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Cysteine represents an attractive target for peptides/proteins modification due to the intrinsic high nucleophilicity of the thiol group and low natural abundance. Herein, a cleavable and tunable covalent modification approach...

We report the first highly enantio-and diastereoselective three-component Povarov reaction between anilines and aldehydes catalyzed by a chiral amine catalyst. A wide variety of substituted tetrahydroquinolines were obtained with moderate to good yields and excellent enantioselectivity and diastereoselectivity (up to 99% ee and >95:5 dr) under the reaction conditions. Furthermore, the reaction intermediates could be efficiently converted to other valuable building blocks. Letter pubs.acs.org/OrgLett

Efficient Pd-catalyzed ortho-olefination of Tyr residues by employing silanol as a directing group with high chemo- and site-selectivity was developed. Orthogonal protection strategies were also successfully applied to SPPS.

Background: To investigate the effect of stereotactic body radiation therapy (SBRT) on pulmonary oligometastases and to analyze the clinical factors and dose parameters affecting local recurrence-free survival (LRFS) and overall survival (OS). Methods: This study retrospectively enrolled a total of 84 patients (148 lesions) treated in our department from May 2015 to November 2018. Pulmonary oligometastases was defined as up to 5 metastatic lesions in the lung and with both the primary tumor and any extra-thoracic metastases being controlled. Patients receiving a BED 10 (biological effective dose, α/β =10) of SBRT ≥75 Gy and a dose/fraction ≥4 Gy were enrolled. The patient group consisted of 52 men (61.9%) and 32 women (38.1%), with a median age 56 years (range, 29-80 years). Median tumor diameter was 1.71cm (range, 1.2-5.0 cm). The BED 10 was 75-119 Gy in 4-15 fractions. Univariate and multivariate Cox regression analyses were performed on factors predicting the outcomes. Results: All patients completed the treatment as planned, and the median follow-up time was 20.3 months.The median OS for the entire group was 34.3 months, with an actuarial 1-, 2-, 3-and 5-year OS of 74.7%, 59.4%, 49.7%, and 36.8%, respectively. Among the 148 lesions in the whole group, 19 (12.8%) lesions had local recurrence (LR). The median LRFS time for all patients was 56.9 months. The LRFS rate was 93.6%, 83.5%, 81.4%, and 76.6% at 1, 2, 3, and 5 years, respectively. No patient developed acute grade 3 or 4 toxicity.On univariate analysis, age ≥63 years old, primary site of colorectal cancer, BED 10 <85.2 Gy, pathological type of adenocarcinoma, planning target volume (PTV) min BED 10 <76.6 Gy, and gross tumor volume (GTV) ≥8.8 cc, were significantly associated with poorer LRFS. Multivariate analysis showed that age ≥63 years old, primary site of colorectal cancer, and PTV min BED 10 <76.6 Gy were significant risk factors affecting LRFS.Conclusions: SBRT is feasible for pulmonary oligometastasis with favorable local control and minimal toxicity. Multiple dose parameters, instead of a prescription dose only, in combination with clinical parameters, should be considered for optimal local control.