IN THE TITLE COMPOUND (SYSTEMATIC NAME 8-chloro-11-{1-[(5-methyl-pyridin-3-yl)meth-yl]piperidin-4-yl-idene}-6,11-di-hydro-5H-benzo[5,6]cyclo-hepta-[1,2-b]pyridine), C26H26ClN3, the dihedral angle between the mean planes of the chloro-phenyl and cyclo-hepta-[1,2-b]pyridinyl rings fused to the cyclo-heptane ring is 56.6 (1)°. The mean planes of the cyclo-hepta-[1,2-b]pyridinyl and 5-methyl-pyridi...

OBJECTIVE(S) Inhibitors of p38 MAP kinase are considered as suitable target in the treatment of inflammatory diseases such as rheumatoid arthritis and bowel inflammatory diseases. The development of 5-alkylthio-1-aryl-2-(4-pyridinyl) triazoles as inhibitors of p38 MAP kinase is described. These are analogues of 4- pyridinyl imidazole p38 MAP kinase inhibitor reported by Merck Research Laborator...

Modified nucleosides in natural RNA molecules are essential for their functions. Non-natural nucleoside analogues have been introduced into RNA to manipulate its structure and function. We have recently developed a new strategy for the in situ modification of RNA based on the functionality transfer reaction between an oligodeoxynucleotide probe and an RNA substrate. 2'-Deoxy-6-thioguanosine (6-...

A series of N-(substituted pyridinyl)-1-methyl(phenyl)-3-trifluoromethyl-1H-pyrazole-4-carboxamide derivatives were synthesized. All target compounds were characterized by spectral data (¹H-NMR, ¹³C-NMR, IR, MS) and elemental analysis and were bioassayed in vitro against three kinds of phytopathogenic fungi (Gibberella zeae, Fusarium oxysporum, Cytospora mandshurica). The results showed that so...

The acid-catalyzed cyclocondensation in refluxing acetonitrile of aqueous glyoxal with N-heteroaryl-N'-phenylureas 4a-f (heteroaryl = 2-thiazolyl, 2-pyrimidinyl,2-pyrazinyl, 2-pyridinyl, 3-pyridinyl and 2-benzimidazolyl) led to the formation of the corresponding 1-heteroaryl-3-phenyl-4,5-dihydroxy-2-imidazolidinones 5a-f. All the products were characterized by elemental and spectroscopic analys...

Highly expressed high mobility group box-1 protein (HMGB1) promotes tumor metastasis. Whether HMGB1 participates in breast cancer cell activation of fibroblasts is unknown. The culture medium 6 lines with different migration potential, and overexpression or knockdown was used to induce fibroblast activation, collagen α-SMA expression were measured. We evaluated the potential MDA-MB-231 cells tr...

Background In human cancers, loss of PTEN, stabilization of hypoxia inducible factor-1a, and activation of Ras and AKT converge to increase the activity of a regulator of glycolysis, 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase (PFKFB3). This enzyme synthesizes fructose-2,6-bisphosphate (F2,6BP), which is an activator of 6-phosphofructo1-kinase, a key step of glycolysis that is tightly ...

The C–H activation by Pd(II) and Pt(II) compounds of a wide range imines related to 2-pyridinecarboxaldehyde, ArCH═NCH2(CH2)nPh (Ar = 2-pyridinyl, 2-picolinyl, 2-quinolinyl, n 0, 1), which can...

In the centrosymmetric title compound, C(18)H(16)N(6)O(2)S(2), the 1,3,4-oxadiazole and the attached pyridinyl ring are twisted by 5.3 (3)°.

In human cancers, loss of PTEN, stabilization of hypoxia inducible factor-1α, and activation of Ras and AKT converge to increase the activity of a key regulator of glycolysis, 6-phosphofructo-2-kinase (PFKFB3). This enzyme synthesizes fructose 2,6-bisphosphate (F26BP), which is an activator of 6-phosphofructo-1-kinase, a key step of glycolysis. Previously, a weak competitive inhibitor of PFKFB3...