Next Article in Journal
Insight into the Structural Requirement of 2-Alkyl-4-(biphenylmethoxy)quinolines as Nonpeptide Angiotensin II Receptor Antagonists: A QSAR Approach
Previous Article in Journal
Alcohol Dehydrogenases as Tools for the Preparation of Enantiopure Metabolites of Drugs with Methyl Alkyl Ketone Moiety
 
 
Search for Articles:
Title / Keyword
Author / Affiliation / Email
Journal
Article Type
 
 
Advanced Search
 
Section
Special Issue
Volume
Issue
Number
Page
 
Journals
Sci. Pharm.
Volume 77
Issue 1
10.3797/scipharm.0811-03
scipharm-logo
Submit to this Journal Review for this Journal Propose a Special Issue
► Article Menu

Article Menu

share Share announcement Help format_quote Cite question_answer Discuss in SciProfiles thumb_up
...
Endorse textsms
...
Comment
Scientia Pharmaceutica is published by MDPI from Volume 84 Issue 3 (2016). Previous articles were published by another publisher in Open Access under a CC-BY (or CC-BY-NC-ND) licence, and they are hosted by MDPI on mdpi.com as a courtesy and upon agreement with Austrian Pharmaceutical Society (Österreichische Pharmazeutische Gesellschaft, ÖPhG).
first_page
settings
Order Article Reprints
Font Type:
Arial Georgia Verdana
Font Size:
Aa Aa Aa
Line Spacing:
Column Width:
Background:
Article

Synthesis of Novel 1,3-Diacetoxy-Acridones as Cytotoxic Agents and their DNA-Binding Studies

by
N. K. SATHISH
1,
V. V. S. RAJENDRA PRASAD
1,
N. M. RAGHAVENDRA
2,
S. M. SHANTA KUMAR
1 and
Y. C. MAYUR
1,*
1
Medicinal Chemistry Research Division, V. L. College of Pharmacy, Raichur-584103, Karnataka, India
2
Acharya and BM Reddy College of Pharmacy, Bangalore, Karnataka, India
*
Author to whom correspondence should be addressed.
Sci. Pharm. 2009, 77(1), 19-32; https://doi.org/10.3797/scipharm.0811-03
Submission received: 4 November 2008 / Accepted: 18 December 2008 / Published: 19 December 2008
Versions Notes

Abstract

A series of novel substituted acridones (1–15) have been synthesized. Their in vitro cytotoxicity against human breast adenocarcinoma (MCF-7) and human promyelocytic leukemia (HL-60) cell lines has been investigated. The compounds 11, 12, 14 and 15 showed moderate activity against MCF-7 cell lines with IC50 value < 5.83 μM. The compounds 8, 10–12, and 15 showed moderate activity against HL-60 cell lines with IC50 value < 1.75 μM. The DNAbinding properties of the compounds were evaluated based on their affinity or intercalation with CT-DNA measured with absorption titration. The compound 12 bearing planar diacetoxy tricyclic ring linked with butyl piperidine side chain showed highest binding affinity with binding constant (Ki) 10.38 ×10 ×M–1. The examination of the relationship between lipophilicity and cytotoxic properties of acridones showed a poor correlation.
Keywords: 1,3-Diacetoxyacridone; Cytotoxicity; MCF-7; HL-60, DNA-binding; Calf-Thymus DNA 1,3-Diacetoxyacridone; Cytotoxicity; MCF-7; HL-60, DNA-binding; Calf-Thymus DNA

Share and Cite

MDPI and ACS Style

SATHISH, N.K.; RAJENDRA PRASAD, V.V.S.; RAGHAVENDRA, N.M.; SHANTA KUMAR, S.M.; MAYUR, Y.C. Synthesis of Novel 1,3-Diacetoxy-Acridones as Cytotoxic Agents and their DNA-Binding Studies. Sci. Pharm. 2009, 77, 19-32. https://doi.org/10.3797/scipharm.0811-03

AMA Style

SATHISH NK, RAJENDRA PRASAD VVS, RAGHAVENDRA NM, SHANTA KUMAR SM, MAYUR YC. Synthesis of Novel 1,3-Diacetoxy-Acridones as Cytotoxic Agents and their DNA-Binding Studies. Scientia Pharmaceutica. 2009; 77(1):19-32. https://doi.org/10.3797/scipharm.0811-03

Chicago/Turabian Style

SATHISH, N. K., V. V. S. RAJENDRA PRASAD, N. M. RAGHAVENDRA, S. M. SHANTA KUMAR, and Y. C. MAYUR. 2009. "Synthesis of Novel 1,3-Diacetoxy-Acridones as Cytotoxic Agents and their DNA-Binding Studies" Scientia Pharmaceutica 77, no. 1: 19-32. https://doi.org/10.3797/scipharm.0811-03

APA Style

SATHISH, N. K., RAJENDRA PRASAD, V. V. S., RAGHAVENDRA, N. M., SHANTA KUMAR, S. M., & MAYUR, Y. C. (2009). Synthesis of Novel 1,3-Diacetoxy-Acridones as Cytotoxic Agents and their DNA-Binding Studies. Scientia Pharmaceutica, 77(1), 19-32. https://doi.org/10.3797/scipharm.0811-03

Article Metrics

Back to TopTop