Anticancer SAR establishment and novel accruing signal transduction model of drug action using biscoumarin scaffold

In this paper, we have established methylenebis (4-hydroxy-2H-chromen-2-one) as a promising anticancer scaffold with kinesin spindle protein (KSP) inhibitory activity under malignant condition. A series of biscoumarin derivatives (MN1 to MN30) with different substituent were synthesized, and their anticancer activity was explored. Six biscoumarin derivatives that were found active were further selected to formulate organic nanoparticles (ONPs). Anticancer activity of both the forms (viz conventional and ONPs) was compared. MN30 was found most potent whereby MN10 showed good anticancer activity in both, i.e., conventional and ONP form; the structural activity relationship (SAR) study has been established. Computational investigation revealed biscoumarin scaffold as a suitable pharmacophore to bind against KSP protein. Molecular dynamics simulation studies revealed protein-ligand stability and dynamic behavior of biscoumarin-KSP complex. Finally, accruing signal transduction model was formulated to explain the observed MTT trend of conventional and ONP form. The model seems useful towards solving population specific varied results of chemotherapeutic agents. According to the model, MN10 and MN30 derivatives have good pharmacodynamics inertia and therefore, both the molecules were able to provide dose-dependent cytotoxic results.     

气垫导轨在刚体转动惯量测定实验中的应用

本文介绍了一种测量刚体转动惯量的新方法。即把气垫导轨和刚体转动仪结合起来来测量刚体的转动惯量,使传统的气垫导轨实验和刚体转动惯量测定实验得以更新,提高了实验测量的精度,拓展了实验内容。     

滚动实验的另一种演示

介绍了另一种滚动演示实验,并对演示结果进行了理论分析和解释     

190区超形变核中转动带的组态结构

通过系统研究A～190区超形变核中转动带的转动惯量、角动量顺排、旋称分裂随转动频率的变化规律, 结合我们用处理对力的粒子数守恒方法的计算结果, 对A～190区所有转动带的组态结构给出了一个整体的描述. 绝大多数超形变带都建立在强耦合轨道上, 例如中子[512]5/2, [624]9/2. 少数超形变带则建立在高j闯入轨道上, 即中子[761]3/2, [752]5/2. 根据我们提出的组态结构所进行的理论计算结果表明, A～190区所有转动带的一般行为、反常变化和带交叉都得到了满意的解释.     

19F+27Al耗散反应中双核系统的转动与形变

测量了¹⁹F+²⁷Al耗散反应产物B,C,N,O,F和Ne的激发函数,入射束流的能量从110.25MeV到118.75MeV, 能量步长为250keV. 从产物的 能量自关联函数中提取了反应中所形成的中间双核系统的转动惯量, 与相粘模型计算的刚体转动惯量相比较, 结果表明形成的双核系统有大的形变.     

关于奇ATm核1/2+[411]转动带的系统分析

壳模型计算表明,1/2⁺[411]出现于¹⁵⁷Tm核的基态可能是由非轴对称形变造成的.但是新近从¹⁵⁷Yb衰变纲图给出的¹⁵⁷Tm低激发谱中,指认了一个建立在1/2⁺[411]带头上的基态转动带,并认为该带的性质是轴对称的,提取了该带的惯性参数与脱耦合参数.通过对奇ATm核1/2⁺[411]转动带的系统分析,强调了在¹⁵⁷Tm核中非轴对称γ自由度效应的重要性.     

摩擦离合器的数学模型及其算例

用力学分析的方法 ,建立了摩擦离合器的数学模型 ,求出了摩擦离合器中扭力弹簧的圈数 ,其计算值与实际值基本一致 .该模型对摩擦离合器的设计有一定的参考价值 .     

切变模量和转动惯量实验的改进

设计了一种基于垂直轴定理的新型吊钩,对切变模量和转动惯量实验进行了改进,使之成为既可测定金属丝切变模量和环、柱等刚体的转动惯量,又可验证反映转动惯量重要性质的平行轴定理及垂直轴定理的多功能实验仪.     

钢丝的切变模量与扭转角度关系

研究了钢丝的切变模量随其扭转角度变化而变化的情况,观察到扭转角大于某一角度时,切变模量趋于定值的规律,得出扭摆实验准确测量的方法.     

全同超形变带转动惯量的粒子数守恒计算

利用推转壳模型的粒子数守恒方法计算了超形变(SD)转动带¹⁹²Hg和¹⁹⁴Hg(1,2,3)的带首转动惯量.分析了带首附近的组态结构及带首转动惯量随对力强度的变化.带首转动惯量之差δJ₀对对力强度十分敏感,而对Nilsson能级参数K、μ及形变参数并不敏感.对力及堵塞效应是造成带首转动惯量差别的主要因素.但与正常形变核相比,对力强度似有较大程度减弱.