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Articles by Said A. Said
Total Records ( 2 ) for Said A. Said
  Said A. Said , Abd El-Galil E. Amr , Hassan A. El- Sayed , Mohamed A. Al- Omar and Mohamed M. Abdalla
  Some of synthesized heterocyclic pyrimidine, pyrimidine, furopyridine derivatives and their nucleoside candidates (2-14) were previously prepared and were founded to have some aspects of structural similarity with many anti-inflammatory agents. Therefore, these agents were screened for this property. The evaluation of the anti-inflammatory activities was based on evaluation of the abilities of these compounds in protection against carrageenan-induced edema. The anti-inflammatory activities of the tested compounds further confirmed based on evaluation of the abilities of these compounds to inhibit plasma PGE2. These compounds showed potent anti-inflammatory activity with low toxicity (LD50) comparable to Valdicoxib® as reference anti-inflammatory drugs.
  Said A. Said , Hassan A. El-Sayed , Abd El-Galil E. Amr and Mohamed M. Abdalla
  A series of the newly substituted thienopyrimidine derivatives 2-13 were synthesized by using 3-amino-6-(4-chlorophenyl)-4-(4-isopropylphenyl) thieno[2,3-b]pyridine-2-carbohydrazide 1 as starting material. Reaction of compound 1 with p-nitrobenzaldehyde in refluxing ethanol afforded the corresponding Shiff base 2, which was cyclized with triethyl orthoformate to give thienopyrimidine derivative 3. Compound 1 was treated with formic acid or acetic anhydride to afford the corresponding thienopyrimidines 4 and 5, respectively. Treatment of 1 with acetylacetone afforded pyrazolothienopyrimidine 6. Treatment of 1 with triethyl orthoformate, carbon disulfide, dimethylformamide and ethyl acetoacetate or diethyl malonate gave compounds 7-11, respectively. Cyclization of 1 with m-nitrophthalic anhydride or formaldehyde afforded thienopyrimidines 12 and 13, respectively. The newly synthesized compounds were found to be potent selective and orally bioavailable CHK1 inhibitors. This elucidated and confirmed via determination of checkpoint abrogation, antiproliferative activity and potentiation of genotoxic drug efficacy in cancer cell lines and also determination of compound concentrations in vivo at selected time points following i.v. and oral dosing.
 
 
 
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