Efficient three-component one-pot synthesis of steroidal polysubstituted anilines

Zhang, Yanling; Li, Yafei; Shi, Yun-Kai; Zhang, Guochen; Qi, Ping; Fu, Dong-Jun; Shan, Lihong

doi:10.1016/j.steroids.2015.07.005

Cited by 16 publications

(3 citation statements)

References 36 publications

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“…All the synthesised sulfonamide-1,2,3-triazole derivatives bearing a dithiocarbamate moiety 8a-i were evaluated for their cytotoxic activity in vitro against three cancer cell lines, MGC-803 (human gastric cancer cell line), EC-109 (human esophageal cancer cell line) and PC-3 (human prostate cancer cell line), using the MTT assay method and compared with the well-known anticancer drug 5-fluorouracil. 15 The antiproliferative activity results are shown in Table 1. All compounds exhibited moderate antiproliferative activity against at least one of the three selected cancer cell lines.…”

Section: Resultsmentioning

confidence: 99%

Design and Synthesis of Sulfonamide-1,2,3-Triazole Derivatives Bearing a Dithiocarbamate Moiety as Antiproliferative Agents

Liu

Yang

et al. 2017

Journal of Chemical Research

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A series of nine novel 1-(4′-sulfamoylphenyl)-1,2,3-triazole derivatives bearing a 4-dithiocarbamylmethyl moiety were designed using the molecular hybridisation approach and synthesised by alkyne/azide click chemistry. Most of the synthesised compounds exhibited moderate to good antiproliferative activity against oesophagus, gastric and prostate cancer cell lines, but a compound containing a 4-( t-butoxycarbonyl)piperazinylthiocarbonyl moiety showed the highest activity. Against a prostate cancer cell line, it had an IC50 value of 2.4 μM, about 10-fold more active than 5-flurouracil. This work shows that novel sulfonamide-1,2,3-triazole derivatives bearing a dithiocarbamate moiety linked to a 4-substituted piperazine are promising lead compounds for the development of antitumour agents.

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Section: Resultsmentioning

confidence: 99%

Design and Synthesis of Sulfonamide-1,2,3-Triazole Derivatives Bearing a Dithiocarbamate Moiety as Antiproliferative Agents

Liu

Yang

et al. 2017

Journal of Chemical Research

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“…Research has investigated their effects on the torsional behavior of these girders, including the impact of spacing, location, and number on stiffness, stress, and strain. (Zhang et al, 2015). Choi et al (Choi et al, 2014) carried out examinations to clarify the effects of the web’s distortional stiffness and the number of diaphragm supports.…”

Section: Introductionmentioning

confidence: 99%

Torsional behavior of curved concrete box beam with small radius

Jiang,

Wang,

Nie

et al. 2023

Advances in Structural Engineering

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Curved concrete box beams are commonly used for their superior integrality performance and greater torsional stiffness. This paper investigates the torsional behavior of these beams using both experimental and finite element analyses. The experiment is based on a 1:6 scale model of a three-span curved girder bridge with a small radius. The study examines six different load cases, including central vertical and eccentric vertical loads. The study reports the detailed reaction forces of the supports, as well as the displacements and strains of the mid-span section. Finite element models are established to analyze the warping behavior of the curved concrete box beams. Based on the experimental and FEM analysis, the following conclusions are noted. Firstly, in the central load case, the strain of the curved concrete box girder is close to a straight line, so the curved concrete box girders follows the plane-section assumption. Besides, the warping normal stress is produced in curved concrete box girder in eccentric load cases. Moreover, the ratio of warping normal stress to bending normal stress is smaller and smoother in the section with diaphragms than that without diaphragms. And this ratio decreases with an increase in the curvature radius and diaphragm number. This study contributes to the theoretical and numerical modeling of a large span curved girder bridge with a small radius.

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“…However, their detailed mechanisms of action are less studied. In continuation with our previous interest in identifying potent anticancer agents, we screened our in-house steroid-based molecular library using the MTT assay [14][15][16][17][18][19][20][21][22][23][24], leading to the identification of a structurally symmetric [1,2,4] triazolo [1,5-a] pyrimidine-based steroidal dimer (named by001) having potent antiproliferative activity against several human cancer cell lines, remarkably more potent than its analogs previously synthesized in our group (Fig. 1).…”

Section: Introductionmentioning

confidence: 99%

Steroidal Dimer by001 Inhibits Proliferation and Migration of Esophageal Cancer Cells via Multiple Mechanisms

Wang¹,

Zhou²,

Shi³

et al. 2017

Preprint

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Following our previous success in identifying new steroid-based anticancer agents, we herein disclosed the structural requirements for retaining high potency against cancer cells and associated modes of action. The structurally novel steroidal dimer by001 inhibited growth of different esophageal cancer cells and colony formation at low micromolar levels, elevated cellular ROS levels and caused mitochondrial dysfunction. Mechanistic studies showed that by001 induced cell death through the mitochondria and death receptor-mediated apoptotic pathways and autophagy induction, as well as inhibited migration.

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Efficient three-component one-pot synthesis of steroidal polysubstituted anilines

Cited by 16 publications

References 36 publications

Design and Synthesis of Sulfonamide-1,2,3-Triazole Derivatives Bearing a Dithiocarbamate Moiety as Antiproliferative Agents

Design and Synthesis of Sulfonamide-1,2,3-Triazole Derivatives Bearing a Dithiocarbamate Moiety as Antiproliferative Agents

Torsional behavior of curved concrete box beam with small radius

Steroidal Dimer by001 Inhibits Proliferation and Migration of Esophageal Cancer Cells via Multiple Mechanisms

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