Analogue-based design, synthesis and biological evaluation of 3-substituted-(methylenehydrazono)indolin-2-ones as anticancer agents

Eur J Med Chem. 2014 May 6:78:275-80. doi: 10.1016/j.ejmech.2014.03.058.

Haytham E Dweedar ¹, Hoda Mahrous ¹, Hany S Ibrahim ², Hatem A Abdel-Aziz ³

Affiliations

1 Industrial Biotechnology Department, Genetic Engineering and Biotechnology Research Institute (GEBRI), Sadat City University, Egypt.
2 Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Egyptian Russian University, Badr City, Helwan, Egypt.
3 Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia; Department of Applied Organic Chemistry, National Research Center, Dokki, Cairo 12622, Egypt. Electronic address: hatem_741@yahoo.com.

PMID: 24686014 DOI: 10.1016/j.ejmech.2014.03.058

Abstract

The docking studies on CDK2 and GSK-3β inspired us to synthesis a series of indoline-2,3-dione hydrazones 10a-l. Treatment of indoline-2,3-dione derivatives 7a-d with hydrazine gave 3-hydrazonoindolin-2-ones 8a-d which were reacted with the appropriate aldehydes 9a-c to yield 3-substituted-(methylenehydrazono)indolin-2-ones 10a-l. Compounds 10a-l showed a significant Anticancer activity against human breast cell line MCF-7. Compounds 10c, f, i exhibited the highest activity almost the same of doxorubicin (IC50 = 6.10 μM) with IC50 = 7.75, 6.75, 6.25 μM, respectively.

Keywords

Analogue-based design; Cancer; Human breast cell line MCF-7; Indoline-2,3-dione hydrazones; Molecular docking.

Name
Email *

	Sorry, but the email address you supplied was invalid.