Anticancer agents are critical for the cancer treatment, but side effects and the drug resistance associated with the currently used anticancer agents create an urgent need to explore novel drugs ...with low side effects and high efficacy. 1,2,3-Triazole is privileged building block in the discovery of new anticancer agents, and some of its derivatives have already been applied in clinics or under clinical trials for fighting against cancers. Hybrid molecules occupy an important position in cancer control, and hybridization of 1,2,3-triazole framework with other anticancer pharmacophores may provide valuable therapeutic intervention for the treatment of cancer, especially drug-resistant cancer. This review emphasizes the recent advances in 1,2,3-triazole-containing hybrids with anticancer potential, covering articles published between 2015 and 2019, and the structure-activity relationships, together with mechanisms of action are also discussed.
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•1,2,3-Triazole drugs have already been used in clinics for cancer treatment.•1,2,3-Triazole-containing hybrids with potential anticancer activity.•The SAR was enriched.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
Human pose estimation is one of the key technologies in action recognition, motion analysis, human-computer interaction, animation generation etc. How to improve its performance has become a current ...research hotspot. Lite-HRNet establishes long range connections between keypoints and exhibits good performance in human pose estimation tasks. However, the scale of this method to extract features is relatively single and lacks sufficient information interaction channels. To solve this problem, we propose an improved lightweight high-resolution network based on multi-dimensional weighting, named MDW-HRNet, which is implemented by the following aspects: first, we propose global context modeling, which can learn multi-channel and multi-scale resolution information weights. Second, a cross-channel dynamic convolution module is designed, it performs inter-channel attention aggregation between dynamic and parallel kernels, replacing the basic convolution module. These make the network capable of channel weighting, spatial weighting and convolution weighting. At the same time, we simplify the network structure to perform information exchange and information compensation between high-resolution modules while ensuring speed and accuracy. Experimental results show that our method achieves good performance on both COCO and MPII human pose estimation datasets, and its accuracy surpasses mainstream lightweight pose estimation networks without increasing computational complexity.
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IZUM, KILJ, NUK, PILJ, PNG, SAZU, UL, UM, UPUK
Aiming at a series of problems such as detection accuracy, calculation blocking, display delay, and so on in the ship detection of surveillance video, an improved YOLOv5 algorithm is proposed in this ...paper. First, to improve the detection performance, it is proposed to optimize the anchor box algorithm in the YOLOv5 network according to the ship target characteristics. Then, the t‐SNE algorithm is used to reduce and visualize the data set label information and perform weighted analysis on the processed features for low‐dimensional data. The mapped kernel k‐means clustering algorithm adaptively selects a more appropriate anchor box and considers the detection performance of large and small ship targets. Secondly, to improve the problem of computational blocking and delay, the BN scaling factor γ is used to compress the YOLOv5 network, so that the model can be reduced without reducing the detection performance. The optimized YOLOv5 framework is trained on the self‐integrated data set. The accuracy of the algorithm is increased by 2.34%, and the ship detection speed reaches 98 fps and 20 fps in the server environment and the low computing power version (Jetson nano), respectively.
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FZAB, GIS, IJS, KILJ, NLZOH, NUK, OILJ, SAZU, SBCE, SBMB, UL, UM, UPUK
A series of diethylene glycol tethered ciprofloxacin–isatin hybrids 5a–j were designed, synthesized, and evaluated for their in vitro antimycobacterial activity against both drug‐sensitive and ...multidrug‐resistant (MDR) Mycobacterium tuberculosis strains in this paper. The preliminary results revealed that all hybrids with greater lipophilicity than the parent ciprofloxacin displayed considerable activity against the tested strains with minimum inhibitory concentration (MIC) in a range of 1.56–64 μg/mL. In particular, hybrid 5f (MIC: 1.56 and 2 μg/mL) with low cytotoxicity in VERO cell line was comparable with the parent ciprofloxacin (MIC: 0.78 and 2 μg/mL) against M. tuberculosis H37Rv and MDR tuberculosis strains and ≥16‐fold more potent than isoniazid and rifampicin (MIC: >128 and 32 μg/mL, respectively) against MDR tuberculosis, suggesting that it may serve as a new and promising candidate for further study.
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FZAB, GIS, IJS, IZUM, KILJ, NLZOH, NUK, OILJ, PILJ, PNG, SAZU, SBCE, SBMB, UL, UM, UPUK
A new class of istain dimers tethered by tetraethylene glycol was designed, synthesized, and evaluated for their in vitro anti‐mycobacterial activities against Mycobacterium tuberculosis H37Rv and ...multidrug‐resistant M. tuberculosis strains. Our results indicated that all the synthesized hybrids exhibited promising anti‐mycobacterial activities against the tested strains and the enriched structure–activity relationship may pave the way to further rational development of istain dimers with a unique mechanism of action different from that of the currently used drugs to overcome the resistance.
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FZAB, GIS, IJS, IZUM, KILJ, NLZOH, NUK, OILJ, PILJ, PNG, SAZU, SBCE, SBMB, UL, UM, UPUK
A series of diethylene glycol tethered bis‐istain derivatives 4 a‐o were designed, synthesized and screened for their biological activities in this paper. Eight bis‐isatin derivatives displayed ...broad‐spectrum activities against all tested drug‐sensitive and drug‐resistant cancer cells with IC50 in a range of 8.32 to 49.73 μM. The most active derivative 4 d was >2.5 folds more potent than etoposide against Hela, HCT‐116, A549 and drug‐resistant MCF‐7/DOX (Doxorubicin‐resistant MCF‐7) cells and was comparable to etoposide against DU145, SKOV3 and MCF‐7. Tubulin inhibitory results suggested that this kind of bis‐istain derivatives could exert their anti‐cancer activities through tubulin inhibition. The eight bis‐isatin derivatives with high anti‐tumor activity were selected for further screen to investigate their anti‐mycobacterial and anti‐HIV activities, but the majority of them only exhibited weak to moderate activities.
A series of diethylene glycol tethered bis‐istain derivatives were designed, synthesized and screened for their biological activities in this paper. Eight bis‐isatin derivatives displayed broad‐spectrum activity against all tested drug‐sensitive and drug‐resistant cancer cell lines, and tubulin inhibitory results suggested that this kind of bis‐istain derivatives could exert their anti‐cancer activities through tubulin inhibition. The eight bis‐isatin derivatives with high anti‐tumor activity were selected for further screened for their anti‐mycobacterial and anti‐HIV activities, but the majority of them only exhibited weak to moderate anti‐mycobacterial and anti‐HIV activities.
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FZAB, GIS, IJS, KILJ, NLZOH, NUK, OILJ, SAZU, SBCE, SBMB, UL, UM, UPUK
We report herein the design and synthesis of a series of novel tetraethylene glycol‐tethered isatin–1,2,3‐triazole–coumarin hybrids and evaluate their in vitro antitumor activities against seven ...common human cancer cell lines including drug‐resistant cell line. Results revealed that all the synthesized hybrids showed weak to moderate activities against the tested seven cancer cell lines. The structure–activity relationship was also discussed, and the enriched structure–activity relationship may pave the way for further rationale design of this kind of hybrids.
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FZAB, GIS, IJS, IZUM, KILJ, NLZOH, NUK, OILJ, PILJ, PNG, SAZU, SBCE, SBMB, UL, UM, UPUK
Herein, we report the design and synthesis of a new set of tetraethylene glycol tethered isatin–coumarin hybrids 7a–l as anticancer agents. Results revealed that all the synthesized hybrids showed no ...or weak activities against their in vitro antitumor activities against drug‐sensitive HepG2, Hela, A549, DU145, SKOV3, and MCF‐7 as well as drug‐resistant MCF‐7/DOX (doxorubicin‐resistant MCF‐7) human cancer cell lines. The structure–activity relationship was also discussed, and the enriched structure–activity relationship may pave the way for further rationale design of this kind of hybrids.
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FZAB, GIS, IJS, IZUM, KILJ, NLZOH, NUK, OILJ, PILJ, PNG, SAZU, SBCE, SBMB, UL, UM, UPUK
A new class of diethylene glycol tethered moxifloxacin–isatin hybrids 5a–l was designed, synthesized, and evaluated for their in vitro antimycobacterial activity against Mycobacterium tuberculosis ...(MTB) H37Rv and multidrug‐resistant tuberculosis (MDR‐TB) strains. Our results showed that all hybrids with higher lipophilicity than the parent moxifloxacin exhibited promising activity against the tested strains with minimum inhibitory concentration (MIC) in a range of 0.2–16 μg/mL. In particular, hybrid 5h (MIC: 0.20 and 0.5 μg/mL), which was found to be most active against MTB H37Rv and MDR‐TB, was twofold more potent than isoniazid (MIC: 0.39 μg/mL) against MTB H37Rv and ≥64‐fold more active than isoniazid and rifampicin (MIC: >128 and 32 μg/mL, respectively) against MDR‐TB.
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FZAB, GIS, IJS, IZUM, KILJ, NLZOH, NUK, OILJ, PILJ, PNG, SAZU, SBCE, SBMB, UL, UM, UPUK
We report herein the design, synthesis, and antimycobacterial activity of a series of diethylene glycol tethered gatifloxacin–isatin hybrids 5a–o in this paper. Results revealed that all hybrids ...showed promising activity against both drug‐sensitive and multidrug‐resistant Mycobacterium tuberculosis strains with minimum inhibitory concentration (MIC) in a range of 1–128 μg/mL. Particularly, hybrid 5j with low cytotoxicity in VERO cell line was comparable with the parent gatifloxacin (MIC: 0.78 and 1 μg/mL) against MTB H37Rv and MDR‐TB strains, and ≥32‐fold more potent than isoniazid and rifampicin (MIC: >128 and 32 μg/mL, respectively) against MDR‐TB, suggesting it may serve as a new and promising candidate for further study.
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FZAB, GIS, IJS, IZUM, KILJ, NLZOH, NUK, OILJ, PILJ, PNG, SAZU, SBCE, SBMB, UL, UM, UPUK
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