Characterization of CIAE developed double-sided silicon strip detector for charged particles

A double-sided silicon strip detector(DSSD)with active area of 48 mm x 48 mm and thickness of300μm has been developed. Each side of DSSD consists of48 strips, each with width of 0.9 mm and inter-strip separation of 0.1 mm. Electrical properties and detection performances including full depletion bias voltage, reverse leakage current, rise time, energy resolution and cross talk have been studied. At a bias of 80 V, leakage current in each strip is less than 15 nA, and rise time for alpha particle at 5157 keV is approximately 15 ns on both sides.Good energy resolutions have been achieved with0.65-0.80% for the junction strips and 0.85-1.00% for the ohmic strips. The cross talk is found to be negligible on both sides. The overall good performance of DSSD indicates its readiness for various nuclear physics experiments.

Discovery of a potential bladder cancer inhibitor CHNQD-01281 by regulating EGFR and promoting infiltration of cytotoxic T cells

As one of the common malignancies that threaten human life,bladder cancer occurs frequently with a high mortality rate in the world,due to its invasion,recurrence and drug resistance.Natural products from marine microorganisms are becoming the hotspots in discovery of new candidate drug entities,especially in the area of cancer.Brefeldin A(BFA)is a natural Arf-GEFs inhibitor,but due to the low aqueous solubility,strong toxicity,and poor bioavailability,it is urgent to conduct structural optimization research.Herein,a new BFA pyridine acrylate derivative CHNQD-01281 with improved solubility was prepared and found to exert moderate to strong antiproliferative activity on a variety of human cancer cell lines.It was noteworthy that CHNQD-01281 was most sensitive to two bladder cancer cell lines T24 and J82(IC50=0.079 and 0.081μmol/L)with high selectivity index(SI=14.68 and 14.32),suggesting a superior safety to BFA.In vivo studies revealed that CHNQD-01281 remarkably suppressed tumor growth in a T24 nude mice xenograft model(TGI=52.63%)and prolonged the survival time(ILS=68.16%)in an MB49 allogeneic mouse model via inducing infiltration of cytotoxic T cells.Further mechanism exploration indicated that CHNQD-01281 regulated both EGFR/PI3K/AKT and EGFR/ERK pathways and mediated the chemotactic effect of chemokines on immune effector cells.Overall,CHNQD-01281 may serve as a potential therapeutic agent for bladder cancer through multiple mechanisms.

Rhodium-Catalyzed Direct C-H Alkenylation of Indoles with Alkenyl Borates

Main observation and conclusion A new Rh(Ⅲ)-catalyzed direct C—H alkenylation of 2,3-unsubstitued indoles with alkenyl borates through C—H activation followed by transmetallation was described.This protocol provides an efficient method for the synthesis of terminal C2-alkenylindoles under mild conditions,and also shows broad substrate scope and high functional group tolerance with respect to both components.Furthermore,the C2-alkenylated indole can be easily transformed into carboline derivative,which is an important polycyclic indole moiety in natural products and drug molecules.