Gene amplification and mutation analysis of epidermal growth factor receptor in hormone refractory prostate cancer.

Background: Amplification and mutation of the epidermal growth factor receptor (EGFR) and Her-2 genes were analyzed in both hormone sensitive and hormone refractory prostate cancer (HRPC).

Methods: Gene amplifications of EGFR and Her-2 were analyzed by fluorescence in situ hybridization (FISH) with direct sequencing. Studies were performed on a total of 10 patients; tissues were sampled at the time of initial diagnosis and after the conversion to HRPC (a total of 20 tissue samples).

Age-specific prostate-specific antigen reference ranges in Korean men.

Objectives: The serum prostate-specific antigen (PSA) level varies widely among different races and increases with age. In this study, we evaluated the variation in serum PSA levels in a multicenter study population to determine a standard age-specific PSA reference range for Korean men without clinically evident prostate cancer.

Methods: We retrospectively analyzed 120,439 Korean men, ranging in age from 30 to 79 years, whose serum PSA levels were measured at one of eight referral hospitals from November 1998 to July 2005.

Application of Pd(0)-catalyzed intramolecular oxazine formation to the efficient total synthesis of (-)-anisomycin.

The enantioselective total synthesis of (-)-anisomycin, a potent antibiotic agent, has been achieved. The key steps are a Pd(0)-catalyzed stereoselective intramolecular oxazine formation from d-tyrosine and pyrrolidine formation by catalytic hydrogenation of the oxazine.

Laparoscopic cholecystectomy under segmental thoracic spinal anaesthesia: a feasibility study.

Background: Laparoscopic surgery is normally performed under general anaesthesia, but regional techniques have been found beneficial, usually in the management of patients with major medical problems. Encouraged by such experience, we performed a feasibility study of segmental spinal anaesthesia in healthy patients.

Methods: Twenty ASA I or II patients undergoing elective laparoscopic cholecystectomy received a segmental (T10 injection) spinal anaesthetic using 1 ml of bupivacaine 5 mg ml-1 mixed with 0.

Stereoselective synthesis of L-threo-sphingosine, L-threo-sphinganine, D-threo-sphingosine, and D-threo-sphinganine via oxazoline formation and olefin cross-metathesis; potent protein kinase C inhibitor analogues.

In this study, we explored a convenient and concise route for synthesis of L-threo-sphingosine, D-threo-sphingosine, L-threo-sphinganine and D-threo-sphinganine from commercially available L- or D-serine. The key steps are the simple preparation of trans-oxazoline and intermolecular olefin cross metathesis.

A concise synthesis of a promising protein kinase C inhibitor: D-erythro-sphingosine.

In this study, we explored a convenient and concise route for synthesis of D-erythro-sphingosine 1 from commercially available and cheap L-serine. The key steps are simple preparation of amino ketone 5 from Weinreb amide 3 and high diastereoselective reduction of amino ketone 5 to give the natural erythro-(anti-) isomer.

Segmental spinal anaesthesia for cholecystectomy in a patient with severe lung disease.

Occasionally patients awaiting heart or lung transplant because of terminal disease require other types of surgery, but present significant challenges to the anaesthetist because of impaired organ function. Regional anaesthesia may have much to offer such patients and we here report one who underwent successfully a laparoscopic cholecystectomy under segmental subarachnoid (spinal) anaesthesia performed at the low thoracic level. The anatomical and physiological consequences of such a technique are discussed.

Diastereoselective synthesis of polysubstituted pyrrolidinone as a key intermediate for the anticancer agents by palladium(II)-catalyzed carboxylation.

Palladium(II)-catalyzed carboxylation of chiral olefins 6a-d has been examined under various conditions. In the weak basic condition (K2CO3), 7a-d were obtained in good yields. Alternatively, in the strong basic condition, pyrrolidinones 8a-d were obtained resulting in excellent yields and with high diastereoselectivity.

Synthesis of 2,3-disubstituted indole on solid phase by the Fischer indole synthesis.

2,3-Disubstituted indoles were synthesized by solid-phase reaction using the Fischer indole synthesis. A "traceless" silicon linker was employed with the silicon-carbon bonding being cleaved with TFA. An oxygen atom was placed into the middle of the spacer/linker so as to enhance solid-phase synthesis by better solvation.

Increased nephron volume is not a cause of supranormal renographic differential renal function in patients with ureteropelvic junction obstruction.

Purpose: Increasing clinical importance is being placed on the role of differential renal function (DRF) in the management of congenital ureteropelvic junction obstruction. Supranormal DRF of the hydronephrotic kidney on renal scan is a puzzling phenomenon and is hypothesized to be due to an increase in single nephron filtration or nephron volume without sound evidence. We studied the histopathological changes of hydronephrotic kidneys to determine whether glomerular hypertrophy underlies supranormal DRF.

Diastereoselective synthesis of anti-1,2-aminoalcohol by palladium(II) catalyzed aza-Claisen rearrangement.

In this study, a highly diastereoselective synthesis of anti-1,2-aminoalcohol was explored starting from L-amino acids as chiral sources. The higher yield and diastereoselectivity was shown when the aza-Claisen rearrangement was performed with allylic trichloroacetimidate 6a in the presence of palladium(II) catalyst.

Total synthesis of sphingofungin F.

[reaction: see text] A concise, stereocontrolled synthesis of sphingofungin F was achieved. Key features involve diastereoselective oxazoline formation catalyzed by palladium(0), MgBr(2)-promoted gamma-alkoxy allylic stannane addition, and palladium(0)-catalyzed coupling of a vinyl iodide with an organozinc reagent.

Syntheses of (+/-)-homoepibatidine analogues.

Syntheses of (+/-)-homoepibatidine analogues (2), which contain the 8-azabicyclo [3.2.1]octane ring system, were achieved by using palladium-catalyzed reductive-coupling reaction from 3 and the analgesic activity was tested by Mouse writhing antinociceptive assay.

Stereoselective syntheses of (+/-)-epibatidine analogues.

Stereoselective syntheses of (+/-)-epibatidine analogues 2, which contain the 8-azabicyclo [3.2.1]octane ring system, were achieved by using palladium-catalyzed cross-coupling reaction from 4 and the analgesic activity was tested by Mouse writhing antinociceptive assay.

Facile and efficient total synthesis of (+)-preussin.

[structure] The enantioselective total synthesis of (+)-preussin, a potent antifungal agent, has been achieved. The key steps are a Pd(0)-catalyzed oxazoline-forming reaction from L-phenylalanine, hydrogenolysis, and subsequent diastereoselective reductive cyclization of the intermediate aminoketone to pyrrolidine using Pearlman's catalyst.

Synthesis and characterization of stereospecific 1-propargyl-2-(dimethoxymethyl)-1-cyclohexanols.

Stereochemical isomers with hydroxy groups were synthesized by reacting 2-(dimethoxymethyl)cyclohexanone with propargylmagnesium bromide. The stereo chemical structures were identified by NMR spectral interpretation and the geometry optimization. To assist the NMR interpretation, geometry optimization based on semi-empirical AM1 and PM3 methods was applied.

Total synthesis of (+/-)-homoepibatidine.

Total synthesis of (+/-)-homoepibatidine (2), which contains the 8-azabicyclo[3.2.1] octane ring system, was achieved by using palladium-catalyzed Heck-type coupling reaction from 3.

Stereoselective synthesis of (+/-)-epibatidine analog:(+/-)-2beta-(2-chloro-5-pyridinyl)-8-azabicyclo[3.2.1] octane.

Stereoselective synthesis of (+/-)-epibatidine analog 2, which contains the 8-azabicyclo[3.2.1]octane ring system, was achieved by using palladium-catalyzed Heck-type coupling reaction from 3.

The facile and efficient synthesis of 8-chloroadenosine 3',5'-cyclic monophosphate by phosphorylative cyclization of 8-chloroadenosine and its characterization by(1)H and (13)C NMR spectroscopy.

Purine nucleosides were chlorinated by the reaction of acyl chloride in DMF with MCPBA under mild conditions with moderate yields. And, satisfactory method for the synthesis of ribonucleoside-3',5'-cyclic phosphates and its characterization by(1)H and(13)C nmr spectroscopy is described.

Conversion factors estimating indicative chronic no-observed-adverse-effect levels from short-term toxicity data.

Data on chronic toxicity are generally required to derive a health-based acceptable exposure limit, such as the acceptable daily intake. However, only acute and/or subacute toxicity data are available for many compounds. In this study, we assessed conversion factors (CFs) to estimate a chronic no-observed-adverse-effect-level (NOAELchronic) from these short-term toxicity data.

Synthesis of antihypertensive agents via coupling reaction of benzothiazepinone and 1,4-dihydropyridine derivatives.

The synthesis of 3a, 3b, 7a and 7b from Benzothiazepinone and 1,4-dihyropyridine derivatives is described. Benzothiazepinone and 1,4-dihydropyridine derivatives were prepared according to literature procedure. The key reactions involve esterification and amidation of benzothiazepinone and 1,4-dihydropyridine derivatives.

Sensitivity to retinal light damage and surgical blood oxygen levels.

Increased oxygen levels decrease the threshold for photochemical retinal damage. We measured arterial oxygen levels in a group of ophthalmic surgical patients. As expected, levels exceeded unanesthetized measurements by one to two times.