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

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

Journal Name: Anti-Cancer Agents in Medicinal Chemistry

Volume 15 , Issue 5 , 2015

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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: 5
Year: 2015
Page: [548 - 554]
Pages: 7
DOI: 10.2174/1871520614666141203124745
Price: $58

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