Podophyllotoxin (PPT, 1) is a phenyltetralin-type of lignan which is widely distributed in higher plants. As a result of the development of etoposide (VP-16, 2) and teniposide (VM-26, 3) as anticancer drugs, semi-synthetic analogues of the naturally occurring PPT have drawn much renewed interest in recent years. It is believed that such analogues of 4Ј-demethylepipodophyllotoxin exert their cytotoxic, antitumor activity through stabilization of a cleavable complex between DNA and type II DNA topoisomerase. This leads ultimately to inhibition of DNA catenation activity and produces single and double strand breaks.1-3) Meanwhile, It has been reported that deoxypodophyllotoxin (DPT, 4) has insecticidal, [4][5][6] phytogrowth inhibitory and ichthytoxic activities. 7)As regards the insecticidal activity, it was confirmed that the symptoms caused by DPT developed slowly; namely, DPT is a delayed toxicant. 4,8,9) This conclusion was supported by the finding that the action of DPT on the 5th instar larvae of silkworm, Bombyx mori LINNE, involved severe damage to the epidermal cells accompanied with coagulation of the chromatin.6) Meanwhile, it was reported that the trans-lactone and the 4Ј-OCH 3 groups in the PPT derivatives were essential to keep the insecticidal activity. 4,10) But up to the present, there has been few reports that deal with insecticidal activity and structure-insecticidal activity relationship studies of PPT analogues. [11][12][13] According to the known structure-activity relationship on the medical research and our previous studies, [14][15][16][17][18][19][20] we found that replacement of the 4b-O-glucosidic substituent of compound 2 with 4b-halogenated anilino moiety yielded a number of compounds which were as potent or more potent than 2 in inhibiting the human DNA topoisomerase II and causing cellular protein-linked DNA breakage because the basic nitrogen and the aromatic ring might cause a bond delocalization to generate a charged 4b-N atom. Considering 4b-halogenated benzoylamino moiety might cause a bond delocalization to generate a more stable benzyl onium ion than 4b-halogenated anilino moiety, thereby allowing the alkylation of the target enzyme to occur and causing protein linked DNA breakage, so we herein, in order to find the more potent compounds than PPT, introduced halogenated benzoylamino moiety into PPT at the C-4b position and have synthesized twelve novel 4b-halogenated benzoylamino compounds 7.1-7.12. The insecticidal activity of these new compounds was tested in vivo against the 5th instar larvae of Pieris rapae LINNAEUS. ExperimentalAll melting points were taken on a Kofler melting point apparatus and uncorrected. IR spectra were obtained on a NIC-5DX spectrophotometer.1 H-NMR spectra were obtained by using either a Bruker AM-400 or AC-80 NMR spectrometer. In all cases, samples were dissolved in deuterochloroform and all chemical shifts were reported in ppm from tetramethylsilane (TMS). The elemental analyses were determined on a Carlo Elba 1106 instrument, mass spectral anal...
Speeded-Up Robust Features (SURF) is a novel scale-invariant and rotation-invariant feature. It is perfect in its high computation speed and robustness.In this paper, we apply SURF in SAR image matching accord to its characteristic, and then acquire its invariant feature for matching in an addition of no any pre-processing. In the process of image matching, we use the nearest neighbor rule for initial matching, whereafter, remove the wrong points of the matches through RANSAC. All this method was called R-SURF (RANSAC-SURF).In this method, the threshold range of the nearest neighbor rule has been obtained with our experiment .Experimental results indicated that the threshold interval was [0. 6~0.7], and the threshold that you choose in this interval, increased little matching time, but got more than 95% correct matching rate. We used three different types of SAR images in experiments which are in order to put to the proof that SURF is more robust in scale change, rotation change and noise.
Abstract. An approach for reconstructing wireframe models of curvilinear objects from three orthographic views is discussed. Our main stress is on the method of generating three-dimensional (3D) conic edges from twodimensional (2D) projection conic curves, which is the pivotal work for reconstructing curvilinear objects from three orthographic views. In order to generate 3D conic edges, a five-point method is firstly utilized to obtain the algebraic representations of all 2D projection curves in each view, and then all algebraic forms are converted to the corresponding geometric forms analytically. Thus the locus of a 3D conic edge can be derived from the geometric forms of the relevant conic curves in three views. Finally, the wireframe model is created after eliminating all redundant elements generated in previous reconstruction process. The approach extends the range of objects to be reconstructed and imposes no restriction on the axis of the quadric surface.
Change point detection is widely used in signal detection, industrial engineering, economy, finance, biomedicine and many other fields. The widely used parametric methods require prior knowledge of the noise signal distribution, which are seldom realistic. In practice, when the distribution of noise is not known, it is desirable to design algorithms based on non-parametric statistics, which, in the null case (no change point), are completely distribution free. To this end, we propose to use two symmetric sliding windows to compute the Area Under the receiver operating characteristic Curve (AUC) as a test statistic to measure the difference between the distribution of two samples. In the stage of change point detection, a threshold is designed according to hypothesis test which is based on the null distribution of the test statistics. This threshold is used to detect the potential change points in the signal. To reduce the probability of false alarm detection, a key parameter K is set to distinguish and delete the false alarms in potential change points. Comparative studies showed that our proposed method outperforms the classical Relative unconstrained Least-Squares Importance Fitting (RuLSIF) algorithm and is also better than the Hawkins, Qiu, and Kang (HQK) algorithm when the noise follows non-normal distributions.
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