Byproduct promoted regioselective sulfenylation of indoles with sulfinic acids.

An unprecedented method to synthesise 3-sulfenylindoles is demonstrated via byproduct promoted sulfenylation of indoles with sulfinic acids in the absence of an external catalyst. The reaction selectively afforded structurally diverse indole thioethers in good to excellent yields in 1,2-dichloroethane at 80 °C.

Catalytic allylation of stabilized phosphonium ylides with primary allylic amines.

A range of ketone-stabilized phosphonium ylides were allylated with high regioselectivity by primary allylic amines in the presence of 5 mol % Pd(PPh3)4 and 10 mol % B(OH)3, and subsequent one-pot Wittig olefination gave structurally diverse α,ß-unsaturated ketones in good to excellent overall yields with excellent E selectivity. The one-pot allylation/olefination reaction was extended to ester- and nitrile-stabilized phosphonium ylides by replacing B(OH)3 with TsOH, and the corresponding α,ß-unsaturated esters and nitriles were obtained in moderate overall yields.

[Correlation between estrogen receptor status and clinicopathologic parameters in endometrial cancer: a comparative study by immunohistochemistry using different scoring systems].

OBJECTIVE: To compare the efficiency of three different estrogen receptor (ER) immunostaining scoring systems by analyzing the correlation between ER status and clinicopathologic features for prediction of prognosis of patients with endometrial carcinoma (EC). METHODS: ER immunostaining (EnVision method) was performed in 160 type I EC and 39 type II EC paraffin samples and was scored by ASCO/CAP criterion, H-Score and Allred scoring system. Correlation between ER status and clinicopathologic features was statistically analyzed. RESULTS: ASCO/CAP criterion, H-Score and Allred (cutoff point: 4-8) scoring system showed high concordance in the following aspects. In EC patients, ER status was significantly associated with presurgical CA125 levels (P = 0.015, P = 0.007, P = 0.023), histologic grades (all P < 0.01) and PR status (all P < 0.01). In type I EC cohort, ER status was significantly correlated with PR status (P = 0.008, P < 0.01, P < 0.01) and p53 status (P = 0.042, P = 0.001, P < 0.01). As of the predictive value of ER status for type I EC patient age, ASCO/CAP (P = 0.027) and H-Score criteria (P = 0.035) were both superior to Allred score system (P = 0.064). Among well-known predictive clinicopathologic parameters, including FIGO stage, lympho-vascular involvement, lymph node metastasis, depth of myometrial invasion and omental involvement, ASCO/CAP scoring offered a better correlation (P = 0.005, P = 0.002, P = 0.021, P = 0.067, and P = 0.067, respectively) than H-Score (P > 0.05) and Allred scoring system (P > 0.05). CONCLUSIONS: Compared with H-Score and Allred scoring system, ASCO/CAP criterion is more closely correlated with predictive clinicopathologic parameters. Therefore it may be used as a simple, highly efficient prognostic indicator for EC patients in routine practice.

Prevalence and incidence of pseudomyxoma peritonei in urban China: A nationwide retrospective cohort study.

BACKGROUND: Pseudomyxoma peritonei (PMP) is an extremely rare condition. Information regarding the disease burden of PMP in developing countries is limited. This study aimed to determine the epidemiology of PMP in China. METHODS: PMP data were extracted from the national databases of Urban Basic Medical Insurance. All cases were identified using the International Classification of Diseases (ICD) codes and Chinese diagnostic terms. The national prevalence from 2012 to 2016 and incidence in 2016 were estimated. RESULTS: In total, 153 patients with PMP were identified. The crude prevalence of PMP in 2016 was 2.47 (95% confidence interval [CI] 1.71 to 3.23) per million person-year, with a higher prevalence in females than males. Prevalence increased with age, with the first peak in those aged 15-29 years and the highest in those aged >80 years. The crude incidence of PMP in 2016 was 1.19 (95% CI 0.59 to 1.78) per million person-years. Similar to the prevalence, the rates were higher in women than in men. The incidence also increased with age, with the highest prevalence in those aged >80 years. Besides, the most frequent comorbidities before and after the first diagnosis of PMP were unspecified secondary malignancies and malignancies of unspecified sites, followed by abdominal malignant tumours. CONCLUSIONS: The rate of PMP was lower in mainland China than in European countries and increased with advancing age. Women were more likely to have PMP than men. Furthermore, an insufficient understanding of this rare disease presents a major challenge in accurately evaluating the disease burden.

[Evaluation of two-tier grading system and significance of p53 protein over-expression in ovarian serous carcinoma].

OBJECTIVE: To evaluate the two-tier MDACC grading system for ovarian serous carcinoma by comparing with the WHO grading system, and to investigate the role of p53 immunostaining in ovarian serous carcinoma grading. METHODS: 72 cases ovarian serous carcinoma of ovary were graded basing on the MDACC and WHO grading systems, respectively. Statistic analyses were made for the relationship between the data obtained from two grading systems and their clinical significance. All the cases were examined immunohistochemically by using antibody against p53 protein and the immunohistochemistry findings were analyzed with the two grading systems and clinical parameters. RESULTS: There was a good correlation between the MDACC and WHO grading system (r=0.543, P=0.000). Neither system has a definite relationship with the disease-free survival time (P=0.170 vs. P=0.075), cytoreduction (P=0.478 vs. P=0.120), and the curative effect of platinum-based chemotherapy (P=0.418 vs. P=0.403). However, compared with the WHO grading system, MDACC grading system has a better correlation with tumor stage (P=0.041 vs. P=0.002), 3-year disease-free survival rate (P=0.077 vs. P=0.004), overall survival time (P=0.080 vs. P=0.046), and p53 immunohistochemistry results (P=0.334 vs. P=0.035). No significant difference was found between p53 immunohistochemistry results with other clinical characteristics and prognostic factors. CONCLUSIONS: Compared with the WHO system, the MDACC system showed a better prognostic value and was more likely correlated with the novel dualistic model for ovarian serous carcinogenesis. Although p53 immunostaining was valuable in assisting MDACC grading, it should be cautious to use it alone as an independent indicator in predicting the prognosis of ovarian serous carcinoma.

Selective benzylic and allylic alkylation of protic nucleophiles with sulfonamides through double Lewis acid catalyzed cleavage of sp3 carbon-nitrogen bonds.

The acid-catalyzed benzylic and allylic alkylation of protic nucleophiles is fundamentally important for the formation of carbon-carbon and carbon-heteroatom bonds, and it is a formidable challenge for benzylic and allylic amine derivatives to be used as the alkylating agents. Herein we report a highly efficient benzylic and allylic alkylation of protic carbon and sulfur nucleophiles with sulfonamides through double Lewis acid catalyzed cleavage of sp(3) carbon-nitrogen bonds at room temperature. In the presence of a catalytic amount of inexpensive ZnCl(2)-TMSCl (TMSCl: chlorotrimethylsilane), 1,3-diketones, beta-keto esters, beta-keto amides, malononitrile, aromatic compounds, thiols, and thioacetic acid can couple with a broad range of tosyl-activated benzylic and allylic amines to give diversely functionalized products in good to excellent yields and with high regioselectivity. Furthermore, the cross-coupling reaction of 1,3-dicarbonyl compounds with benzylic propargylic amine derivatives has been successfully applied to the one-step synthesis of polysubstituted furans and benzofurans.

[Preliminary study of vulvar and vaginal intraepithelial neoplasias].

OBJECTIVE: To detect the clinical features of vulvar and vaginal intraepithelial neoplasias (VIN and VAIN, respectively). METHODS: Total 148 women were performed vulvar or vaginal coloposcopy-directed biopsy pathology tests, from Sep. 2004 to Dec. 2007. RESULTS: Among 148 women, vulvar or vaginal histologic results were vulvar cancer for 1, VIN or VAIN 2, 3 for 23, VIN or VAIN for 16, condyloma for 61, vulvitis and vaginitis for 47. Eighty-five percent (33/39) women with VIN or VAIN 2, 3 were more than 30 years old. Compared to women with cervical intraepithelial neoplasia (CIN), women with VIN or VAIN were older. The rate of high-risk HPV DNA in women with vulvar or vaginal lesions was 84% (84/100). VAIN occurred mainly in the upper vagina (90%, 69/75). VIN or VAIN often accompanied or followed CIN or cervical cancer (79%, 31/39), and VIN or VAIN 2, 3 often accompanied or followed CIN 2, 3 or cervical cancer (70%, 16/23). CONCLUSION: Our data suggest that women with high-risk HPV infection are at risk of developing VIN or VAIN 2, 3. The vulva and vagina should be carefully inspected by colposcopic examination at the time of colposcopy for any abnormal findings.

Catalytic selective bis-arylation of imines with anisole, phenol, thioanisole and analogues.

The first highly efficient double Friedel-Crafts reaction of N-tosyl imines with anisole, phenol, thioanisole and analogues has been developed to produce the corresponding symmetric diarylmethanes and triarylmethanes with high regioselectivity in the presence of a catalytic amount of Bi(2)(SO(4))(3)-TMSCl at room temperature.

[Lung pathology and pathogenesis of severe acute respiratory syndrome: a report of six full autopsies].

OBJECTIVE: Severe acute respiratory syndrome (SARS) is an emerging infectious disease that first manifested in humans in November 2002. The SARS-associated coronavirus (SARS-CoV) has been identified as the causal agent, but the pathology and pathogenesis are still not quite clear. METHODS: Post-mortem lung samples from six patients who died from SARS from April to July 2003 were studied by light and electron microscopy, Masson trichromal staining and immunohistochemistry. Evidence of infection with the SARS-CoV was determined by reverse-transcription PCR (RT-PCR) , serological examination and electron microscopy. RESULTS: Four of six patients had serological and RT-PCR evidence of recent infection of SARS-CoV. Morphologic changes are summarized as follows: (1) Diffuse and bilateral lung consolidation was seen in all patients (6/6) with increasing lung weight. (2) Diffuse alveolar damage was universal (6/6) with hyaline membrane formation (6/6), intra-alveolar edema/hemorrhage (6/6), fibrin deposition (6/6), pneumocyte desquamation (6/6). A marked disruption in the integrity of the alveolar epithelium was confirmed by immunostaining for the epithelial marker AE1/AE3 (6/6). (3) Type II pneumocytes, with mild hyperplasia, atypia, cytomegaly with granular amphophilic cytoplasm and intracytoplasmic lipid accumulation (5/6). (4) Giant cells in the alveoli were seen in five of 6 patients (5/6) , most of which were positive for the epithelial marker AE1/AE3 (5/6), but some cells were positive for the macrophage marker CD68(2/6). (5) A pronounced increase of macrophages were seen in the alveoli and the interstitium of the lung (6/6), which was confirmed by histological study and immunohistochemistry. (6) Haemophagocytosis was present in five of the 6 patients(5/6). (7) Lung fibrosis was seen in five patients(5/6), with alveolar septa and interstitium thickening(5/6), intraalveolar organizing exudates (6/6) and pleura thickening (4/6). Proliferation of collagen was confirmed by Masson trichromal staining, most of which was type III collagen by immunostaining. The formation of distinctive fibroblast/myofibroblast foci was seen in five patients (5/6) by light microscopy and immunochemistry. (8) Squamous metaplasia of bronchial mucosa was seen in five patients(5/6). (9) Thrombi was seen in all patients(6/6). (10) Accompanying infection was present in two patients, one was bacteria, the other was fungus. In addition, electron microscopy revealed viral particles in the cytoplasm of alveolar epithelial cells and endothelial cells corresponding to coronavirus. CONCLUSION: Direct injury of SARS-CoV on alveolar epithelium, prominent macrophage infiltration and distinctive fibroblast/myofibroblast proliferation may play major roles in the pathogenesis of SARS.

Differential thymosin beta 10 expression levels and actin filament organization in tumor cell lines with different metastatic potential.

BACKGROUND: To investigate the differential expression levels of thymosin beta 10 (T beta 10) and the corresponding changes of actin filament organization in human tumor cell lines with different metastatic potential. METHODS: Four groups of nine human tumor cell lines with different metastatic potential were analyzed for the amount of T beta 10 mRNAs by Northern blot and for their peptide expression levels by immunohistochemistry. The filamentous actin (F-actin) was observed by staining of TRITC-phalloidin to detect changes in actin organization. RESULTS: In comparison with non-/weakly metastatic counterparts, T beta 10 was upregulated in highly metastatic human lung cancer, malignant melanoma and breast cancer cell lines. Staining of TRITC-phalloidin revealed less actin bundles, a fuzzy network of shorter filaments and some F-actin aggregates in the highly metastatic tumor cells. Meanwhile, the actin filaments were robust and orderly arranged in the non-/weakly metastatic cancer cell lines. CONCLUSION: T beta 10 levels correlate positively with the metastatic capacity in human tumors currently examined. The increasing metastatic potential of tumor cells is accompanied by a loss of F-actin, poorly arranged actin skeleton organizations and presence of F-actin aggregates. There is a consistent correlation between the elevated T beta 10 expression and the disrupted actin skeleton.

[Thymosin beta10 expression and actin filament organization in tumor cell lines with different metastatic potential].

OBJECTIVE: To investigate the expression of thymosin beta10 (Tbeta10) and related changes of actin filament organization in human tumor cell lines with different metastatic potential. METHODS: Four groups of nine human tumor cell lines with different metastatic potential were analyzed for the expression of Tbeta10 mRNA detected by northern-blot and its peptide by immunohistochemical staining. The filamentous actin (F-actin) was stained with TRITC-phalloidin to detect changes in actin organization. RESULTS: In comparison with the non and/or weakly metastatic counterparts, Tbeta10 was upregulated in highly metastatic human lung cancer, malignant melanoma and breast cancer cell lines. TRITC-phalloidin staining revealed less actin bundles and a fuzzy network of shorter filaments in the highly metastatic tumor cells, while in the non and/or weakly metastatic cancer cell lines, there were thick and orderly arranged actin filaments. CONCLUSIONS: Tbeta10 levels correlate positively with the metastatic phenotype in human tumors currently examined. The increased metastatic potential of tumor cells is accompanied by the loss of F-actin and poorly organized actin skeleton. There is a consistent correlation between the elevated Tbeta10 expression and the disrupted actin skeleton.

Catalytic stereospecific alkylation of malononitriles with enantioenriched primary allylic amines.

An unprecedented alkylation reaction of malononitriles with enantioenriched primary allylic amines has been developed in a stereospecific manner through palladium-catalyzed sp(3) C-N bond cleavage without additives at room temperature.

Ferric chloride-catalyzed C-N bond cleavage for the cyclization of arylallenes leading to polysubstituted indenes.

A range of arylallenes undergo carbocation-initiated cyclization reaction with N-benzylic and N-allylic sulfonamides in the presence of 10 mol% ferric chloride to give structurally diverse polysubstituted indenes in good yields with extremely high regioselectivity.

Catalytic regioselective synthesis of structurally diverse indene derivatives from N-benzylic sulfonamides and disubstituted alkynes.

An unprecedented protocol has been developed for the regioselective synthesis of structurally diverse indene derivatives from readily accessible N-benzylic sulfonamides and disubstituted alkynes through FeCl(3)-catalyzed cleavage of sp(3) carbon-nitrogen bonds to generate benzyl cation intermediates. In the presence of 10 mol % of FeCl(3), a broad range of N-benzylic sulfonamides smoothly react with internal alkynes, alkynylcarbonyl compounds, alkynyl chalcogenides, or alkynyl halides to afford various functionalized indene derivatives with extremely high regioselectivity.

Natural history of infections with high-risk HPV in Chinese women with abnormal cervical cytology findings at baseline.

OBJECTIVE: To clarify the natural history of disease in Chinese women with benign cytologic observation and positive for high-risk human papillomavirus (HR-HPV). METHOD: From September 1, 2004, to June 30, 2008, this prospective study followed up 893 women positive for HR-HPV who also had benign cytologic findings at baseline. RESULTS: After 3 to 57 months, the viral clearance rate was higher for patients younger than 30 years and for patients who had a low viral load at baseline than for those in their comparison groups. Conversely, the occurrence rate of cervical intraepithelial neoplasia (CIN) 2 or 3 was higher for patients with persistent HR-HPV infection, those who had CIN 1 at baseline, and those whose the second viral load was increased. CONCLUSION: Age, viral load, and presence of CIN 1 at the first evaluation were the main factors affecting the natural history of HR-HPV infection in women with benign baseline cytologic findings. The result(s) of the second HR-HPV testing were independent indicators of histologic progression.

Catalyst-free alkylation of sulfinic acids with sulfonamides via sp(3) C-N bond cleavage at room temperature.

An unprecedented catalyst-free alkylation of sulfinic acids with sulfonamides has been developed via sp(3) C-N bond cleavage at room temperature. In the absence of external catalysts and additives, a wide variety of N-benzylic and N-allylic sulfonamides couple with sulfinic acids to give structurally diversified sulfones in moderate to excellent yields. Furthermore, the reaction of N-(2-acyl)allylic sulfonamides with sulfinic acids provides a convenient access to trisubstituted allyl sulfones with exclusive Z selectivity.