Lead optimization of 2-cyclohexyl-N-[(Z)-(3-methoxyphenyl/3-hydroxyphenyl) methylidene] hydrazinecarbothioamide for targeting HER-2 over expressed breast cancer cell line SKBr-3

Journal Article

Al-Omar., Mashooq A. Bhat, Abdullah Al-Dhfyan, Ahmed M. Naglah, A A Khan, Mohamed A. . 2015

• Magazine \ Newspaper: . Molecules
• Issue Number: 10
• Volume Number: 20
• Pages: 18246-18263

Publication Abstract

Lead derivatives of 2-cyclohexyl-N-[(Z)-(3-methoxyphenyl/3-hydroxyphenyl)
methylidene]hydrazinecarbothioamides 1–18 were synthesized, characterized and evaluated
in vitro against HER-2 overexpressed breast cancer cell line SKBr-3. All the compounds showed
activity against HER-2 overexpressed SKBr-3 cells with IC50 = 17.44 ± 0.01 μM to 53.29 ±
0.33 μM. (2Z)-2-(3-Hydroxybenzylidene)-N-(3-methoxyphenyl)hydrazinecarbothioamide
(12, IC50 = 17.44 ± 0.01 μM) was found to be most potent compound of this series targeting
HER-2 overexpressed breast cancer cells compared to the standard drug 5-fluorouracil
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Molecules 2015, 20 18247
(5-FU) (IC50 = 38.58 ± 0.04 μM). Compound 12 inhibited the cellular proliferation via
DNA degradation.