Synthesis and biological evaluation of carbocyclic analogues of pachastrissamine.

A series of carbocyclic analogues of naturally-occurring marine sphingolipid pachastrissamine were prepared and biologically evaluated. The analogues were efficiently synthesized via a tandem enyne/diene-ene metathesis reaction as a key step. We found that the analogue 4b exhibited comparable cytotoxicity and more potent inhibitory activity against sphingosine kinases, compared to pachastrissamine.

Total synthesis and structure confirmation of elatenyne: success of computational methods for NMR prediction with highly flexible diastereomers.

Elatenyne is a small dibrominated natural product first isolated from Laurencia elata. The structure of elatenyne was originally assigned as a pyrano[3,2-b]pyran on the basis of NMR methods. Total synthesis of the originally proposed pyrano[3,2-b]pyran structure of elatenyne led to the gross structure of the natural product being reassigned as a 2,2'-bifuranyl.

Percutaneous core needle biopsy for small (≤ 10 mm) lung nodules: accurate diagnosis and complication rates.

Purpose: To evaluate accurate diagnosis and complication rates of percutaneous core needle biopsy (PCNB) with an automated gun for small lung nodules that are 10 mm or less in diameter.

Materials And Methods: Forty-two cases of small lung nodules with diameters ≤ 10 mm (mean diameter, 9 mm) that received a PCNB were included in this study. Imaging guidance was fluoroscopy in 30 cases and computed tomography (CT) in 12 cases.

Syntheses of sulfur and selenium analogues of pachastrissamine via double displacements of cyclic sulfate.

Bioisosteric analogues of pachastrissamine that contain sulfur and selenium atoms replacing the oxygen in the ring system, were efficiently prepared from a cyclic sulfate intermediate by sequential intermolecular and intramolecular S(N)2 displacement reactions of the dianions. The analogues exhibited cytotoxicities comparable to that of pachastrissamine.

Coexistence of primary squamous cell carcinoma of thyroid with classic papillary thyroid carcinoma.

Primary squamous cell carcinoma of the thyroid gland is very rare and its histogenesis is poorly defined so far. Although there have been some cases of squamous cell carcinoma with variant types of papillary thyroid carcinoma (PTC), the present case is the first primary squamous cell carcinoma with classic PTC to be reported. A 43-year-old woman presented with a 20 year history of neck mass.

Laparoscopic assisted distal rectal cancer resection with preoperative concurrent chemoradiotherapy.

Purpose: Anatomy of deep pelvis, narrow distal margin and tumor invasion into neighbor organ are obstacles for curative radical resection for advanced cancer of distal rectum. Technically, laparoscopic application after downstaging the tumor with preoperative concurrent chemotherapy (CCRT) may give a solution to overcome the anatomical difficulties. We compared the results of laparoscopic surgery in the patients who received CCRT with those of patients who had conventional surgery.

OECD validation of the rodent Hershberger assay using three reference chemicals; 17alpha-methyltestosterone, procymidone, and p,p'-DDE.

The rodent Hershberger assay is being validated as an in vivo test method for detecting androgenic or antiandrogenic compounds by the Organization for Economic Cooperation and Development (OECD). As part of the international validation work, we studied 17alpha-methyltestosterone for evaluating androgenic activity, and procymidone and p,p'-DDE for evaluating antiandrogenic activity. Male Sprague-Dawley rats were castrated at postnatal day 42, and only the rats that showed preputial separation were used in this study.

Total synthesis and antiangiogenic activity of cyclopentane analogues of fumagillol.

Novel cyclopentane analogues of fumagillol were synthesized and their endothelial cell proliferation inhibitory activities were evaluated. The cyclopentane-fumagillol derivatives were synthesized from (-)-2,3-O-isopropylidene-D-erythronolactone via stereoselective glycolate Claisen rearrangement and intramolecular ester enolate alkylation as key steps.

A stereoselective asymmetric synthesis of antibiotic (-)-fumagillol using claisen rearrangement and intramolecular ester enolate alkylation as key steps.

(-)-Fumagillol (1), a hydrolysis product of fumagillin, has been synthesized by several group from commercially available 1,2:5,6-di-O-isopropylidene-alpha-D-allofuranose in a highly stereoselective manner. Chiral centers on C5 and C6 came from D-allofuranose and the asymmetric center on C4 was accomplished by 1,3-chirality transfer using the Claisen rearrangement on a chiral allyl alcohol. Chirality, which is necessary on an epoxide consisting of the spiro-ring system, was diastereoselectively constructed by the well-known reaction, intramolecular ester enolate alkylation (IEEA), which showed that this reaction can be applied to the alpha-alkoxy ester system.

Solid phase synthesis of 3-(4-hydroxyphenyl)coumarin: preliminary experiments for combinatorial synthesis of substituted 3-phenylcoumarin derivatives.

Coumarin and its derivatives occur widely in nature. Many attempts were made for synthesis of various coumarin derivatives because of their interesting biological activities. In this study, solid phase synthetic approach of 3-(4-hydroxyphenyl)coumarin was achieved for combinatorial synthesis of substituted 3-phenylcoumarin analogues.

A steerable guiding device: the new method in ultrasound guidance.

Rationale And Objectives: A working model (WM) of a newly designed device for ultrasound-guided puncture was tested.

Materials And Methods: WM featured a wheel-shaped metallic guide that passively rotated within the plane of view as the operator tried to redirect the needle. Four operators performed US-guided intercostal puncture of 24 targets in phantoms using a commercially available preset needle guide (PG).