Microtubule Destabilizing Sulfonamides as an Alternative to Taxane-Based Chemotherapy

Pan-Gyn cancers entail 1 in 5 cancer cases worldwide, breast cancer being the most commonly diagnosed and responsible for most cancer deaths in women. The high incidence and mortality of these malignancies, together with the handicaps of taxanes—first-line treatments—turn the development of alternative therapeutics into an urgency. Taxanes exhibit low water solubility that require formulations that involve side effects. These drugs are often associated with dose-limiting toxicities and with the appearance of multi-drug resistance (MDR). Here, we propose targeting tubulin with compounds directed to the colchicine site, as their smaller size offer pharmacokinetic advantages and make them less prone to MDR efflux. We have prepared 52 new Microtubule Destabilizing Sulfonamides (MDS) that mostly avoid MDR-mediated resistance and with improved aqueous solubility. The most potent compounds, N-methyl-N-(3,4,5-trimethoxyphenyl-4-methylaminobenzenesulfonamide 38, N-methyl-N-(3,4,5-trimethoxyphenyl-4-methoxy-3-aminobenzenesulfonamide 42, and N-benzyl-N-(3,4,5-trimethoxyphenyl-4-methoxy-3-aminobenzenesulfonamide 45 show nanomolar antiproliferative potencies against ovarian, breast, and cervix carcinoma cells, similar or even better than paclitaxel. Compounds behave as tubulin-binding agents, causing an evident disruption of the microtubule network, in vitro Tubulin Polymerization Inhibition (TPI), and mitotic catastrophe followed by apoptosis. Our results suggest that these novel MDS may be promising alternatives to taxane-based chemotherapy in chemoresistant Pan-Gyn cancers.     

GPRS手机入网测试自动化

全球移动通信系统(GSM)广泛的应用于现代通信系统就在于其良好的兼容性,不同的移动设备之间在遵守一定协议规范的条件下可以相互通信;本设计测试的是GSM第11系列GSM11.10,他包括诸多测试项,只对接收机参考灵敏度电平在GSM900与DCS1800两个频段进行测量。给出了传统形式下的手动测试和自动测试平台的比较,并建立了收信机参考灵敏度指标的自动测试平台。     

AUTOCAM简介及其初步使用的心得

一般来说,新闻直播中镜头是固定的,不需要太多的操作。如今,使用可远程遥控的摄像设备已成为一个热点。本文主要以东方卫视为例,从选型、使用及日常维护等方面,对对AUTOCAM的进行简单介绍。     

首钢中板厂矫直机控制系统

介绍了首钢中板厂矫直机技术指标、自动化系统构成及功能等，详细介绍了压下伺服电机变频控制系统在精确定位方面的应用。     

10MW高温气冷实验堆(HTR-10)燃耗测量系统控制方案的改进

基于10MW高温气冷实验堆(HTR-10)的FCA系统及CFC系统的设计原理及运行规程,在不改变FCA系统原有设备部件的前提下,对FCA系统运行逻辑关系进行了优化,改进了原燃耗测量程序,实现了燃耗测量过程的自动运行及测量结果的自动建库.在此基础上,设计了CFC系统与FCA系统PLC的通信协议,实现了燃耗测量流程与控制系统的实时数据通信.上述改进的结果使得燃料装卸流程不再需要另设运行班组,提高了效率,将人为操作的步骤最少化,降低了误操作的可能性.     

四种别藻蓝蛋白三聚体的时间分辨荧光光谱研究

研究了从Ａｎａｂａｎａｖａｒｉｂｉｌｉｓ中提取的４种别藻蓝蛋白ＡＰＣＩ，ＡＰＣＩＩ，ＡＰＣＩＩ及ＡＰＣＢ三聚体的稳态光谱和皮秒荧光光谱。采用Ｍｏｎｔｅ－Ｃａｒｌｏ方法对瞬态荧光光谱进行拟合，实验结果表明：ＡＰＣＩ荧光有两个带，其中第一个带位于６６２ｎｍ，有两个时间组分：３５．８ｐｓ和１．６７ｎｓ；第二个带位于６８０ｎｍ，有两个时间组分：３４．２ｐｓ和１．６４ｎｓ；ＡＰＣＩＩ瞬态荧光位于６６０ｎｍ，有两个时间组分：２０．４ｐｓ和１．６４ｎｓ；ＡＰＣＩＩ瞬态荧光位于６６０ｎｍ，有两个时间组分：２３．８ｐｓ和１．７６ｎｓ；ＡＰＣＢ瞬态荧光有两个带，其中第一个带位于６６２ｎｍ，有两个时间组分：３６．６ｐｓ和１．４５ｎｓ；第二个带位于６８０ｎｍ，有两个时间组分：２５．８ｐｓ和１．６２ｎｓ。实验结果一方面说明了藻胆体核内４种别藻蓝蛋白形成能量传递的两条途径；另一方面瞬态荧光解叠结果揭示了ＡＰＣＩ和ＡＰＣＢ三聚体内能量传递的超快过程。     

Household energy consumption versus income and relative standard of living: A panel approach

Our fundamental premise is that energy consumption at the household level is a key indicator of standard of living. We employ state-of-the-art panel cointegration techniques to evaluate the nature of the relationship between income measures and energy consumption measures for seven East Indian Ocean countries. The general finding is that income and household electricity consumption are not cointegrated. Given this finding, we conclude that standard of living measures that rely on income measures and do not include household-level energy consumption information will necessarily miss important indications of both levels and changes of standard of living.     

200kA预焙槽节能降耗的几点尝试

通过对200kA预焙槽节能方面做的几点尝试，探索出了200kA预焙电解槽在节约能源方面的措施，并取得了较好的节能效果。     

稳定同位素井间示踪技术在深层块状稠油油藏水驱特征研究的应用

经对冷43块深层块状普通稠油水驱注水5个试验井组开展的稳定同位素示踪测试，利用中子活化技术分析样品，采用先进的示踪剂定量分析与流动模拟相互结合的方法，以示踪数值模拟为手段，评价了油井连通、油层平面及纵向上的非均质性、隔层的封隔性等因素对水驱控制程度及动用状况的影响，通过优化注水推进方向及速度，强化动态调整措施，提高了稳产基础。     

西门子PLC与计算机间的通讯程序设计

介绍了西门子（Siemens）公司生产的S7－200型PLC与计算机之间的通讯网络构成及主要通讯指令，说明了利用PLC进行通信的实质和设计步骤，给出了PLC与计算机通讯时上位机和下位机的相应程序。