الفهرس 
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Abstract
Cancer received a considerable interest as it is one of the most fatal diseases in the world. This thesis pointed towards the anticancer and anti-inflammatory activities of 4-phenyl, 5-(un)substituted phenyl thiazole derivatives. In the present work, the new compounds were designed and synthesized depending on the incorporation of several structural features and functional groups that are believed to positively contribute to the anticancer and anti-inflammatory properties hoping to reach derivatives of high potency and low side effects.
This thesis consists of the following parts:
1. Introduction:
In this section, a literature review about cancer, inflammation, thiazoles of anticancer and anti-inflammatory activities of thiazoles and different methods adopted for thiazole preparation.
2. Rationale:
It includes the research objectives and the major aims that direct the theoretical and practical work.
3. Discussion:
It deals with the discussion of the experimental methods used for the synthesis of the designed compounds with a summarized data about the characterization of these new compounds.
4. Experimental:
In this part, the practical methods adopted for the preparation of the reported and new intermediates as well as the new final compounds are presented. Also, their spectral and elemental microanalytical data are cited.
The following compounds are prepared.
Reported intermediates (5 compounds):
1) 2-Hydroxy-1,2-diphenyl-ethanone II. (141)
2) 2-Chloro-1,2-diphenyl-ethanone III. (142)
3) 4,5-Diphenyl-thiazol-2-ylamine IV. (143)
4) N-(4,5-Diphenyl-thiazol-2-yl)-formamide V. (144)
5) (4,5-Diphenyl-thiazol-2-ylamino)-acetic acid ethyl ester VI. (144)
New intermediates (10 compounds):
1) [5-(4-Chlorosulfonyl-phenyl)-4-phenyl-thiazol-2-ylamino]-acetic acid VII.
2) [4-Phenyl-5-(4-sulfamoyl-phenyl)-thiazol-2-ylamino]-acetic acid VIII.
3) [4-Phenyl-5-(4-sulfamoyl-phenyl)-thiazol-2-ylamino]-acetic acid ethyl ester IX.
4) (4,5-Diphenyl-thiazol-2-ylamino)-acetic acid hydrazide Xa.
5) 4-[2-(Hydrazinocarbonylmethyl-amino)-4-phenyl-thiazol-5-yl]-benzenesulfonamide Xb.
6) (4,5-Diphenyl-thiazol-2-ylamino)-acetyl azide XIV.
7) 2-(2-(4,5-Diphenylthiazol-2-ylamino)acetyl)-N-phenylhydrazinecarbo- thioamide XVIa.
8) 2-(2-(4,5-Diphenylthiazol-2-ylamino)acetyl)-N-(4-methylphenyl)hydrazine carbo- thioamide XVIb.
9) 2-(2-(4,5-Diphenylthiazol-2-ylamino)acetyl)-N-(4-bromophenyl)hydrazine carbo-thioamide XVIc.
10) 2-(2-(4-phenyl-5-(4-sulfamoyl-phenyl)-thiazol-2-ylamino)acetyl)-N-(4-methylphenyl) hydrazine carbo-thioamide XVId.
New final compounds (24 compounds):
1) (4,5-Diphenyl-thiazol-2-ylamino)-acetic acid (1-methyl-3-oxo-butylidene) –hydrazide XIa.
2) 3-{[2-(4,5-Diphenyl-thiazol-2-ylamino)-acetyl]-hydrazono}-butyric acid ethyl ester XIb.
3) 5-[(4,5-Diphenyl-thiazol-2-ylamino)-methyl]-3H-[1,3,4]oxadiazole-2-thione XII.
4) 2-(4,5-Diphenyl-thiazol-2-ylamino)-N-(4-oxo-2-phenyl-thiazolidin-3-yl)-acetamide XIIIa.
5) 2-(4,5-Diphenyl-thiazol-2-ylamino)-N-(4-oxo-2-p-tolyl-thiazolidin-3-yl)-acetamide XIIIb.
6) N-[2-(4-Chloro-phenyl)-4-oxo-thiazolidin-3-yl]-2-(4,5-diphenyl-thiazol-2-ylamino)-acetamide XIIIc.
7) [2-(4,5-Diphenyl-thiazol-2-ylamino)-acetylamino]-acetic acid methyl ester XVa.
8) 2-[2-(4,5-Diphenyl-thiazol-2-ylamino)-acetylamino]-propionic acid ethyl ester XVb.
9) 2-[2-(4,5-Diphenyl-thiazol-2-ylamino)-acetylamino]-3-hydroxy-propionic acid methyl ester XVc.
10) 2-[2-(4,5-Diphenyl-thiazol-2-ylamino)-acetylamino]-3-(4-hydroxy-phenyl)-propionic acid ethyl esterXVd.
11) 2-[2-(4,5-Diphenyl-thiazol-2-ylamino)-acetylamino]-3-(1H-indol-3-yl)-propionic acid ethyl ester XVe.
12) 5-[(4,5-Diphenyl-thiazol-2-ylamino)-methyl]-4-phenyl-2,4-dihydro-[1,2,4]triazole-3-thione XVII.
13) {5-[(4,5-Diphenyl-thiazol-2-ylamino)-methyl]-[1,3,4]thiadiazol-2-yl}-phenyl-amine XVIII.
14) 1-(3,5-Dimethyl-pyrazol-1-yl)-2-(4,5-diphenyl-thiazol-2-ylamino)-ethanone XIXa.
15) 2-[2-(4,5-Diphenyl-thiazol-2-ylamino)-acetyl]-5-methyl-2,4-dihydro-pyrazol-3-one XIXb.
16) 4-{2-[2-(3,5-Dimethyl-pyrazol-1-yl)-2-oxo-ethylamino]-4-phenyl-thiazol-5-yl}-benzenesulfonamide XIXc.
17) N-(2,5-Dioxo-2,5-dihydro-pyrrol-1-yl)-2-(4,5-diphenyl-thiazol-2-ylamino)-acetamide XXa.
18) (4,5-Diphenyl-thiazol-2-ylamino)-acetic acid (2-oxo-1, 2-dihydro-indol-3-ylidene)-hydrazide XXb.
19) N-(2,5-Dioxo-2,5-dihydro-pyrrol-1-yl)-2-[4-phenyl-5-(4-sulfamoyl-phenyl)-thiazol-2-ylamino]-acetamide XXc.
20) (4,5-Diphenyl-thiazol-2-ylamino)-acetic acid benzylidene-hydrazide XXIa.
21) (4,5-Diphenyl-thiazol-2-ylamino)-acetic acid (4-methyl-benzylidene)-hydrazide XXIb.
22) (4,5-Diphenyl-thiazol-2-ylamino)-acetic acid (4-chloro-benzylidene)-hydrazide XXIc.
23) 4-{2-[(Benzylidene-hydrazinocarbonylmethyl)-amino]-4-phenyl-thiazol-5-yl}-benzenesulfonamide XXId.
24) 4-{2-[(4-Methyl-benzylidene-hydrazinocarbonylmethyl)-amino]-4-phenyl-thiazol-5-yl}-benzenesulfonamide XXIe.
5. Pharmacological Screening:
a. Anticancer Screening:
26 compounds of the new and intermediate compounds were evaluated for their anticancer activity using MTT assay method using doxorubicin as standard. Most of the tested compounds showed moderate activity in comparison with doxorubicin. COX-1/COX-2 selectivity index was performed for some selected compounds. All of tested compounds show high results.
b. Anti-inflammatory Screening:
17 compounds were evaluated for their anti-inflammatory activity using ”rat paw carrageenan edema” method.
6. References:
This part includes 188 references covering the period 1941-2017.