Basic Informations
C.V
name: fatma magdy maher
job: demonestrator
Master Title
Synthesis of Some N ew Thiazole Derivatives As Potential Antic ancer Agents
Master Abstract
Abstract
I
Synthesis of some
new thiazole derivatives
as potent
ial anticancer agents
In the search for new cytotoxic agents with improved anticancer profile,
some new thiazole derivatives which bearing a free sulfonamide moiety were
synthesized. All the newly
synthesized target compounds were subjected to
in
vitro
anticancer screening against
human breast cancer cell line MCF
-
7
.The
most potent compounds, as concluded from the
ir
in vitro
anticancer screening,
were selected to be evaluated for their
in vitro
inh
ibitory
activity against
carbonic anhydrase enzyme. Moreover, a molecular docking study was carried
out by docking
the newly synthesized compounds in the active site of the
carbonic anhydrase enzyme.
The thesis includes the following parts:
1.
Introduction
This part includes a brief literature review on cancer, chemotherapy and
radiotherapy
then on
the reported anticancer activity of
different thiazole
derivatives and
sulfonamide derivatives and their mechanism
s
of action. In
addition, various methods fo
r the synthesis of thiazole and thiazolodinone
derivatives were discussed.
2.
Aim of the present investigation:
The present investigation deals with the design and the synthesis of novel thiazole
derivatives bearing a sulfonamide moiety in their molecul
es in order to explore the
effect of combining the thiazole moiety with the biologically active sulfonamide group
on the antitumor activity of the synthesized compounds.
Abstract
II
3.
Theoretical Discussion:
This part deals with the discussion of
the
experimental
methods adopted for
the synthesis of the t
arget compounds
,
as well as
the analytical methods
adopted for the identification and verification of the structures of the
synthesized compounds by elemental analysis and spectroscopic methods. In
addition, this s
ection includes schemes (1
-
4) which illustrate the synthetic
pathways adopted for the preparation of the designed compounds.
4.
Experimental:
This part includes the detailed practical methods fo
r the synthesis of twenty
new compounds, one new intermediate
and fourteen
known intermediates that
are listed below with their elemental analyses and spectral data (IR,
1
H
-
NMR
and mass spectroscopy).
Known intermediates:
?
2
-
Chloro
-
N
-
(4
-
sulfamoylphenyl)
acetamide
(II).
?
4
-
((4
-
Oxo
-
4,5
-
dihydrothiazol
-
2
-
yl)amino)benzenesulfonamide
(III).
?
4
-
((4
-
Chlorothiazol
-
2
-
yl)amino)benzenesulfonamide
(V).
?
2
-
Benzamidoacetic acid
(IXa).
?
2
-
(4
-
Chlorobenzamido)acetic acid
(IXb).
?
4
-
Benzylidene
-
2
-
phenyloxazol
-
5(4
H
)
-
one
(Xa).
?
4
-
(4
-
Chloro
benzylidene)
-
2
-
phenyl
oxazol
-
5(4
H
)
-
one
(
X
b).
?
4
-
[4
-
(Dimethylamino)benzylidene]
-
2
-
phenyloxazol
-
5(4
H
)
-
one
(Xc).
?
4
-
Benzylidene
-
2
-
(4
-
chlorophenyl)oxazol
-
5(4
H
)
-
one
(Xd).
?
4
-
(4
-
Chlorobenzylidene)
-
2
-
(4
-
chlorophenyl)oxazol
-
5(4
H
)
-
one
(Xe).
PHD Title
analysis of drugs
PHD Abstract
Abstract
I
Synthesis of some
new thiazole derivatives
as potent
ial anticancer agents
In the search for new cytotoxic agents with improved anticancer profile,
some new thiazole derivatives which bearing a free sulfonamide moiety were
synthesized. All the newly
synthesized target compounds were subjected to
in
vitro
anticancer screening against
human breast cancer cell line MCF
-
7
.The
most potent compounds, as concluded from the
ir
in vitro
anticancer screening,
were selected to be evaluated for their
in vitro
inh
ibitory
activity against
carbonic anhydrase enzyme. Moreover, a molecular docking study was carried
out by docking
the newly synthesized compounds in the active site of the
carbonic anhydrase enzyme.
The thesis includes the following parts:
1.
Introduction
This part includes a brief literature review on cancer, chemotherapy and
radiotherapy
then on
the reported anticancer activity of
different thiazole
derivatives and
sulfonamide derivatives and their mechanism
s
of action. In
addition, various methods fo
r the synthesis of thiazole and thiazolodinone
derivatives were discussed.
2.
Aim of the present investigation:
The present investigation deals with the design and the synthesis of novel thiazole
derivatives bearing a sulfonamide moiety in their molecul
es in order to explore the
effect of combining the thiazole moiety with the biologically active sulfonamide group
on the antitumor activity of the synthesized compounds.
Abstract
II
3.
Theoretical Discussion:
This part deals with the discussion of
the
experimental
methods adopted for
the synthesis of the t
arget compounds
,
as well as
the analytical methods
adopted for the identification and verification of the structures of the
synthesized compounds by elemental analysis and spectroscopic methods. In
addition, this s
ection includes schemes (1
-
4) which illustrate the synthetic
pathways adopted for the preparation of the designed compounds.
4.
Experimental:
This part includes the detailed practical methods fo
r the synthesis of twenty
new compounds, one new intermediate
and fourteen
known intermediates that
are listed below with their elemental analyses and spectral data (IR,
1
H
-
NMR
and mass spectroscopy).
Known intermediates:
?
2
-
Chloro
-
N
-
(4
-
sulfamoylphenyl)
acetamide
(II).
?
4
-
((4
-
Oxo
-
4,5
-
dihydrothiazol
-
2
-
yl)amino)benzenesulfonamide
(III).
?
4
-
((4
-
Chlorothiazol
-
2
-
yl)amino)benzenesulfonamide
(V).
?
2
-
Benzamidoacetic acid
(IXa).
?
2
-
(4
-
Chlorobenzamido)acetic acid
(IXb).
?
4
-
Benzylidene
-
2
-
phenyloxazol
-
5(4
H
)
-
one
(Xa).
?
4
-
(4
-
Chloro
benzylidene)
-
2
-
phenyl
oxazol
-
5(4
H
)
-
one
(
X
b).
?
4
-
[4
-
(Dimethylamino)benzylidene]
-
2
-
phenyloxazol
-
5(4
H
)
-
one
(Xc).
?
4
-
Benzylidene
-
2
-
(4
-
chlorophenyl)oxazol
-
5(4
H
)
-
one
(Xd).
?
4
-
(4
-
Chlorobenzylidene)
-
2
-
(4
-
chlorophenyl)oxazol
-
5(4
H
)
-
one
(Xe).