Copper-catalyzed intermolecular formal (5 + 1) annulation of 1,5-diynes with 1,2,5-oxadiazoles.

One-carbon homologation reactions based on one-carbon insertion into the N-O bond of heterocycles have received tremendous interest over the past decades. However, these protocols have to rely on the use of hazardous and not easily accessible diazo compounds as precursors, and examples of the relevant asymmetric catalysis have not been reported. Here we show that a copper-catalyzed intermolecular formal (5 + 1) annulation of 1,5-diynes with 1,2,5-oxadiazoles involving one-carbon insertion into the heterocyclic N-O bond via non-diazo approach.

Construction of Axially Chiral Arylpyrroles via Atroposelective Diyne Cyclization.

Axially chiral biaryls widely exist in natural products and pharmaceuticals and are used as chiral ligands and catalysts in asymmetric synthesis. Compared to the well-established axially chiral 6-membered biaryl skeletons, examples of 5-membered biaryls have been quite scarce, and mono-substituted 3-arylpyrrole atropisomers have not been reported. Here, we disclose a copper-catalyzed atroposelective diyne cyclization for the construction of a range of axially chiral arylpyrrole biaryls in good to excellent yields with generally excellent enantioselectivities via oxidation and X-H insertion of vinyl cations.

Copper-Catalyzed Enantioselective Doyle-Kirmse Reaction of Azide-Ynamides via α-Imino Copper Carbenes.

[2,3]-Sigmatropic rearrangement reaction involving sulfonium ylide (Doyle-Kirmse reaction) generated from metal carbenes represents one of the powerful methods for the construction of C(sp )-S and C-C bonds. Although significant advances have been achieved, the asymmetric versions via the generation of sulfonium ylides from metal carbenes have been rarely reported to date, and they have so far been limited to diazo compounds as metal carbene precursors. Here, we describe a copper-catalyzed enantioselective Doyle-Kirmse reaction via azide-ynamide cyclization, leading to the practical and divergent assembly of an array of chiral [1,4]thiazino[3,2-b]indoles bearing a quaternary carbon stereocenter in generally moderate to excellent yields and excellent enantioselectivities.

Famitinib with Camrelizumab and Nab-Paclitaxel for Advanced Immunomodulatory Triple-Negative Breast Cancer (FUTURE-C-Plus): An Open-Label, Single-Arm, Phase II Trial.

Purpose: Camrelizumab, an mAb against programmed cell death protein 1 (PD-1), plus nab-paclitaxel exhibited promising antitumor activity in refractory metastatic immunomodulatory triple-negative breast cancer (TNBC). Famitinib is a tyrosine kinase inhibitor targeting VEGFR2, PDGFR, and c-kit. We aimed to assess the efficacy and safety of a novel combination of famitinib, camrelizumab, and nab-paclitaxel in advanced immunomodulatory TNBC.

Concurrent neoadjuvant chemotherapy and estrogen deprivation in patients with estrogen receptor-positive, human epidermal growth factor receptor 2-negative breast cancer (CBCSG-036): A randomized, controlled, multicenter trial.

Background: The current randomized, controlled, multicenter clinical trial was conducted to investigate the efficacy of concurrent neoadjuvant chemotherapy (NCT) and estrogen deprivation in patients with estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative breast cancer.

Methods: Eligible patients with AJCC stage IIB to stage IIIC, ER-positive, HER2-negative breast cancer were enrolled and randomly assigned to receive NCT with or without estrogen deprivation. The primary endpoint was the objective response rate (ORR).

Weekly paclitaxel plus carboplatin with or without trastuzumab as neoadjuvant chemotherapy for HER2-positive breast cancer: loss of HER2 amplification and its impact on response and prognosis.

Purpose: Neoadjuvant chemotherapy (NCT) plus anti-HER2 agents are the standard of care for locally advanced HER2-positive breast cancer. The aim of this study was to evaluate the prevalence and prognostic impact of HER2 loss in patients with HER2-positive disease treated with neoadjuvant therapy with or without trastuzumab.

Methods: 549 consecutive HER2-positive patients were included in this study.

Pathological complete response as a surrogate for relapse-free survival in patients with triple negative breast cancer after neoadjuvant chemotherapy.

We retrospective analyzed triple negative breast cancer (TNBC) patients who received either taxane-based or anthracycline-based neoadjuvant chemotherapy, evaluated whether pathological complete response (pCR) is a surrogate endpoint for relapse free survival (RFS) in TNBC and explored which subgroup of patients benefits more from superior treatment regimen. 186 patients received taxane-based (Group A) or anthracycline-based (Group B) neoadjuvant chemotherapy, median follow-up was 48.1 months.

Progesterone receptor loss identifies luminal-type local advanced breast cancer with poor survival in patients who fail to achieve a pathological complete response to neoadjuvant chemotherapy.

The aim of this study was to investigate the potential of progesterone receptor (PgR) as a biomarker for differentiating estrogen receptor (ER)-positive patients who fail to achieve a pathological complete response to neoadjuvant chemotherapy (NCT) with different prognoses. A total of 327 consecutive, locally advanced breast cancer patients with ER-positive disease were included in this study. According to their HER-2 and Ki-67 status, the patients were classified into the Luminal-A or Luminal-B subtype.

ER-poor and HER2-positive: a potential subtype of breast cancer to avoid axillary dissection in node positive patients after neoadjuvant chemo-trastuzumab therapy.

Purpose: The study was to estimate the likelihood of axillary downstaging and to identify the factors predicting a pathologically node negative status after neoadjuvant chemotherapy (NAC) with or without trastuzumab in HER2-positive breast cancer.

Methods: Patients with HER2-positive, stage IIa-IIIc breast cancer were enrolled. Axillary status was evaluated by palpation and fine needle aspiration (FNA) before NAC.

Lymph node counts and ratio in axillary dissections following neoadjuvant chemotherapy for breast cancer: a better alternative to traditional pN staging.

Background: Neoadjuvant chemotherapy (NCT) for breast cancer might change the number of involved and detected nodes in axillary lymph node dissections (ALND). In this study, we analyzed whether the number of dissected nodes and the lymph node ratio (LNR, defined as the proportion of involved nodes in dissected nodes) would have a better prognostic value than traditional pN staging.

Methods: A total of 569 patients with stage II, III breast cancer were included in this retrospective study.

Weekly paclitaxel/carboplatin/trastuzumab therapy improves pathologic complete remission in aggressive HER2-positive breast cancers, especially in luminal-B subtype, compared with a once-every-3-weeks schedule.

Background: The efficacy and tolerability of two different schedules of paclitaxel, carboplatin, and trastuzumab (PCarH) for HER2-positive, locally aggressive (stage IIB-IIIC) breast cancers were evaluated in this phase II trial.

Methods: Patients were randomly assigned to receive either weekly (12 doses over 16 weeks) or once-every-3-weeks (4 doses over 12 weeks) treatment. The primary endpoint was pathologic complete remission (pCR) in the breast and axilla.

Obesity or overweight is associated with worse pathological response to neoadjuvant chemotherapy among Chinese women with breast cancer.

Background: To evaluate the relationship between body mass index (BMI) and response to neoadjuvant chemotherapy (NCT) for breast cancer among Chinese women.

Patients And Methods: A total of 307 eligible patients were assigned to receive four cycles of paclitaxel and carboplatin before standard surgery for breast cancer from 2007 to 2011 at Shanghai Cancer Hospital. The patients were categorized as obese, overweight, normal weight, or underweight based on BMI according to World Health Organization (WHO) criteria.

Association of HER-2 copy number and HER-2/CEP-17 ratio with neoadjuvant taxane-containing chemotherapy sensitivity in locally advanced breast cancer.

Purpose: Aneusomy 17 causes inconsistency in fluorescence in situ hybridization (FISH)-based human epidermal growth factor receptor (HER)-2 status assessment using different algorithms (copy number or the HER-2/centromere enumerator probe 17 [CEP-17] ratio). We investigated the effects of FISH-based HER-2 status assessment and aneusomy 17 on responsiveness to neoadjuvant chemotherapy (NAC).

Patients And Methods: This prospective study recruited 152 patients with locally advanced breast cancer who underwent four-cycle weekly paclitaxel plus carboplatin without trastuzumab.

Prognostic value of a positive-to-negative change in hormone receptor status after neoadjuvant chemotherapy in patients with hormone receptor-positive breast cancer.

Background: To investigate the prognostic value of positive-to-negative changes in hormone receptor (HR) status after neoadjuvant chemotherapy (NCT) in patients with HR-positive breast cancer.

Methods: Data from 224 stage II-III breast cancer patients with positive HR status before NCT who had residual disease in the breast after NCT were collected. HR status of the residual tumors was retested after NCT.

A prognostic model to predict outcome of patients failing to achieve pathological complete response after anthracycline-containing neoadjuvant chemotherapy for breast cancer.

Background: The aim of this study was to evaluate factors that could possibly affect the outcome of patients failing to achieve pathological complete response (pCR) after anthracycline-containing neoadjuvant chemotherapy (NCT) for breast cancer, and built a prognostic model to predict patients' outcome.

Patients And Methods: Data from 199 stage II-III breast cancer patients who failed to achieve pCR after NCT were used. Variables at baseline and at surgery (age, menopausal status, tumour size, grade, histotype, node status, vascular invasion, ER, PR, HER-2, Cathepsin D, P53, Topo-IIα, Nm-23, Bcl-2, BAX, MDR, GSTN, PS2, P27, Cyclin D1 and Ki-67) were investigated.

Molecular subtype can predict the response and outcome of Chinese locally advanced breast cancer patients treated with preoperative therapy.

We investigated whether molecular subtype can predict the response and prognosis in Chinese locally advanced breast cancer (LABC) patients treated with preoperative therapy. LABC patients treated with preoperative therapy in Cancer Hospital, Fudan University between August 2001 and May 2008 were retrospectively analyzed. Molecular subtypes were constructed from the immunohistochemical results of hormonal receptors (HR) and HER2 status, which were classified as luminal (HR+/HER2-), triple negative (HR-/HER2-) and HER2 positive subtypes.

[Effect of postoperative pregnancy upon prognosis of young breast cancer patients].

Objective: To examine the effect of postoperative pregnancy upon the prognosis of young Chinese breast cancer patients.

Methods: Four hundred and thirty-two female unilateral breast cancer patients aged 35 or younger were retrospectively reviewed. Kaplan-Meier analysis and Log Rank test were used for univariate analysis of factors predictive of disease-free survival (DFS) and overall survival (OS).

[Study on predictors of long term results for neo-adjuvant chemotherapy in locally advanced breast cancer].

Objective: To identify predictive markers of the long-term outcome for neo-adjuvant chemotherapy (NC) in locally advanced breast cancer (LABC) treated with intravenous vinorelbine (V) and epirubicin (E) combination regimen.

Methods: One hundred and nineteen patients with LABC were treated from September 2001 to May 2006. All patients were diagnosed as invasive breast cancer by 14G core needle biopsy and treated with three cycles of VE regimen before the operation.

[A study on the relationship between breast cancer molecular classification and prognosis].

Objective: To investigate the relationship between breast cancer molecular classification and prognosis.

Methods: From January 2002 to December 2003, 708 female primary breast cancer patients with a mean age of 53 years old were retrospectively analyzed. The classification of breast cancer was according to the immunohistochemical results of estrogen receptor (ER), progesterone receptor (PR) and human epidermal growth factor receptor (HER2) status.

Neoadjuvant chemotherapy with vinorelbine-containing regimens in elderly patients with locally advanced breast cancer.

Background: The purpose of this study was to evaluate retrospectively the efficacy and safety of neoadjuvant chemotherapy with vinorelbine-containing regimens in elderly patient with locally advanced breast cancer (LABC).

Patients And Methods: From 2002 to 2006, 14 female elderly patients with LABC underwent neoadjuvant chemotherapy with vinorelbine-containing regimens. Vinorelbine alone or in combination with pirarubicin/epirubicin was administered every 3 weeks (25 mg/m2, i.

Fiberoptic ductoscopy combined with cytology testing in the patients of spontaneous nipple discharge.

Fiberoptic ductoscopy system (FDS) offers a safe alternative to ductography in diagnosing intraductal lesions and serves as a guide for subsequent surgery in women with nipple discharge. In this article, we reported the outcomes of FDS combined with cytology testing for diagnosis of spontaneous nipple discharge. From 1997 to 2005, 1,048 women (1,093 breasts total) in the outpatient department underwent successful diagnostic FDS.

[Stereotactic biopsy for non-palpable breast lesions: evaluation and choice of minimal invasive and excisional biopsy].

Objective: To evaluate three biopsy methods which are currently used in stereotactic breast biopsy.

Methods: A total of 361 cases of stereotactic breast biopsies were carried out since 2000, including 73 cases of true cut core needle biopsies (ST-CNB), 74 cases of vacuum assisted biopsies (ST-VAB) and 214 cases of excisional biopsies. After medium follow-up time of 18 months (6 to 66 months), the accuracy as well as the clinical benefits of the three stereotactic biopsy procedures were analyzed retrospectively.

[A study of the combination of vinorelbine and epirubicin as neoadjuvant chemotherapy regimen in the treatment of locally advanced breast cancer].

Objective: To evaluate the clinical efficacy and toxicity of vinorelbine (N) and epirubicin (E) as the neoadjuvant chemotherapy regimen in the treatment of locally advanced breast cancer (LABC).

Methods: From September 2001 to December 2004, 158 patients with LABC were treated with NE chemotherapy before operation. Neoadjuvant chemotherapy containing vinorelbine (N), 25 mg/m(2) (days 1 and 8) and epirubicin (E), 60 mg/m(2) (days 1) was administered every 3 weeks for three cycles before local treatment.