Document Detail


11H-Pyrido[3',2':4,5]pyrrolo[3,2-c]cinnoline and pyrido[3',2':4,5]pyrrolo[1,2-c][1,2,3] benzotriazine: two new ring systems with antitumor activity.
MedLine Citation:
PMID:  25317694     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
Derivatives of new ring systems 11H-pyrido[3',2':4,5]pyrrolo[3,2-c]cinnoline and pyrido[3',2':4,5]pyrrolo[1,2-c][1,2,3]benzotriazine were prepared from the key intermediates 2-(1H-pyrrolo[2,3-b]pyridin-2-yl)anilines in excellent yields (94-99%) and screened by the National Cancer Institute (NCI, Bethesda, USA), on about 60 human tumor cell lines derived from nine cancer cell types. Tested compounds exhibited antiproliferative activity against all the human cell lines showing comparable MG_MID range 0.74-1.15 µM. A particular efficacy was observed against the leukemia sub-panel (GI50 range 0.73-0.0090 µM). Flow cytometric analysis of cell cycle demonstrated an increase of percentage of cells in G2/M phase. They cause apoptosis of the cells, mitochondrial depolarization, generation of reactive oxygen species, and activation of caspase-3, caspase-8 and caspase-9. Moreover, they acted as a topoisomerase I inhibitors.
Authors:
Patrizia Diana; Barbara Parrino; Anna Carbone; Marina Muscarella; Virginia Spano'; Alessandra Montalbano; Paola Barraja; Alessia Salvador; Daniela Vedaldi; Girolamo Cirrincione
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2014-10-15
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  -     ISSN:  1520-4804     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2014 Oct 
Date Detail:
Created Date:  2014-10-15     Completed Date:  -     Revised Date:  2014-10-16    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
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