D-Ring-Modified Analogues of Luotonin A with Reduced Planarity: Design, Synthesis, and Evaluation of Their Topoisomerase Inhibition-Associated Cytotoxicity
Joint Authors
Suresh Kumar, Raju
Almansour, Abdulrahman I.
Arumugam, Natarajan
Bianchini, Giulia
Menéndez, J. Carlos
Mohammad, Faruq
Dupadahalli, Kotresha
Altaf, Mohammad
Source
Issue
Vol. 2019, Issue 2019 (31 Dec. 2019), pp.1-12, 12 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2019-11-13
Country of Publication
Egypt
No. of Pages
12
Main Subjects
Abstract EN
A- and D-ring-modified luotonin-inspired heterocycles have been synthesized and were evaluated for their activity against the viability of four cancer cell lines in vitro, namely, MCF7, HCT116, JURKAT, and NCI-H460.
The analysis of results indicated that two of the synthesized derivatives displayed good inhibition against the growth of the human colon cancer HCT116 cell line, with potencies lower than but in the same order of magnitude as camptothecin (CPT).
These two luotonin analogues also showed an activity similar to that of the highly potent alkaloid CPT as inhibitors of topoisomerase I and also inhibited topoisomerase II.
These results show that complete planarity is not a strict requirement for topoisomerase inhibition by luotonin-related compounds, paving the way to the design of analogues with improved solubility.
American Psychological Association (APA)
Almansour, Abdulrahman I.& Suresh Kumar, Raju& Arumugam, Natarajan& Bianchini, Giulia& Menéndez, J. Carlos& Mohammad, Faruq…[et al.]. 2019. D-Ring-Modified Analogues of Luotonin A with Reduced Planarity: Design, Synthesis, and Evaluation of Their Topoisomerase Inhibition-Associated Cytotoxicity. BioMed Research International،Vol. 2019, no. 2019, pp.1-12.
https://search.emarefa.net/detail/BIM-1123889
Modern Language Association (MLA)
Almansour, Abdulrahman I.…[et al.]. D-Ring-Modified Analogues of Luotonin A with Reduced Planarity: Design, Synthesis, and Evaluation of Their Topoisomerase Inhibition-Associated Cytotoxicity. BioMed Research International No. 2019 (2019), pp.1-12.
https://search.emarefa.net/detail/BIM-1123889
American Medical Association (AMA)
Almansour, Abdulrahman I.& Suresh Kumar, Raju& Arumugam, Natarajan& Bianchini, Giulia& Menéndez, J. Carlos& Mohammad, Faruq…[et al.]. D-Ring-Modified Analogues of Luotonin A with Reduced Planarity: Design, Synthesis, and Evaluation of Their Topoisomerase Inhibition-Associated Cytotoxicity. BioMed Research International. 2019. Vol. 2019, no. 2019, pp.1-12.
https://search.emarefa.net/detail/BIM-1123889
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1123889