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

被引：5

作者：

Bhat, Mashooq Ahmad ^{[1
]}

Al-Tahhan, M. ^{[2
]}

Al-Omar, Mohamed A. ^{[1
]}

Naglah, Ahmed M. ^{[3
,4
]}

Al-Dhfyan, Abdullah ^{[2
,5
]}

机构：

[1] King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, Riyadh 11451, Saudi Arabia

[2] King Faisal Specialist Hosp & Res Ctr, Stem Cell & Tissue Reengn Program, Res Ctr, MBC-03,POB 3354, Riyadh 11211, Saudi Arabia

[3] King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, DEDC, Riyadh 11451, Saudi Arabia

[4] Natl Res Ctr, Peptide Chem Dept, Chem Ind Res Div, Cairo 12622, Egypt

[5] King Saud Univ, Coll Pharm, Dept Pharmacol & Toxicol, POB 2457, Riyadh 11451, Saudi Arabia

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2019年 / 16卷 / 04期

关键词：

Thiosemicarbazones; MCF-7 cell line; MDA-MB-231 cell line; breast cancer; anti-cancer activity; verapamil; RIBONUCLEOTIDE REDUCTASE; INHIBITORS; CELLS; DERIVATIVES;

D O I：

10.2174/1570180815666181008100944

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 mu M - 185.35 mu M) and (IC50 = 12.97 mu M - 107.33 mu M), respectively. Compound 9 presented ( IC50 = 12.76 mu M and 12.97 mu M) 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 mu M concentration. It showed superiority to block side population by more than 80% at 5 mu M concentration compared to the reference drug verapamil.

引用

页码：446 / 452

页数：7