Synthesis and biological assessment of 3,7-dihydroxytropolones.

3,7-Dihydroxytropolones (3,7-dHTs) are highly oxygenated troponoids that have been identified as lead compounds for several human diseases. To date, structure-function studies on these molecules have been limited due to a scarcity of synthetic methods for their preparation. New synthetic strategies towards structurally novel 3,7-dHTs would be valuable in further studying their therapeutic potential. Here we describe the successful adaptation of a [5 + 2] oxidopyrilium cycloaddition/ring-opening for 3,7-dHT synthesis, which we apply in the synthesis of a plausible biosynthetic intermediate to the natural products puberulic and puberulonic acid. We have also tested these new compounds in several biological assays related to human immunodeficiency virus (HIV), hepatitis B virus (HBV) and herpes simplex virus (HSV) in order to gain insight into structure-functional analysis related to antiviral troponoid development.

Lymphoscintigraphy in tumors of the head and neck using double tracer technique.

UNLABELLED: Knowledge of possible lymphatic drainage may facilitate planning of surgery for patients with head and neck tumors. Therefore, the aim of this study was to present a method of lymphoscintigraphy with special attention to an accurate correlation of lymphatic drainage to anatomic regions. METHODS: Lymphoscintigraphy was performed using a double tracer technique before surgery in a total of 75 patients with squamous cell carcinoma of the head and neck. All patients received 100 MBq 99mTc-colloid at three to four peritumoral sites. A perchlorate solution (2 mL) was given orally to block salivary glands and the thyroid gland. Patients received 50 MBq 99mTc-pertechnetate intravenously for body contouring 20 min postinjection. Planar images were obtained over 5 min each, at 30 min and 4 h postinjection from anterior, right lateral and left lateral views with a large-field-of-view gamma camera. Lymphatic drainage was assessed by visual inspection and assigned to six cervical compartments. RESULTS: Neither the salivary glands nor the thyroid gland were seen in any of the patients. In 22 of 75 patients (29.3%), the injection site was the only focal tracer uptake seen. In contrast, lymphatic drainage was identified in the remaining 53 patients (70.7%), and lymph nodes could be assigned easily to the six cervical compartments. Of 75 patients, 36 (48%) exhibited ipsilateral lymphatic drainage. In addition, 17 patients (22.7%) with unilateral tumor showed bilateral (n = 12), contralateral (n = 2) or retropharyngeal (n = 3) lymphatic drainage. In 3 of these 17 patients, bilateral lymph node metastases were proven. A subgroup of 12 patients (16%) exhibited N2c nodal status, despite a unilateral localized primary tumor. In 3 of these 12 patients, surgery was extended as a result of scintigraphic findings from unilateral toward bilateral neck dissection, and histology confirmed nodal involvement in these patients. CONCLUSION: Lymphoscintigraphy using the double tracer technique allows an accurate correlation of lymphatic drainage to the six cervical compartments. This may provide the basis for a re-evaluation of its impact in treatment planning of patients with head and neck tumors.

Transoral carbon dioxide laser resection of supraglottic carcinoma.

Between 1981 and 1994, 34 patients with squamous cell carcinoma of the supraglottis were treated by transoral carbon dioxide laser resection, 12 of them palliatively. Additional treatment included neck dissection in 21 patients and radiotherapy in 24 patients. The 3-year overall survival was 62%, and the actuarial survival 80%. The overall survival for T1 and T2 tumors was 71%, and that for T3 and T4 tumors was 47%. The overall 3-year survival for the early stages, I and II, was 88%, and that for the advanced stages, III and IV, was 50%. These results are comparable to the outcome after conventional open partial resection. Given the significantly lower morbidity (only 7 patients required tracheostomy), we do not observe an age limit anymore. The transoral method can be recommended as curative treatment in T1 and T2 tumors and in selected T3 and T4 tumors in concert with neck dissection and/or radiotherapy. In patients with advanced inoperable tumors, laser surgery is an excellent alternative to tracheostomy and palliative radiotherapy. Prerequisites for successful application of the transoral carbon dioxide laser resection are adequate resection techniques.

Mycosis fungoides of the larynx: case report and review of the literature.

Mycosis fungoides is a rare cutaneous lymphoma. Dissemination to extra-cutaneous sites occurs at advanced stages of disease. Laryngeal manifestations of mycosis fungoides have been reported in only 13 cases in the available literature. We present a further calla of mycosis fungoides of the larynx at the terminal stage of disease with an additional manifestation in the left maxillary sinus and review the cases published to date. To our knowledge this is the first reported case of mycosis fungoides with laryngeal and paranasal sinus manifestation. Concluding from the present case and from literature therapy should be palliative to improve quality of life.

[Malignant melanoma of the uvula and soft palate]. / Malignes Melanom der Uvula und des weichen Gaumens.

Malignant melanoma of the uvula and soft palate is very rare. We describe a case demonstrating the typical aggressive behavior of mucosal melanoma in contrast to cutaneous melanoma. Regional lymph node and distant metastases often develop rapidly in this type of melanoma. Despite aggressive surgical approaches, other treatment options are often limited and usually palliative. Therefore, early diagnosis is critical in patients with mucosal melanoma.

[Lymphoscintigraphy with double tracer technique in carcinomas of the head-neck region]. / Lymphszintigraphie in Doppeltracertechnik bei Karzinomen im Kopf-Hals-Bereich.

BACKGROUND: Lymphoscintigraphy has been used since the early 1960s to demonstrate lymphatic drainage of head and neck tumors, but did not prove satisfactory. With the increasing importance of highly sophisticated neck dissection procedures, lymphoscintigraphy may have greater diagnostic impact. This assumes that lymphoscintigraphy will allow an accurate correlation of lymphatic drainage with anatomic structures. In this paper, we report on a method of lymphoscintigraphy with simultaneous body contouring. METHODS: Double-tracer lymphoscintigraphy was performed in 78 patients with squamous cell carcinoma. Patients received 100 MBq 99mTc-colloid in 0.1-0.2 ml in 3-4 peritumoral localizations. Ten patients were injected during surgery. Two milliliters of perchlorate solution were given orally in order to block the thyroid. Twenty minutes later patients received 50 MBq 99mTc-pertechnetate i.v. for body contouring. Planar images were obtained over 5 min each at 30 min and 4-6 h after injection from anterior, right lateral and left lateral using a LFOV-gamma camera. RESULTS: The thyroid was not visualized in any of the patients. In 28 of 78 patients (36%), the injection site was the only focal activity seen. In 50 of 78 patients (64%), lymph drainage was observed. Thirty-six of 78 patients (46%) showed unilateral lymphatic drainage, and 14 of 78 (18%) showed bilateral drainage. In all 50 patients showing lymphatic drainage, lymph nodes could be easily assigned to the six cervical lymph node compartments described. CONCLUSIONS: Double-tracer lymphoscintigraphy enables an accurate correlation of cervical lymph nodes and anatomic structures of the head and neck region. These findings suggest that the impact of these studies on the preoperative planning for neck dissection should be reevaluated.

Sentinel lymph-node biopsy in head and neck cancer.

The aim of the study was to assess the diagnostic value of the sentinel node method in patients suffering from squamous cell carcinoma of the upper aerodigestive tract. In 50 patients with oral, pharyngeal or laryngeal carcinomas staged N0 up to 50 MBq technetium-99m colloid were injected peritumorally. Sentinel nodes were localised using a gamma-probe in the setting of an elective neck dissection. Pathological findings of sentinel nodes and corresponding neck specimens were compared. In 46 patients sentinel nodes were detected. Of these 34 patients were free of metastatic disease in the sentinel nodes and in the neck specimens. In 12 patients clinically occult metastases were found in the sentinel nodes. Three metastases were detected only after additional sectioning of the sentinel nodes. In four patients, a sentinel lymph node could not be localised. Our results support the sentinel node concept in head and neck cancer and a definition of the sentinel nodes as the three nodes with the highest activity. Careful clinical staging of the neck and thorough pathological evaluation of the sentinel nodes are necessary to avoid false-negative results.