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Deep Regression for Precise Geometric Dimension Measurement
Thang Duong Nhat,Binh Nguyen Duc,Phuong Le Khac,Ngoc Tu Nguyen,Mai Nguyen Thi Phuong 한국정밀공학회 2019 한국정밀공학회지 Vol.36 No.8
A planar-dimensions vision measurement method is proposed by developing a Neural Network to measure real-world distance between any two points on the plane. The system leveraging Neural Network ability to search in the solution space is a highly non-linear model that could map points’ location on the pixel plane of image(s) with the actual distance between them considering the non-uniform geometric distortion in captured images caused by the entocentric lens in a common camera. The method was tested with a printed calibration chessboard, placed in different locations on the plane, with measured distance between tested points. Experimental results show the proposed method’s mean absolute error is 1.24 × 10-2 mm and standard deviation is 1.63 × 10-3 mm, tested with 10-folds cross-validation method.
Hieu, Doan Thanh,Anh, Duong Tien,Tuan, Nguyen Minh,Hai, Pham-The,Huong, Le-Thi-Thu,Kim, Jisung,Kang, Jong Soon,Vu, Tran Khac,Dung, Phan Thi Phuong,Han, Sang-Bae,Nam, Nguyen-Hai,Hoa, Nguyen-Dang Elsevier 2018 Bioorganic chemistry Vol.76 No.-
<P><B>Abstract</B></P> <P>In our search for novel small molecules targeting histone deacetylases, we have designed and synthesized several series of novel <I>N</I>-hydroxybenzamides/<I>N</I>-hydroxypropenamides incorporating quinazolin-4(3<I>H</I>)-ones (<B>4a-h</B>, <B>8a-d, 10a-d)</B>. Biological evaluation showed that these hydroxamic acids were generally cytotoxic against three human cancer cell lines (SW620, colon; <I>PC</I>-3, prostate; NCI-H23, lung cancer). It was found that the <I>N</I>-hydroxypropenamides (<B>10a-d)</B> were the most potent, both in term of HDAC inhibition and cytotoxicity. Several compounds, e.g. <B>4e</B>, <B>8b-c</B>, and <B>10a-c</B>, displayed up to 4-fold more potent than SAHA (suberoylanilide hydroxamic acid, vorinostat) in term of cytotoxicity. These compounds also comparably inhibited HDACs with IC<SUB>50</SUB> values in sub-micromolar range. Docking experiments on HDAC2 isozyme revealed some important features contributing to the inhibitory activity of synthesized compounds, especially for propenamide analogues. Importantly, the free binding energy computed was found to have high quantitative correlation (<I>R</I> <SUP>2</SUP> ∼ 95%) with experimental results.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Novel quinazolin-4(3H)-one-based <I>N</I>-hydroxybenzamides/<I>N</I>-hydroxypropenamides were synthesized. </LI> <LI> The <I>N</I>-hydroxybenzamides/<I>N</I>-hydroxypropenamides exhibited potent HDAC inhibition. </LI> <LI> The <I>N</I>-hydroxybenzamides/<I>N</I>-hydroxypropenamides exhibited good cytotoxicity. </LI> <LI> Docking studies and ADMET estimation were carried out. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>Two series of novel, simple <I>N</I>-hydroxybenzamides/<I>N</I>-hydroxypropenamides incorporating quinolin-4(3H)-one (<B>4a-h</B>, <B>8a-d, 10a-d</B>) were designed and synthesized. Biological evaluation showed that these benzamides/propenamides potently inhibited HDAC with IC<SUB>50</SUB> values in sub-micromolar range. A number of compounds also exhibited cytotoxicity up to 4-fold more potent than SAHA, a positive control.</P> <P>[DISPLAY OMISSION]</P>