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Said M.M.,National Research Center of Egypt | Abdulla M.,Hi Care Pharmaceutical Co.
Egyptian Journal of Chemistry | Year: 2012

A SERIES of pyrimidine and fused triazolopyrimidine derivatives were newly synthesized using aminopyrazole carbonitrile 1 as a had starting material and compounds 14 and 16 are intermediates. Initially, the acute toxicity of the compounds was assayed via the determination of their LD50, and all compounds were interestingly less toxic and had lower ulcerogenic activities than Diclophenac® as a reference drug. Regarding the protection against Carrageenan induced edema; the pharmacological screening showed that compounds 17, 11, 13 and 5 have good anti-inflammatory activities comparable to the reference drug. On the other hand, in searching for COX-2 inhibitor, the inhibition of plasma prostaglandine (PGE2) for the compounds was determined and the same four compounds were found the more potent agents. The detailed synthesis, spectroscopic data, pharmacological screening and acute toxicity LD50 for the synthesized compounds were reported.


Farag A.M.,Cairo University | Ali K.A.K.,National Research Center of Egypt | El-Debss T.M.A.,Cairo University | Mayhoub A.S.,Al - Azhar University of Egypt | And 4 more authors.
European Journal of Medicinal Chemistry | Year: 2010

The versatile hitherto unreported 3-[(E)-3-(dimethylamino)acryloyl]-1,5- diphenyl-1H-pyrazole-4-carbonitrile (3) was prepared via the reaction of 3-acetyl-1,5-diphenyl-1H-pyrazole-4-carbonitrile (1) with dimethylformamid- dimethylacetal (DMF-DMA). The latter product and 3-((E)-3-morpholin-4-yl- acryloyl)-1,5-diphenyl-1H-pyrazole-4-carbonitrile (4) underwent regioselective 1,3-dipolar cycloaddition with nitrilimines to afford the corresponding pyrazole derivatives. In vivo anti-estrogenic activity and acute toxicity after single oral dose of the newly synthesized compounds were evaluated. In vitro disease-oriented primary antitumor screening utilizing 14 cell lines of breast and ovarian tumor subpanels has been also carried out. All tested compounds showed anti-estrogenic properties equipotent or superior to the reference drug, letrozole. 3-[3-(4-Cyano-1,5-diphenyl-1H-pyrazole-3-yl)-1-(4-methylphenyl)-1H- pyrazole-4-carbonyl]-1,5-diphenyl-1H-pyrazole-4-carbonitrile (27c) and 3-(3-acetyl-1-phenyl-1H-pyrazole-4-carbonyl)-1,5-diphenyl-1H-pyrazole-4- carbonitrile (8a) showed a significant cytotoxic activity in a nanomolar range against certain types of breast and ovarian tumors with tolerable toxicity. © 2010 Elsevier Masson SAS. All rights reserved.


Shalaby A.M.,National Research Center of Egypt | Al-Salam O.I.A.,National Research Center of Egypt | Kalmouch A.,National Research Center of Egypt | El-Shihaby S.E.,National Research Center of Egypt | Abdullah M.,Hi Care Pharmaceutical Co.
Egyptian Journal of Chemistry | Year: 2013

A NEW series of N-3-(2-furanyl) acryloyl, N-3-(5-methyl)-2-(furanyl)-acryoyl amino acids, peptide and piprazines amids, were structurally designed and synthesized. About 23 compounds (5a-w) were synthesized and their anti-allergic and anti-inflamatory activities were evaluated relative to those of Loratadine (Clorinix®) and Diclofenac®. All the obtained products showed good anti-allergic activities with the greatest activities recorded for compounds (5g, 5h, 5j, 5k, 5m, 5n, 5v and 5w). All compounds showed LD50 with safety margin. On the other hand most compounds have no anti-inflamatory activities except products (5d, 5e and 5p).


Farag A.M.,Cairo University | Mayhoub A.S.,Al - Azhar University of Egypt | Eldebss T.M.A.,Cairo University | Amr A.-G.E.,National Research Center of Egypt | And 3 more authors.
Archiv der Pharmazie | Year: 2010

Several 4-cyano-1,5-diphenylpyrazoles attached to different heterocyclic ring systems at position 3 were synthesized starting from ethyl 4-cyano-1,5-diphenyl-1H-pyrazole-3-carboxylate 1. The newly synthesized compounds were tested in vivo for their anti-estrogenic effects and evaluated in vitro for their cytotoxic properties against estrogen-dependent tumors. 3-(5-Mercapto-1,3,4-oxadiazole-2-yl)-1,5-diphenyl-1H-pyrazole-4-carbonitrile 13 revealed the highest cytotoxic activity with a GI50 value equal to 40 nM against the IGROVI ovarian tumor cell line. It also showed an anti-estrogen activity 1.6 more effective than the reference drug, in addition to a high tolerable dose. 3-(5-(Methylthio)-4-phenyl-4H-1,2,4-triazol-3-yl)-1,5-diphenyl- 1H-pyrazole-4-carbonitrile 7 was found to have the highest anti-estrogenic activity, while 1,5-diphenyl-3-[5-(phenylamino)-1,3,4-thiadiazol-2-yl]-1H- pyrazole-4-carbonitrile 11 showed the lowest activity. The oral LD50 values revealed that most of the tested compounds are relatively nontoxic. © 2010 Wiley-VCH Verlag GmbH & Co. KGaA.


Attaby F.A.,Cairo University | Abdel-Fattah A.M.,Cairo University | Shaif L.M.,Cairo University | Elsayed M.M.,Hi Care Pharmaceutical Co.
Journal of Heterocyclic Chemistry | Year: 2014

1-Pyridin-3-yl-3-(2-thienyl of 2-furyl)prop-2-en-1-ones 1a, 1b reacted with 2-cyanoethanethioamide 2 to afford the corresponding 4-(thiophen-2-yl or furan-2-yl)-6-sulfanyl-2,3′-bipyridine-5-carbonitriles 3a, 3b. The synthetic potentiality of compounds 3a, 3b were investigated in the present study via their reactions with several active halogen containing compounds 4a-h. Our aim here is the synthesis of 4-(2-thienyl or 2-furyl)-6-pyridin-3- ylthieno[2,3-b]pyridin-3-amines 6a-e, g-n, via 6-(alkyl-thio)-4-(2-thienyl or 2-furyl)-2,3′-bipyridine-5-carbonitriles 5a-e, i-m. The structures of all newly synthesized heterocyclic compounds were elucidated by considering the data of IR, 1H-NMR, mass spectra, as well as that of elemental analyses. Anti-cancer, anti-Alzheimer, and anti-COX-2 activities were investigated for all the newly synthesized heterocyclic compounds. © 2013 HeteroCorporation.

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