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Indenoindolone derivatives as topoisomerase II-inhibiting anticancer agents

Kashyap, Maneesh ; Kandekar, Somnath ; Baviskar, Ashish T ; Das, Dipon ; Preet, Ranjan ; Mohapatra, Purusottam LU ; Satapathy, Shakti Ranjan LU ; Siddharth, Sumit ; Guchhait, Sankar K and Kundu, Chanakya N , et al. (2013) In Bioorganic & Medicinal Chemistry Letters 23(4). p.934-938
Abstract

Based on known heterocyclic topoisomerase II inhibitors and anticancer agents, various indenoindolone derivatives were predicted as potential topoisomerase II-inhibiting anticancer agents. They are hydrazones, (thio)semicarbazones, and oximes of indenoindolones, and indenoindolols. These derivatives with suitable substitutions exhibited potent specific inhibition of human DNA TopoIIα while not showing inhibition of topoisomerase I and DNA intercalation, despite the fact that parent indenoindolones are known poor/moderate inhibitors of topoisomerase II. The potent topoisomerase II inhibitor indenoindolone derivatives exhibited good anticancer activities compared to etoposide and 5-fluorouracil, and relatively low toxicity to normal... (More)

Based on known heterocyclic topoisomerase II inhibitors and anticancer agents, various indenoindolone derivatives were predicted as potential topoisomerase II-inhibiting anticancer agents. They are hydrazones, (thio)semicarbazones, and oximes of indenoindolones, and indenoindolols. These derivatives with suitable substitutions exhibited potent specific inhibition of human DNA TopoIIα while not showing inhibition of topoisomerase I and DNA intercalation, despite the fact that parent indenoindolones are known poor/moderate inhibitors of topoisomerase II. The potent topoisomerase II inhibitor indenoindolone derivatives exhibited good anticancer activities compared to etoposide and 5-fluorouracil, and relatively low toxicity to normal cells. These derivatizations of indenoindolones were found to result in enhancement of anticancer activities.

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publishing date
type
Contribution to journal
publication status
published
keywords
Antineoplastic Agents/chemistry, DNA Topoisomerases, Type II/chemistry, Humans, Indoles/chemistry, Models, Molecular, Neoplasms/drug therapy, Topoisomerase II Inhibitors/chemistry
in
Bioorganic & Medicinal Chemistry Letters
volume
23
issue
4
pages
934 - 938
publisher
Elsevier
external identifiers
  • scopus:84872939428
  • pmid:23321564
ISSN
0960-894X
DOI
10.1016/j.bmcl.2012.12.063
language
English
LU publication?
no
additional info
Copyright © 2012 Elsevier Ltd. All rights reserved.
id
83e5fe3c-1436-4200-ac26-6b545c2bf07d
date added to LUP
2025-01-30 10:31:09
date last changed
2025-06-06 13:53:22
@article{83e5fe3c-1436-4200-ac26-6b545c2bf07d,
  abstract     = {{<p>Based on known heterocyclic topoisomerase II inhibitors and anticancer agents, various indenoindolone derivatives were predicted as potential topoisomerase II-inhibiting anticancer agents. They are hydrazones, (thio)semicarbazones, and oximes of indenoindolones, and indenoindolols. These derivatives with suitable substitutions exhibited potent specific inhibition of human DNA TopoIIα while not showing inhibition of topoisomerase I and DNA intercalation, despite the fact that parent indenoindolones are known poor/moderate inhibitors of topoisomerase II. The potent topoisomerase II inhibitor indenoindolone derivatives exhibited good anticancer activities compared to etoposide and 5-fluorouracil, and relatively low toxicity to normal cells. These derivatizations of indenoindolones were found to result in enhancement of anticancer activities.</p>}},
  author       = {{Kashyap, Maneesh and Kandekar, Somnath and Baviskar, Ashish T and Das, Dipon and Preet, Ranjan and Mohapatra, Purusottam and Satapathy, Shakti Ranjan and Siddharth, Sumit and Guchhait, Sankar K and Kundu, Chanakya N and Banerjee, Uttam C}},
  issn         = {{0960-894X}},
  keywords     = {{Antineoplastic Agents/chemistry; DNA Topoisomerases, Type II/chemistry; Humans; Indoles/chemistry; Models, Molecular; Neoplasms/drug therapy; Topoisomerase II Inhibitors/chemistry}},
  language     = {{eng}},
  month        = {{02}},
  number       = {{4}},
  pages        = {{934--938}},
  publisher    = {{Elsevier}},
  series       = {{Bioorganic & Medicinal Chemistry Letters}},
  title        = {{Indenoindolone derivatives as topoisomerase II-inhibiting anticancer agents}},
  url          = {{http://dx.doi.org/10.1016/j.bmcl.2012.12.063}},
  doi          = {{10.1016/j.bmcl.2012.12.063}},
  volume       = {{23}},
  year         = {{2013}},
}