2. Academic Validation
  3. Targeting HER-2 over expressed breast cancer cells with 2-cyclohexyl-N-[(Z)-(substituted phenyl/furan-2-yl/thiophene-2-yl)methylidene]hydrazinecarbothioamide

Targeting HER-2 over expressed breast cancer cells with 2-cyclohexyl-N-[(Z)-(substituted phenyl/furan-2-yl/thiophene-2-yl)methylidene]hydrazinecarbothioamide

  • Bioorg Med Chem Lett. 2015 Jan 1;25(1):83-7. doi: 10.1016/j.bmcl.2014.11.009.
Mashooq Ahmad Bhat 1,  Abdullah Al-Dhfyan,  Azmat Ali Khan,  Nouf Al-Harbi,  P S Manogaran,  Amer M Alanazi,  Hoong-Kun Fun,  Mohamed A Al-Omar
Affiliations

Affiliation

  • 1 Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, PO Box 2457, Riyadh 11451, Saudi Arabia. mashooqbhat@rediffmail.com
PMID: 25466196 DOI: 10.1016/j.bmcl.2014.11.009
Abstract

Cyclohexyl thiosemicarbazone derivatives (C1-14) were synthesized, characterized and evaluated against HER-2 over expressed breast Cancer cells. The synthesized compounds were screened in vitro against four breast Cancer cell lines; SKBr-3, MCF-7, MDA-MB-468 and MDA-MB-231. All the compounds showed activity against HER-2 over expressed SKBr-3 cells with (IC₅₀ = 25.6 ± 0.07 μM-61.6 ± 0.4 μM). The most active compounds inhibit ALDH⁺ breast Cancer Stem Cells more effectively than the Cancer Stem Cells specific agent Salinomycin. Immunohistochemistry staining also confirmed that these compounds inhibit the expression of HER-2 on SKBr-3 cells. Compound C2 significantly inhibited the cell migration and cell adhesion of breast Cancer cell lines. Compound C2 was found to most active compound of this series targeting HER-2 over expressed breast Cancer cells.

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