Design and Synthesis of Novel Antineoplastic Agents Inspired from Marine Bromopyrrole Alkaloids

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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Editor-in-Chief:
Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France


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Design and Synthesis of Novel Antineoplastic Agents Inspired from Marine Bromopyrrole Alkaloids



Anti-Cancer Agents in Medicinal Chemistry, 15(5): 548-554.

Author(s): Rajesh A. Rane, Pavan Kumar Bangalore, Shital S. Naphade, Harun M. Patel, Mahesh B. Palkar and Rajshekhar Karpoormath.

Affiliation: Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Durban 4001, South Africa.

Abstract

Azetidin-2-one, a β -lactam four-membered heterocyclic ring is widely identified for its diverse medicinal properties. Ezetimibe a cholesterol absorption inhibitor and Aztreonam a potent cephalosporinase inhibitor proved the medicinal value of azetidin-2-ones. On the other hand marine bromopyrrole alkaloids are well known for their diverse biological significance. Hence twenty novel conjugates of azetidin-2-ones integrated with 4,5-dibromopyrrole motif were synthesized and screened for antineoplastic activity using MTT assay. Synthesized hybrids displayed good antineoplastic profile particularly towards breast cancer cell line MCF7, where hybrid 5e displayed maximum cytotoxicity (IC50 = 0.5 µM). The selective cytotoxicity displayed by these conjugates towards tested cancer cells with non-toxicity against normal human VERO cells indicated their potential for further antineoplastic drug development.




Keywords:

Antineoplastic, azetidinone, bromopyrrole alkaloid, natural product.



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Article Details

Volume: 15
Issue Number: 5
First Page: 548
Last Page: 554
Page Count: 7
DOI: 10.2174/1871520614666141203124745
Price: $58
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