Synthesis and Biological Evaluation of Diaryl Ether Linked DC-81 Conjugates as Potential Antitumor Agents

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 16, 12 Issues, 2016

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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  • 27th of 59 in Chemistry, Medicinal

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Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex

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Synthesis and Biological Evaluation of Diaryl Ether Linked DC-81 Conjugates as Potential Antitumor Agents

Anti-Cancer Agents in Medicinal Chemistry, 13(10): 1590-1600.

Author(s): Ahmed Kamal, A. Viswanath, M. Janaki Ramaiah, J. N.S.R.C. Murty, Farheen Sultana, E. Vijaya Bharathi, G. Ramakrishna, Pranjal Sarma, A. Lavanya, S. N.C.V.L. Pushpavalli and Manika pal Bhadra.

Affiliation: Medicinal Chemistry and Pharmacology, Chemical Biology Laboratory, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India.


A series of new diaryl ether linked pyrrolobenzodiazepine (PBD) conjugates (4a-i, 5a-i and 6a-f) was synthesized and evaluated for their anticancer activity against a panel of 11 human cancer cell lines. These conjugates exhibited significant anticancer activity with GI50 values in the range of 0.1-3.88 μM. Some of the potent conjugates (4b, 4h, 5h, 6b, 6c and 6e) were further investigated on cell cycle distribution. FACS analysis showed the accumulation of cells in G0 phase indicating the apoptosis inducing nature of these conjugates. Moreover, compound 6b caused a decrease in the mitochondrial membrane potential, which indicates the apoptotic nature of the compound through mitochondrial mediated pathway. Further conjugates 4b, 4h and 6b induce the activation of caspase and PARP proteins, followed by apoptotic cell death in MCF7 cell line.


Anticancer activity, apoptosis, caspase, diaryl ether, mitochondrial membrane potential, poly-(ADP-ribose) polymerase, pyrrolobenzodiazepines.

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Article Details

Volume: 13
Issue Number: 10
First Page: 1590
Last Page: 1600
Page Count: 11
DOI: 10.2174/1871520613666131125122408
Price: $58

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