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Article

Design, Syntheses, and Bioevaluations of Some Novel N2-Acryloylbenzohydrazides as Chemostimulants and Cytotoxic Agents

1
Drug Discovery and Development Research Cluster, College of Pharmacy and Nutrition, University of Saskatchewan, 107 Wiggins Road, Saskatoon, SK S7N 5E5, Canada
2
Department of Biological Sciences, Border Biomedical Research Center, The University of Texas at El Paso, 500 West University Avenue, El Paso, TX 79968-0519, USA
3
Department of Pathology and Laboratory Medicine, University of Saskatchewan, 107 Wiggins Road, Saskatoon, SK S7N 5E5, Canada
*
Authors to whom correspondence should be addressed.
Academic Editor: Hiroshi Sakagami
Medicines 2021, 8(6), 27; https://doi.org/10.3390/medicines8060027
Received: 13 May 2021 / Revised: 29 May 2021 / Accepted: 29 May 2021 / Published: 3 June 2021
A series of novel N2-acryloylhydrazides 1a–m and a related series of compounds 6a–c were prepared as potential chemostimulants. In general, these compounds are cytotoxic to human HCT 116 colon cancer cells, as well as human MCF-7 and MDA-MB-231 breast cancer cell lines. A representative compound N1-(3,4-dimethoxyphenylcarbonyl)-N2-acryloylhydrazine 1m sensitized HCT 116 cells to the potent antineoplastic agent 3,5-bis(benzylidene)-4-piperidone 2a, and also to 5-fluorouracil. A series of compounds was prepared that incorporated some of the molecular features of 2a and related compounds with various N2-acryloylhydrazides in series 1. These compounds are potent cytotoxins. Two modes of action of representative compounds are the lowering of mitochondrial membrane potential and increasing the concentration of reactive oxygen species. View Full-Text
Keywords: acryloylhydrazides; cytotoxins; chemosensitization; antineoplastic agents; mitochondrial membrane potential; reactive oxygen species acryloylhydrazides; cytotoxins; chemosensitization; antineoplastic agents; mitochondrial membrane potential; reactive oxygen species
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MDPI and ACS Style

Lakhani, K.; Borrego, E.A.; Cano, K.G.; Dimmock, J.R.; Aguilera, R.J.; Das, S.; Roayapalley, P.K.; Sharma, R.K.; Das, U. Design, Syntheses, and Bioevaluations of Some Novel N2-Acryloylbenzohydrazides as Chemostimulants and Cytotoxic Agents. Medicines 2021, 8, 27. https://0-doi-org.brum.beds.ac.uk/10.3390/medicines8060027

AMA Style

Lakhani K, Borrego EA, Cano KG, Dimmock JR, Aguilera RJ, Das S, Roayapalley PK, Sharma RK, Das U. Design, Syntheses, and Bioevaluations of Some Novel N2-Acryloylbenzohydrazides as Chemostimulants and Cytotoxic Agents. Medicines. 2021; 8(6):27. https://0-doi-org.brum.beds.ac.uk/10.3390/medicines8060027

Chicago/Turabian Style

Lakhani, Kinjal, Edgar A. Borrego, Karla G. Cano, Jonathan R. Dimmock, Renato J. Aguilera, Swagatika Das, Praveen K. Roayapalley, Rajendra K. Sharma, and Umashankar Das. 2021. "Design, Syntheses, and Bioevaluations of Some Novel N2-Acryloylbenzohydrazides as Chemostimulants and Cytotoxic Agents" Medicines 8, no. 6: 27. https://0-doi-org.brum.beds.ac.uk/10.3390/medicines8060027

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