Anti-mitotic Activity of the Benzothiazole-pyrazole Hybrid Derivatives

Author(s):

M. Bhat*, S.L. Belagali, N.K.H. Kumar and S. Jagannath   Pages 66 - 73 ( 8 )

Abstract:

Background: Nitrogen-containing heterocyclics are abundant in natural products and also in synthetic drug molecules because of a variety of applications and superior pharmacological profile action. Pyrazoles are the integral architects of many of the heterocyclic compounds with superior biological activity.

Methods: Two series of the pyrazole conjugated Benzothiazole derivatives were synthesized. The pyrazoles were synthesized by the Vilsmeier-Haack reaction and then conjugated with benzothiazole hydrazine and hydrazide by imine bond formation. The synthesized compounds were screened for anti-mitotic activity using Allium assay.

Results: Here, the anti-mitotic activity, the percentage of cell division and the percentage of inhibition compared to the control were calculated. Compound 4b (-OMe), 4c (-OH), 5b (-OMe), 5c (- OH) and 5d (-CH3) had electron donating groups which showed excellent activity, was followed by 4f and 5f where they contain p-Bromo substitution, showing moderate activity.

Conclusion: In the two series, benzothiazole linked to pyrazole through the hydrazide bridging (5a-5i) had superior to hydrazine bridging (4a-4i). The observed chromosomal aberrations are because of the structural morphology and binding sites of the molecule with the chromosome.

Keywords:

Pyrazole, benzothiazole, antimitotic activity, ID50 value, hydrazine, chromosome.

Affiliation:

Environmental Chemistry Laboratory, Department of Studies in Environmental Science, University of Mysore, Manasagangothri, Mysore -570 006, Karnataka, Environmental Chemistry Laboratory, Department of Studies in Environmental Science, University of Mysore, Manasagangothri, Mysore -570 006, Karnataka, Department of Studies in Botany, University of Mysore, Manasagangothri, Mysore -570 006, Karnataka, Department of Studies in Botany, University of Mysore, Manasagangothri, Mysore -570 006, Karnataka

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