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Letters in Drug Design & Discovery

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ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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Research Article

Design and Synthesis of Novel Thiosemicarbazones as Potent Anti-breast Cancer Agents

Author(s): Mashooq Ahmad Bhat*, M. Al-Tahhan, Mohamed A. Al-Omar, Ahmed M. Naglah and Abdullah Al-Dhfyan

Volume 16, Issue 4, 2019

Page: [446 - 452] Pages: 7

DOI: 10.2174/1570180815666181008100944

Abstract

Background: Thiosemicarbazones and its derivatives received a great pharmaceutical importance due to their prominent biological activities.

Methods: A series of disubstituted thiosemicarbazone derivatives (1-12) were designed and synthesized as pure compounds in good yield. All the synthesized compounds were analyzed by spectral data. The anticancer activity of all the compounds was performed against breast cancer MCF-7 and MDA-MB-231 cell lines.

Results: Most of the compounds showed activity against breast cancer MCF-7 and MDA-MB-231 cell lines with (IC50 = 12.25 µM ‒ 185.35 µM) and (IC50 = 12.97 µM ‒ 107.33 µM), respectively. Compound 9 presented (IC50 = 12.76 µM and 12.97 µM) against MCF-7 and MDA-MB-231 cell lines, respectively.

Conclusion: Compound 9, was found to exhibit significant anti-breast cancer activity. This compound was further evaluated for side population percent inhibition assay on the breast cancer cell line MCF-7 at 5 and 10 µM concentration. It showed superiority to block side population by more than 80% at 5 μM concentration compared to the reference drug verapamil.

Keywords: Thiosemicarbazones, MCF-7 cell line, MDA-MB-231 cell line, breast cancer, anti-cancer activity, verapamil.

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