الفهرس 
. IntroductionOnly 14 pages are availabe for public view
 |  | from | 32 |  |  |
| | | from | 32 | | |
Abstract
A general survey about the cancer, anti-cancer drugs and their mechanism of action, as well as a survey about the methods of synthesis of indoline-2,3-dione. Finally, a small introduction about different approaches of computer aided drug design for that purpose.
The docking studies on CDK2 and GSK-3β inspired me 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.
The present investigation involves the synthesis of the following new intermediates:
1- 3-((Furan-2-ylmethylene)hydrazono)indolin-2-one (10a)
2- 3-((Furan-2-ylmethylene)hydrazono)-5-methylindolin-2-one (10b)
3- 5-Chloro-3-((furan-2-ylmethylene)hydrazono)indolin-2-one (10c)
4- 5-Fluoro-3-((furan-2-ylmethylene)hydrazono)indolin-2-one (10d)
5- 3-((Thiophen-2-ylmethylene)hydrazono)indolin-2-one (10e)
6- 5-Methyl-3-((thiophen-2-ylmethylene)hydrazono)indolin-2-one (10f)
7- 5-Chloro-3-((thiophen-2-ylmethylene)hydrazono)indolin-2-one (10g).
8- 5-Fluoro-3-((thiophen-2-ylmethylene)hydrazono)indolin-2-one (10h)
9- 3-(((1H-Pyrrol-2-yl)methylene)hydrazono)indolin-2-one (10i)
10- 3-(((1H-Pyrrol-2-yl)methylene)hydrazono)-5-methylindolin-2-one (10j).
11- 3-(((1H-Pyrrol-2-yl)methylene)hydrazono)-5-chloroindolin-2-one (10k).
12- 3-(((1H-Pyrrol-2-yl)methylene)hydrazono)-5-fluoroindolin-2-one (10l).