共 25 条
Lead Optimization of 2-Cyclohexyl-N-[(Z)-(3-methoxyphenyl/3-hydroxyphenyl) methylidene]hydrazinecarbothioamides for Targeting the HER-2 Overexpressed Breast Cancer Cell Line SKBr-3
被引:11
作者:

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Al-Dhfyan, Abdullah
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King Faisal Specialized Hosp & Res Ctr, Stem Cell & Tissue Reengn Program, Riyadh 11211, Saudi Arabia
King Saud Univ, Dept Pharmacol & Toxicol, Coll Pharm, Riyadh 11451, Saudi Arabia King Saud Univ, Dept Pharmaceut Chem, Coll Pharm, Riyadh 11451, Saudi Arabia

Naglah, Ahmed M.
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King Saud Univ, Dept Pharmaceut Chem, Coll Pharm, Drug Explorat & Dev Chair, Riyadh 11451, Saudi Arabia
Natl Res Ctr, Chem Ind Res Div, Peptide Chem Dept, Cairo 12622, Egypt King Saud Univ, Dept Pharmaceut Chem, Coll Pharm, Riyadh 11451, Saudi Arabia

Khan, Azmat Ali
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King Saud Univ, Dept Pharmaceut Chem, Coll Pharm, Riyadh 11451, Saudi Arabia King Saud Univ, Dept Pharmaceut Chem, Coll Pharm, Riyadh 11451, Saudi Arabia

Al-Omar, Mohamed A.
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King Saud Univ, Dept Pharmaceut Chem, Coll Pharm, Drug Explorat & Dev Chair, Riyadh 11451, Saudi Arabia King Saud Univ, Dept Pharmaceut Chem, Coll Pharm, Riyadh 11451, Saudi Arabia
机构:
[1] King Saud Univ, Dept Pharmaceut Chem, Coll Pharm, Riyadh 11451, Saudi Arabia
[2] King Faisal Specialized Hosp & Res Ctr, Stem Cell & Tissue Reengn Program, Riyadh 11211, Saudi Arabia
[3] King Saud Univ, Dept Pharmacol & Toxicol, Coll Pharm, Riyadh 11451, Saudi Arabia
[4] King Saud Univ, Dept Pharmaceut Chem, Coll Pharm, Drug Explorat & Dev Chair, Riyadh 11451, Saudi Arabia
[5] Natl Res Ctr, Chem Ind Res Div, Peptide Chem Dept, Cairo 12622, Egypt
来源:
MOLECULES
|
2015年
/
20卷
/
10期
关键词:
thiosemicarbazones;
HER-2;
SKBr-3;
cells;
BT-474;
cancer stem cells;
STEM-CELLS;
IDENTIFICATION;
RESISTANCE;
INHIBITORS;
CARCINOMA;
MARKER;
D O I:
10.3390/molecules201018246
中图分类号:
Q5 [生物化学];
Q7 [分子生物学];
学科分类号:
071010 ;
081704 ;
摘要:
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 mu M to 53.29 +/- 0.33 mu M. (2Z)-2-(3-Hydroxybenzylidene)-N-(3-methoxyphenyl)hydrazinecarbothioamide (12, IC50 = 17.44 +/- 0.01 mu M) was found to be most potent compound of this series targeting HER-2 overexpressed breast cancer cells compared to the standard drug 5-fluorouracil (5-FU) (IC50 = 38.58 +/- 0.04 mu M). Compound 12 inhibited the cellular proliferation via DNA degradation.
引用
收藏
页码:18246 / 18263
页数:18
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:3212-3219

Greenbaum, DC
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机构: Univ Calif San Francisco, Sandler Ctr Basic Res Parasit Dis, Dept Pathol, San Francisco, CA 94143 USA

Mackey, Z
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机构: Univ Calif San Francisco, Sandler Ctr Basic Res Parasit Dis, Dept Pathol, San Francisco, CA 94143 USA

Hansell, E
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机构: Univ Calif San Francisco, Sandler Ctr Basic Res Parasit Dis, Dept Pathol, San Francisco, CA 94143 USA

Doyle, P
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机构: Univ Calif San Francisco, Sandler Ctr Basic Res Parasit Dis, Dept Pathol, San Francisco, CA 94143 USA

Gut, J
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机构: Univ Calif San Francisco, Sandler Ctr Basic Res Parasit Dis, Dept Pathol, San Francisco, CA 94143 USA

Caffrey, CR
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机构: Univ Calif San Francisco, Sandler Ctr Basic Res Parasit Dis, Dept Pathol, San Francisco, CA 94143 USA

Lehrman, J
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机构: Univ Calif San Francisco, Sandler Ctr Basic Res Parasit Dis, Dept Pathol, San Francisco, CA 94143 USA

Rosenthal, PJ
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机构: Univ Calif San Francisco, Sandler Ctr Basic Res Parasit Dis, Dept Pathol, San Francisco, CA 94143 USA

McKerrow, JH
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机构: Univ Calif San Francisco, Sandler Ctr Basic Res Parasit Dis, Dept Pathol, San Francisco, CA 94143 USA

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