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Letters in Drug Design & Discovery

Author(s): Rana Asif Nadeem, Muhammad Abdul Qadir, Mahmood Ahmed* and Imran Sajid

DOI: 10.2174/1570180815666180820144621

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Cephalosporin Conjugated Sulfonamides: Synthesis, Characterization and Anticancer Activities

Page: [264 - 270] Pages: 7

  • * (Excluding Mailing and Handling)

Abstract

Background: In the present study, eight new cephalosporin conjugated sulfonamides were synthesized to investigate the anticancer activity.

Methods: All the compounds were characterized on the basis of FTIR, 1HNMR, MS and elemental analysis (CHN). The new compounds were evaluated against the Vero and Hep G2 cancer cell lines for their anticancer activities. Cytotoxicity of all the compounds was determined against brine shrimp at 20 μg concentration.

Results and Conclusion: The results revealed that ceftriaxone conjugated sulfonamide was the most potent and showed cytotoxicity (86.4 %) comparable to the standard reference drug actinomycin D (90.0 %). The compounds with lower cLogP value showed more antiproliferative effect due to their higher cell permeability. Ceftriaxone conjugated with 4-acetamido benzene sulfonyl was the most active compound against both cell lines with IC50 3.95 μM (Vero) and 5.11 μM (Hep G2) values whereas its activity was comparable with 5-fluorouracil used as reference drug (IC50 = 2.84 μM).

Keywords: Sulfonamides, anticancer agents, heterocyclics, Vero, Hep G2, cephalosporin.

Graphical Abstract

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