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1.
Egyptian Journal of Chemistry. 2009; 52 (3): 431-450
in English | IMEMR | ID: emr-135693

ABSTRACT

New series of coumarin derivatives was synthesized and evaluated as antitumor agents against breast cancer in human cell line [MCF 7]. The key compound 8-acetyl-7-hydroxy-4-methyl coumarin [1] was synthesized and condensed with phenyl hydrazine to form the hydrazone derivative 2. Also, 1 condensed with different alkylating agents to give the corresponding sulphonyl derivatives 3a, b which further condensed with 2,4-dinitrophenyihydrazine to give the corresponding hydrazones 4a,b. One pot reaction of 5 with different aldehydes, ethylcyanoacetate and ammoniumacetate gave pyridone derivatives 6a-e. Also. compound 5 condensed with different aldehydes then cyclized to give the pyrazoline derivatives 9a,b and 10a,b. While, on condensation of 5 with thiosemicarbazide derivatives followed by cyclization the resulting product, gave the oxathiazoline 12 and thiazolidine 13. Some of these newly synthesized compounds showed noderate activity against breast carcinoma cell line[MCF7] in human


Subject(s)
Coumarins/chemical synthesis , Cytotoxins/chemical synthesis , Breast Neoplasms/therapy , Pyridones
2.
Egyptian Journal of Chemistry. 2008; 51 (Special Issue): 91-105
in English | IMEMR | ID: emr-86357

ABSTRACT

A series of coumarin derivatives bearing heterocyclic substituents was synthesized. Bromination of the key compound 8-acetyl-7-hydroxy-4-methylcoumarin [I] under varied conditions gave the brominated derivatives II, III and IV, Conversions of III by several cyclocondensations gave the corresponding thiazole V, quinoxaline VI, quinoxalinone VIII and furanone IX derivatives. Also, methylation and cyclocondensation of the methylene-active acetyl groups of II with several aldehydes gave the corresponding pyridone various amines gave the corresponding amino side chains. Some of these newly synthesized products were studied for their chemoprophylatic effect on Schistosoma mansoni infected mice. Compound Xc a showed moderate effect


Subject(s)
Animals, Laboratory , Heterocyclic Compounds/chemistry , Chemoprevention , Thiazoles/chemistry , Quinoxalines/chemistry , Schistosoma mansoni , Mice
3.
Egyptian Journal of Chemistry. 2008; 51 (5): 701-714
in English | IMEMR | ID: emr-175532

ABSTRACT

A new series of some new N-arylidene-4-[1,2,3,4-tetrahydr onaphthalene-6-yl]thiazol-2-amine Schiff bases Il cyclized either by thioglycolic acid or thiosalicylic acid afforded thiazolidinone and benzothiazine derivatives III and IV, respectively. Also, amine I condensed with alpha-halocarbonyl compounds to give the corresponding amino derivatives V. Cyclocondcnsation of the chloroacetamido derivative Vd gave the pyrazine, quinoxaline, benzoxazine and chlorobenzoxazine derivatives VI-VIIIb, respectively. Compounds IIc, III, Vb, VI are evaluated as anticancer agents in human liver carcinoma cell line [HePG2] and breast carcinoma cell line [MCF7] and showed promising activities against these two cell lines

5.
Egyptian Journal of Chemistry. 2005; 48 (5): 587-604
in English | IMEMR | ID: emr-70474

ABSTRACT

A series of coumarin derivatives carrying different biologically active side chains and heterocyclic substituents were synthesized from 8-acetyl-4-methyl-7-hydroxycoumarin. Among these side chains are alkylamino, semicarbazono- and N[4]-substituted thiosemicarbazonoethyl, I-hydrazonoethyl and substituted I-hydroximinoethyl groups, while heterocyclic substituents were derived from pyran, oxadiazole, thiadiazole and thiazolidinone rings. Also, some derivatives of pyrano [2,3-h]chromen-9-carbaldehyde were synthesized. Some of these new products were studied for their chemoprophylactic effect in Schistosoma mansoni infected mice


Subject(s)
Chemoprevention , Schistosomiasis , Mice , Models, Animal
6.
Egyptian Pharmaceutical Journal [National Research Center]. 2004; 3: 49-65
in English | IMEMR | ID: emr-65794

ABSTRACT

2-cyclocondensation 2 underwent with different alpha-cyanocinnamonitriles to give the corresponding poly substituted pyran derivatives 3[a-d] which upon treatment with carbon disulphide gave the pyranopyrimidindithione derivatives 4[a-c]. Also, treatment of 2 with different aldehydes afforded the corresponding cinnamonitrile derivatives 5[a,b] which upon reaction with 3-methyl-1- phenylpyrazol-5-one gave the corresponding pyranopyrazole derivatives 6[a,b]. Moreover imidazo [2,3-b] thiazoles 8[a,c]; 1,2,3- thia- or 1,2,3- selena-diazoles 10[a,b]; thiazolidinones 16[a,b] and benzoxazin-4-one derivatives 18[a,b] derivatives were synthesized starting with 2-acetyltetralin. Compounds 3[c],11[b],12 were tested as antibilharzial agents and compounds 6[a],8[a] as antileukemia agents in experimental animals. Some of these compounds showed moderate activity


Subject(s)
Heterocyclic Compounds , Biological Assay , Anti-Bacterial Agents , Antineoplastic Agents , Schistosomicides , Magnetic Resonance Spectroscopy
7.
Egyptian Journal of Chemistry. 2003; 46 (1): 135-52
in English | IMEMR | ID: emr-61936

ABSTRACT

A series of some new 1,8-naphthyridine derivatives such as, 3-[2-thioxo-l,3,4-thiadiazolin-5-yl]-1,8-naphthyridines, 3-[2-substituted amino-1,3,4-thiadiazol-5-yl]-1,8-naphthyridines, 3-[6-substituted imidazo-[2,1-b]-l,3,4-thiadiazol-2-yl]-1,8-naphthyridines and other nitrogen, sulphur and/or oxygen heterocycles incorporated into 1,8-naphthyridine moities through an amide linkage has been synthesized for the purpose of biological evaluation. Compounds [2, 3, 5, 6, 8d, 10c, 11, 12, 14c] were tested for their antimicrobial activity against Gram +ve and Gram -ve bacteria and against a fungus [Aspergillus niger]. Among of these compounds only compounds 5 and 6 showed moderate activity against Aspergillus niger. Also, compounds 4a and 8c were tested against Ehrlich ascites carcinoma in mice and then measured for their cytotoxic activity against P388 Leukemia cells. Compounds 9b, 10b and 12 were tested against different types of turner cells in [USA]


Subject(s)
Biological Assay , Microbiology , Anti-Bacterial Agents , Cytotoxins
8.
Egyptian Journal of Chemistry. 1986; 29 (6): 687-94
in English | IMEMR | ID: emr-7188

ABSTRACT

The photolysis of p-quinoneimines have been casully explored. In the present investigation we examine the photolysis of 2-chloro-p-benzoquinonedibenzenesulphonimide [I] in ethanol

9.
Egyptian Journal of Pharmaceutical Sciences. 1985; 26 (1-4): 311-6
in English | IMEMR | ID: emr-5580
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