In this paper, we described the synthesis of 2-aminoflfiazole sublibrary containing methyl, bromo, phenylor butylidene at 4- or/and 5-position of its core. All target compounds were evaluated tbr their antitumor activ...In this paper, we described the synthesis of 2-aminoflfiazole sublibrary containing methyl, bromo, phenylor butylidene at 4- or/and 5-position of its core. All target compounds were evaluated tbr their antitumor activitiesagainst human lung cancer cell line H1299 and human glioma cell line SHG-44. Among the compotmds screened,4,5,6,7-tetrahydrobenzo[d]thiazole（26b） exhibited the most potent antittunor activities with IC50 values of 4.89 and4.03 μmol/L against the two tested cell lines, respectively. Preliminary structure-activity relationship（SAR） studies ofthese compound were subsequently investigated.展开更多
For projects with thousands of files, finding the locations of bugs is time-consuming and labor-intensive. Bug reports as a potential resource to help locate bugs in source codes have been used to design automatic too...For projects with thousands of files, finding the locations of bugs is time-consuming and labor-intensive. Bug reports as a potential resource to help locate bugs in source codes have been used to design automatic tools to solve this problem. Existing information retrieval(IR)-based bug localization methods rely heavily on the similarity score between bug report and historical reports. As deep learning methods show great advantages in calculating text semantic similarity, we adapt the transformer network with IR-based bug localization methods to design a novel approach, TSLocator, to bug localization. In TSLocator, we propose five new features between bug reports and source codes. We use SVMRank to model the relation between all the six features and the actual buggy file. Given a new bug report, TSLocator automatically calculates the features and linearly weights the features to produce a suspicious score for all candidate files. TSLocator recommends a list of suspicious buggy files ranked by the score. The experimental results show that TSLocator outperforms existing methods in accuracy and performance of bug localization.展开更多
Based on the hit 5-hydroxy-2-methyl-10-propyl-2,3-dihydro-4H,8H-pyrano[2,3-j]chromene-4,8-dione（1）, a series of pyrano[2,3-f]chromene-4,8-dione derivatives was designed and synthesized using pb_loroghicinol as start...Based on the hit 5-hydroxy-2-methyl-10-propyl-2,3-dihydro-4H,8H-pyrano[2,3-j]chromene-4,8-dione（1）, a series of pyrano[2,3-f]chromene-4,8-dione derivatives was designed and synthesized using pb_loroghicinol as startingmaterial. Meanwhile, a regioselective synthetic route was developed for 5-methoxy-2,3-dihydro-4H,8H-pyrano-[2,3-f]chromene-4,8-dione products（11a-11f）, and their structures were further confirmed by nuclear Overhausereffect（NOE）. The evaluation of anticancer activities of these compounds against four human cancer cell lines,including human glioma cell line （SHG-44）, human lung cancer cell line（H1299）, breast cancer cell line（/vICF7） andhuman colon carcinoma cell line（HCT-116） in vitro shows that 5-methoxy-2,2-dimethyl-9-chloro-10-trifluormethyl-2,3-dihydro-4H,8H-pyrano[2,3-f]chromene-4,8-dione（lle） possesses the best anticancer activities with IC50 values of6.68, 7.90, 5.16 and 4.82 gmol/L, respectively. Finally, the preliminary structure-activity relationships（SARs） weresttmmarized, which could pave the way for generating more potent anticancer agents with drug-like properties.展开更多
文摘In this paper, we described the synthesis of 2-aminoflfiazole sublibrary containing methyl, bromo, phenylor butylidene at 4- or/and 5-position of its core. All target compounds were evaluated tbr their antitumor activitiesagainst human lung cancer cell line H1299 and human glioma cell line SHG-44. Among the compotmds screened,4,5,6,7-tetrahydrobenzo[d]thiazole（26b） exhibited the most potent antittunor activities with IC50 values of 4.89 and4.03 μmol/L against the two tested cell lines, respectively. Preliminary structure-activity relationship（SAR） studies ofthese compound were subsequently investigated.
文摘For projects with thousands of files, finding the locations of bugs is time-consuming and labor-intensive. Bug reports as a potential resource to help locate bugs in source codes have been used to design automatic tools to solve this problem. Existing information retrieval(IR)-based bug localization methods rely heavily on the similarity score between bug report and historical reports. As deep learning methods show great advantages in calculating text semantic similarity, we adapt the transformer network with IR-based bug localization methods to design a novel approach, TSLocator, to bug localization. In TSLocator, we propose five new features between bug reports and source codes. We use SVMRank to model the relation between all the six features and the actual buggy file. Given a new bug report, TSLocator automatically calculates the features and linearly weights the features to produce a suspicious score for all candidate files. TSLocator recommends a list of suspicious buggy files ranked by the score. The experimental results show that TSLocator outperforms existing methods in accuracy and performance of bug localization.
文摘Based on the hit 5-hydroxy-2-methyl-10-propyl-2,3-dihydro-4H,8H-pyrano[2,3-j]chromene-4,8-dione（1）, a series of pyrano[2,3-f]chromene-4,8-dione derivatives was designed and synthesized using pb_loroghicinol as startingmaterial. Meanwhile, a regioselective synthetic route was developed for 5-methoxy-2,3-dihydro-4H,8H-pyrano-[2,3-f]chromene-4,8-dione products（11a-11f）, and their structures were further confirmed by nuclear Overhausereffect（NOE）. The evaluation of anticancer activities of these compounds against four human cancer cell lines,including human glioma cell line （SHG-44）, human lung cancer cell line（H1299）, breast cancer cell line（/vICF7） andhuman colon carcinoma cell line（HCT-116） in vitro shows that 5-methoxy-2,2-dimethyl-9-chloro-10-trifluormethyl-2,3-dihydro-4H,8H-pyrano[2,3-f]chromene-4,8-dione（lle） possesses the best anticancer activities with IC50 values of6.68, 7.90, 5.16 and 4.82 gmol/L, respectively. Finally, the preliminary structure-activity relationships（SARs） weresttmmarized, which could pave the way for generating more potent anticancer agents with drug-like properties.
