054 (2) angstrom and a maximum deviation of 0.098 (2) angstrom from the mean plane for the triazole ring C atom that is bonded to the thiazole ring. The thiazole and benzene rings are twisted by 66.36 (7) and 56.32 (7)degrees respectively, with respect to the mean plane of the triazoloisoquinoline ring system. In the crystal structure, molecules are linked by intermolecular C-H center dot center dot center dot N interactions along the a axis. The molecular conformation is stabilized by a weak intramolecular pi-pi interaction involving the thiazole and benzene rings, with a centroid-centroid distance of 3.6546 (11) angstrom . In addition, two other intermolecular pi-pi stacking interactions are observed, between the triazole and benzene rings and between the dihydropyridine and benzene rings [centroid-centroid distances = 3.6489 (11) and 3.5967 (10) angstrom, respectively].