Akama, Tsutomu Freund, Yvonne R. Berry, Pamela W. Carter, David S. Easom, Eric E. Jarnagin, Kurt Lunde, Christopher S. Plattner, Jacob J. Rock, Fernando Stefanakis, Rianna
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Published in
ACS Infectious Diseases
A series of benzimidazole–benzoxaborole hybrid molecules linked via an amide linker are described that exhibit good in vitro activity against Onchocerca volvulus , a filarial nematode responsible for the disease onchocerciasis, also known as river blindness. The lead identified in this series, 8a (AN8799), was found to have acceptable pharmacokine...
Carter, David S. Jacobs, Robert T. Freund, Yvonne R. Berry, Pamela W. Akama, Tsutomu Easom, Eric E. Lunde, Christopher S. Rock, Fernando Stefanakis, Rianna McKerrow, James
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Published in
ACS Infectious Diseases
The optimization of a series of benzimidazole–benzoxaborole hybrid molecules linked via a ketone that exhibit good activity against Onchocerca volvulus , a filarial nematode responsible for the disease onchocerciasis, also known as river blindness, is described. The lead identified in this series, 21 (AN15470), was found to have acceptable pharmaco...
Yu, Chen Guang Bondada, Vimala Ghoshal, Sarbani Singh, Ranjana Pistilli, Christina K Dayaram, Kavi Iqbal, Hina Sands, Madison Davis, Kate L Bondada, Subarrao
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Published in
Journal of neurotrauma
We previously reported the serendipitous observation that fenbendazole, a benzimidazole anthelmintic, improved functional and pathological outcomes following thoracic spinal cord contusion injury in mice when administered pre-injury. Fenbendazole is widely used in veterinary medicine. However, it is not approved for human use and it was uncertain i...
Kubíček, Vladimír Skálová, Lenka Skarka, Adam Králová, Věra Holubová, Jana Štěpánková, Jana Šubrt, Zdeněk Szotáková, Barbora
Published in
Frontiers in pharmacology
Flubendazole (FLU), an anthelmintic drug of benzimidazole type, is now considered a promising anti-cancer agent due to its tubulin binding ability and low system toxicity. The present study was aimed at determining more information about FLU reduction in human liver, because this information has been insufficient until now. Subcellular fractions fr...
Tao, Jiali Zhao, Hongmei Xie, Xiaochen Luo, Man Gao, Zhiwei Sun, Hong Huang, Ziming
Published in
OncoTargets and therapy
Background and objectives The nuclear factor kappa B (NF-κB) signaling is activated in esophageal squamous cell carcinoma (ESCC) and can be used as a potential target for anti-ESCC drug discovery. In this study, we aimed to investigate the function of flubendazole as a novel NF-κB inhibitor in ESCC cells. Materials and methods Cell Counting Kit-8 a...
Hanušová, Veronika Skálová, Lenka Králová, Věra Matoušková, Petra
Published in
Anti-cancer agents in medicinal chemistry
Colon cancer is the most common type of gastrointestinal cancer. Despite advances during the last two decades, the efficacy of colorectal cancer treatment is still insufficient and new anticancer agents are necessary. In our study, colon cancer cells derived from a primary tumor (SW480) and lymph node metastasis (SW620) from the same patient were u...
Čáňová, Kristýna Rozkydalová, Lucie Rudolf, Emil
Published in
Acta medica (Hradec Kralove)
Flubendazole is a widely used anthelmintic drug belonging to benzimidazole group. The molecular mechanism of action of flubendazole is based on its specific binding to tubulin, which results in disruption of microtubule structure and function, and in the interference with the microtubule-mediated transport of secretory vesicles in absorptive tissue...
Vialpando, Monica Smulders, Stefanie Bone, Scott Jager, Casey Vodak, David Van Speybroeck, Michiel Verheyen, Loes Backx, Katrien Boeykens, Peter Brewster, Marcus E
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Published in
Journal of pharmaceutical sciences
This study investigates 3 amorphous technologies to improve the dissolution rate and oral bioavailability of flubendazole (FLU). The selected approaches are (1) a standard spray-dried dispersion with hydroxypropylmethylcellulose (HPMC) E5 or polyvinylpyrrolidone-vinyl acetate 64, both with Vitamin E d-α-tocopheryl polyethylene glycol succinate; (2)...
Hou, Zhi-Jie Luo, Xi Zhang, Wei Peng, Fei Cui, Bai Wu, Si-Jin Zheng, Fei-Meng Xu, Jie Xu, Ling-Zhi Long, Zi-Jie
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Published in
Oncotarget
Cancer stem-like cell (CS-like cell) is considered to be responsible for recurrence and drug resistance events in breast cancer, which makes it a potential target for novel cancer therapeutic strategy. The FDA approved flubendazole, has been widely used in the treatment of intestinal parasites. Here, we demonstrated a novel effect of flubendazole o...
Vandenberge, V Delezie, E Delahaut, P Pierret, G De Backer, P Daeseleire, E Croubels, S
Published in
Poultry science
Chemical residues may be present in eggs from laying hens' exposure to drugs or contaminants. These residues may pose risks to human health. In this study, laying hens received experimental feed containing flubendazole or tylosin at cross contamination levels of 2.5, 5, and 10% of the therapeutic dose. Eggs were collected daily and analysis of the ...
