Design and synthesis of mono-and di-pyrazolyl-s-triazine derivatives, their anticancer profile in human cancer cell lines, and in vivo toxicity in zebrafish embryos

2019 ◽  
Vol 87 ◽  
pp. 457-464 ◽  
Author(s):  
Muhammad Farooq ◽  
Anamika Sharma ◽  
Zainab Almarhoon ◽  
Abudalla Al-Dhfyan ◽  
Ayman El-Faham ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Zebrafish Embryos ◽  
Human Cancer Cell ◽  
In Vivo Toxicity ◽  
Human Cancer Cell Lines ◽  
Design And Synthesis ◽  
Triazine Derivatives

scholarly journals The Design, Synthesis, and Evaluation of Hypoxia-Activated Prodrugs of the KDAC Inhibitor Panobinostat

2020 ◽  
Author(s):  
Ewen Calder ◽  
Anna Skwarska ◽  
Deborah Sneddon ◽  
Lisa Folkes ◽  
Ishna N. Mistry ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Parent Drug ◽  
Human Cancer Cell ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Design And Synthesis ◽  
Initial Validation

The design and synthesis of four hypoxia-activated prodrugs of the KDAC inhibitor panobinostat is described. Initial validation of these compounds using isolated enzymes, and in two human cancer cell lines, reveals that the nitroimidazole-based prodrug (NI-Pano, CH-03) undergoes efficient bioreduction and fragmentation to release the parent drug, panobinostat. NI-Pano was identified as the optimum compound for use in further studies in cells, spheroid tumor models, and <i>in vivo</i>.

scholarly journals The Design, Synthesis, and Evaluation of Hypoxia-Activated Prodrugs of the KDAC Inhibitor Panobinostat

2020 ◽  
Author(s):  
Ewen Calder ◽  
Anna Skwarska ◽  
Deborah Sneddon ◽  
Lisa Folkes ◽  
Ishna N. Mistry ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Parent Drug ◽  
Human Cancer Cell ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Design And Synthesis ◽  
Initial Validation

The design and synthesis of four hypoxia-activated prodrugs of the KDAC inhibitor panobinostat is described. Initial validation of these compounds using isolated enzymes, and in two human cancer cell lines, reveals that the nitroimidazole-based prodrug (NI-Pano, CH-03) undergoes efficient bioreduction and fragmentation to release the parent drug, panobinostat. NI-Pano was identified as the optimum compound for use in further studies in cells, spheroid tumor models, and <i>in vivo</i>.

scholarly journals Design and synthesis of substituted (1-(benzyl)-1H-1,2,3-triazol-4-yl)(piperazin-1-yl)methanone conjugates: study on their apoptosis inducing ability and tubulin polymerization inhibition

2020 ◽  
Vol 11 (11) ◽  
pp. 1295-1302
Author(s):  
Kesari Lakshmi Manasa ◽  
Sowjanya Thatikonda ◽  
Dilep Kumar Sigalapalli ◽  
Sowmya Vuppaladadium ◽  
Ganthala Parimala Devi ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Proliferative Potential ◽  
Tubulin Polymerization ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Design And Synthesis ◽  
Substituted 1

Herein, we have designed and synthesized a library of substituted (1-(benzyl)-1H-1,2,3-triazol-4-yl)(piperazin-1-yl)methanone derivatives (10aa–ef) and evaluated for their anti-proliferative potential against a panel of human cancer cell lines.

scholarly journals Synthesis of Novel Class of N-Alkyl-isatin-3-iminobenzoic Acid Derivatives and Their Biological Activity in Zebrafish Embryos and Human Cancer Cell Lines

2018 ◽  
Vol 41 (3) ◽  
pp. 350-359 ◽  
Author(s):  
Muhammad Farooq ◽  
Zainab Mohammed Al Marhoon ◽  
Nael Abu Taha ◽  
Almohannad Abdulrahman Baabbad ◽  
Mohammed Ahmed Al-Wadaan ◽  
...  
Keyword(s):  
Biological Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Zebrafish Embryos ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

ChemInform Abstract: Design and Synthesis of C35-Fluorinated Solamins and Their Growth Inhibitory Activities Against Human Cancer Cell Lines.

ChemInform ◽  
2012 ◽  
Vol 43 (9) ◽  
pp. no-no
Author(s):  
Naoto Kojima ◽  
Yuki Suga ◽  
Hiromi Hayashi ◽  
Takao Yamori ◽  
Takehiko Yoshimitsu ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Design And Synthesis ◽  
Growth Inhibitory ◽  
Inhibitory Activities
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