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Synthesis and biological evaluation of chalcones having heterosubstituent(s)

Author(s): Sweety1, S Kumar1, K Nepali1, S Sapra1, OP Suri1, KL Dhar1, GS Sarma1, AK Saxena2
1Department of Pharmaceutical Chemistry, ISF College of Pharmacy, Moga - 142 001, India 2Department of Pharmacology, IIIM, Canal Road, Jammu - 180 001, India

Correspondence Address:
K L Dhar Department of Pharmaceutical Chemistry, ISF College of Pharmacy, Moga - 142 001 India E-mail: [email protected]

Chalcones and their synthetic analogues appear to have the same binding site of tubuline as phenstatin, combretastatin steganacin and podophylotoxin and are therefore capable to inhibit cancer cell proliferation. The phenyl rings with appropriate substitutions maintain a fixed distance between two centers of aryl rings. The two aromatic rings in these molecules are arranged like the two wings of a butterfly having certain dihedral angle between them, therefore a "butterfly model" is proposed an important structural feature responsible for their antitubulin activity. In this sequence a series of chalcones were synthesized and evaluated for in vitro cytotoxic activity against a panel of human cancer cell lines. In addition the synthetics reduced MIC of ciprofloxacin upto four fold this indicates their bioavailability enhancing potential.

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