Stereoselective transformation of Baylis-Hillman acetates 1 into corresponding (Z)-allyl iodides 2 has been achieved by treatment of 1 with samarium triiodide in THF. Remarkable rate acceleration of samarium triiodide-mediated iodination of 1 was found when ionic liquid 1-n-butyl-3-methyl-imidazolium tetrafluroborate ([bmim]BF(4)) was used as reaction media in stead of THF. This novel approach proceeds readily at 50 degrees C within a few minutes to afford (Z)-allyl iodides 2 in excellent yields. A mechanism involving stereoselective iodination of the acetates of Baylis-Hillman adducts by samarium triiodide is described, in which a six-membered ring transition state played a key role in the stereoselective formation of 2.
Acetates ; chemistry ; Iodides ; chemical synthesis ; Ions ; Kinetics ; Samarium ; chemistry ; Solutions

In order to investigate various physical and biological properties of dental magnetic attachments studies on retentive characteristics, corrosion properties, cytotoxicity of different magnetic systems for dental applications were done. For the study of retentive characteristics changes of retentive force by increasing air gap, wear properties of various attachment systems and loss of magnetic force by heat treatment were measured. For the study of corrosion property of magnet covering metal electrochemical corrosion was done in artificial saliva and 0.9% NaCl solution between -1,000 mVSCE and +1,000 mVSCE. Anodic polarization curves are obtained about 6 types of samples and 2 types of solution. Corroded surfaces were examined with metallurgical microscope, scanning electron microscope and surface profilometer. For the study of cytotoxicity of magnetic attachment and its field cell growth and agar overlay test were done. The results of this study were as follows. 1.In Magnetic attachments using closed circuit retentive force at zero air gap was greater than magnets using open circuit, but decrease of retentive force by increasing air gap was also greater than open systems. 2.After 40,000 cycles of wear test all mechanical attachment resulted in varing degree of retention loss but in magnetic attachments no loss of retentive force was observed. 3.The magnetic attachment using Neodymium magnet showed early loss of retentive force about 200degrees C but attachment using Samarium magnet showed some resistance to heat treatment and complete retention loss was observed about 500degrees C. The keeper was not influenced by heat treatment in retention. 4.In electrochemical corrosion test Dyna magnetic attachment covering metal showed the highiest corrosion resistance and Shiner magnet covering metal showed the least corrosion resistance and examination of corroded surface with metallurgical microscope, scanning electron microscope and surface profilometer also showed same results with anodic polarization curves. 5.The result of cell culture tests on the magnet covered with metal showed least recognizable cytotoxicity.
Agar ; Cell Culture Techniques ; Corrosion ; Cyprinidae ; Hot Temperature ; Neodymium ; Population Characteristics* ; Saliva, Artificial ; Samarium

Amides can be obtained in good to excellent yield by Sm/TiCl(4) mediated reductive cleavage of N=N bond in azo compounds and successive acylation in one pot. It offers an alternative method for the synthesis of amides from very simple starting materials directly.
Azo Compounds ; chemistry ; Chlorine Compounds ; chemistry ; Combinatorial Chemistry Techniques ; methods ; Halogens ; chemistry ; Samarium ; chemistry ; Titanium ; chemistry

AIMTo study the biochemistry of lanthanides, the cooperative action of inorganic and organic anti-tumor drugs.

METHODSA series of rare earth complexes were synthesized with Ln(NO3) 6H2O, Phen and 5-Fu. Their anti-tumor activity was measured by the improved MTT, SRB methods.

RESULTSThe formula of complex Ln[(Phen)2(5-Fu)3(NO3)](NO3)2(Ln = Y, La, Ce, Sm, Gd, Dy, Er; Phen = 1, 10-phenanthroline; 5-Fu = fluorouracil) was characterized by elemental analyses, molar conductivity, IR, TGA, and 13C NMR spectra. The preliminary biological activity studies indicated that Lanthanide complex has strong anti-tumor activity in vitro.

CONCLUSIONThe complex might have anti-tumor cooperation action.

Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Cerium ; chemistry ; Drug Synergism ; Dysprosium ; chemistry ; Erbium ; chemistry ; Fluorouracil ; chemistry ; Gadolinium ; chemistry ; Humans ; Lanthanoid Series Elements ; chemistry ; Lanthanum ; chemistry ; Phenanthrolines ; chemistry ; Samarium ; chemistry ; Structure-Activity Relationship ; Yttrium ; chemistry

Bone metastases are the main driver of morbidity and mortality in advanced prostate cancer. Targeting the bone microenvironment, a key player in the pathogenesis of bone metastasis, has become one of the mainstays of therapy in men with advanced prostate cancer. This review will evaluate the data supporting the use of bone-targeted therapy, including (1) bisphosphonates such as zoledronic acid, which directly target osteoclasts, (2) denosumab, a receptor activator of nuclear factor-kappa B (RANK) ligand inhibitor, which targets a key component of bone stromal interaction, and (3) radium-223, an alpha-emitting calcium mimetic, which hones to the metabolically active areas of osteoblastic metastasis and induces double-strand breaks in the DNA. Denosumab has shown enhanced delay in skeletal-related events compared to zoledronic acid in patients with metastatic castration-resistant prostate cancer (mCRPC). Data are mixed with regard to pain control as a primary measure of efficacy. New data call into question dosing frequency, with quarterly dosing strategy potentially achieving similar effect compared to monthly dosing for zoledronic acid. In the case of radium-223, there are data for both pain palliation and improved overall survival in mCRPC. Further studies are needed to optimize timing and combination strategies for bone-targeted therapies. Ongoing studies will explore the impact of combining bone-targeted therapy with investigational therapeutic agents such as immunotherapy, for advanced prostate cancer. Future studies should strive to develop biomarkers of response, in order to improve efficacy and cost-effectiveness of these agents.
Bone Density Conservation Agents/therapeutic use* ; Bone Neoplasms/secondary* ; Denosumab/therapeutic use* ; Diphosphonates/therapeutic use* ; Endothelins/antagonists & inhibitors* ; Humans ; Male ; Prostatic Neoplasms/pathology* ; Protein Kinase Inhibitors/therapeutic use* ; Radioisotopes/therapeutic use* ; Radiopharmaceuticals/therapeutic use* ; Radium/therapeutic use* ; Samarium/therapeutic use* ; Strontium Radioisotopes/therapeutic use*