Design and Synthesis of Novel Antineoplastic Agents Inspired from Marine Bromopyrrole Alkaloids
Rajesh A. Rane,
Pavan Kumar Bangalore,
Shital S. Naphade,
Harun M. Patel,
Mahesh B. Palkar,
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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