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Design, synthesis, and molecular docking of pyrazole carboxamide derivatives bearing benzene sulfonamide tail as potential anticancer agents


1 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard, India
2 Department of pharmaceutical Chemistry, Product Development Cell-II, National Institute of Immunology, New Delhi, India
3 Department of Biotechnology, College of Pharmacy, Madras Medical College, Chennai, Tamil Nadu, India

Correspondence Address:
Ozair Alam,
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard
India
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Source of Support: None, Conflict of Interest: None

Introduction: Cancer has been found to be the leading cause of death worldwide resulting in 8.2 million deaths and an estimated 14.1 million new cases being reported. [1] The major concerns related to design of new cancer therapeutic agents are improving its potency, selectivity and safety profile. Materials and Method: The compounds were synthesized using the reported procedures and characterized by IR, NMR and maas spectrometry and then evaluated for anti-cancer activity usinng MTT assay against MCF-7 breast cancer cell lines. Results: In the screening studies, synthesized compounds were evaluated for their in vitro anticancer activity against MCF 7 (Breast cancer) cell line using tamoxifen as reference standard. All compounds were tested in vitro at a concentration of 0.5 200΅M. The compound (VIIIb) displayed significant anticancer activity comparable to that of standard drug Tamoxifen. Order of potency is as follows: VIIIb > VIIIh > VIIIf > VIIIc > VIIId > VIIIk > VIIIg > VIIIj > VIIIa > VIIIe. Conclusion: Compound (VIIIb) was found to be the most potent compound with IC50 value 5.8 ΅M as compared to the reference standard tamoxifen (8.1΅M). The promising results of the derivative (VIIIb) was subjected to check for its stability with the protein using molecular dynamics study so as to understand the inter-atomic interaction patterns and stability of ligand in the CDK receptor.


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    -  Uthuppan J
    -  Alam O
    -  Naim MJ
    -  Nawaz F
    -  Alam MJ
    -  Panda AK
    -  Alam MA
    -  Devaraji V
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