Chemistry of the pyrrolo[1,2-alpha]benzimidazole antitumor agents: influence of the 7-substituent on the ability to alkylate DNA and inhibit topoisomerase II

This study addresses the influence the 7-substituent on the cytotoxicity of pyrrolo[1,2-alpha]-benzimidazole quinones possessing a 6-aziridinyl group (PBIs) and a 6-acetamido group (APBIs). Reduction of a PBI to the aziridinyl hydroquinone results in both nucleophile trapping (alkylation) and 1,5-sigmatropic shift reactions. The latter process is essentially an internal redox reaction wherein the hydroquinone causes reductive opening of the aziridinyl ring. The 7-substituent controls the fate of the aziridinyl ring by means of steric and electronic effects. An electron-rich 7-substituent favors the 1,5-sigmatropic shift reaction. If the 7-substituent distorts the 6-aziridinyl group from the conformation required for the 1,5-sigmatropic shift, then nucleophile trapping occurs. The 7-methyl substituent results in significant nucleophilic trapping, and the 7-unsubstituted and 7-methoxy substituents favor the 1,5-sigmatropic reaction. Thus, the 7-methyl PBIs show the most cytotoxicity of the analogues studied. The APBIs are cytotoxic only as quinones, and reduction to the hydroquinone results in loss of activity. Consistent with this observation, the change from 7-methyl to the more electron-rich 7-methoxy results in a substantial loss of APBI cytotoxicity as well as decreased topoisomerase II inhibition. The mechanism of inhibition is thought to involve the interacalation of only electron deficient APBIs into DNA.     

Magnetization and rotation of MTG HTSC ring in magnetic field

The magnetization of a melt-texture growth (MTG) HTSC ring has been studied. It is shown that the magnetic field inside the ring is larger than the external field under a certain range of external magnetic fields. We have also investigated the magnetic field dependence of the response of a detective coil near a rotating superconducting ring. The responses of the MTG sample are different for different cooling methods.     

HA型粘结剂性能评判的研究

冷固结球团直接还原工艺成功的关键因素之一是成型粘结剂的选用。粘结剂性能评判 ,传统的方法是通过考查球团矿的机械强度来说明粘结剂性能的优劣 ,步骤繁锁。经过试验研究 ,本文提出了用粘度大小来评判粘结剂性能的直接方法并从理论上进行了论证。对于 HA型复合粘结剂 ,在六速旋转粘度计上测量 ,50 g复合粘结剂的粘度若大于或等于 6.5× 1 0 -3 Pa·s,表示粘结剂性能较好 ,能满足铁精矿冷固球团直接还原工艺的要求 ;若小于或等于 3.0× 1 0 -3 Pa· s,则表示该粘结剂性能较差。     

新疆伊犁托海水电站拱坝坝体变形监测分析

根据托海拱坝5号坝段、7号坝段例垂线实测资料分析，说明了新疆寒冷地区坝体采取聚胺脂喷涂施工措施后对坝体变形的影响，以及右坝肩渗漏对右坝肩岩体的影响，分析结果为托海水电站通过国家电力公司大坝安全监察中心大坝安全首次定检提供了科学依据。     

深基坑支护结构计算的有限元方法

针对软土地基的特性，本文提出了考虑土体抗力释放与结构模型随施工过程改变的新杆系有限元法，并 编制了求解支护结构内力与变形的计算程序，通过对事例分析．计算结果与实际情况非常吻合，证明了该方法的合理 性。     

液压系统广义可靠性设计

介绍了广义可靠性和有效度的基本概念，简要论述了对液压系统进行广义可靠性设计的重要性，并从可靠性设计和维修性设计两方面提出了提高液压系统有效度的具体措施。／     

氧化铝生产过程结疤溶解的研究

针对氧化铝生产过程结疤现象。研制出一种新型清洗溶剂，溶垢率可达95%，清洗效果达到《工业设备化学清洗质量标准》要求。     

深穿透复合射孔技术在中原油田的应用

深穿透复合射孔是一项把射孔与高能气体压裂两种技术有机地结合在一起的综合改造油气层的新技术。重点对它的技术原理，包括设计原理、枪身内火药燃烧气体对射孔孔眼的冲刷作用原理、火药燃烧气体射流的高能气体压裂作用原理等进行了研究与探讨，同时对它的施工工艺、现场应用等方面进行了阐述，经中原油田189口井现场应用证明，其工艺简便，成本低廉，可实现多层跨隔层使用，处理后增产效果显著，投入产出比高，可代替传统的聚能射孔技术，具有广阔的推广和应用价值。     

由乙腈一步法制备乙酸丁酯的研究

以丁醇和制备丙烯腈的副产物乙腈为原料 ,采用一步法合成了乙酸丁酯。通过正交实验得到了影响反应的 4种因素。确定了最佳的工艺条件为 :催化剂的量为样品质量的 40 % ;n(CH3CN)∶ n(C4 H9OH) =1∶ 1 .0 5 ;反应温度为 1 0 5℃ ;反应时间为 8h。在此反应条件下 ,乙酸丁酯的收率为 88.8% ,纯度可达 99.5 %。并用气相色谱及红外光谱对产品的纯度进行了表征