Publications by authors named "Ahmed A Fayed"

9 Publications

  • Page 1 of 1

In Vitro and In Vivo Anti-Breast Cancer Activities of Some Newly Synthesized 5-(thiophen-2-yl)thieno-[2,3-d]pyrimidin-4-one Candidates.

Molecules 2019 Jun 17;24(12). Epub 2019 Jun 17.

Zoology Department, Bioproducts Research Chair, Faculty of Science, King Saud University, Riyadh 11451, Saudi Arabia.

In this study, some of new thiophenyl thienopyrimidinone derivatives - were prepared and tested as anti-cancer agents by using thiophenyl thieno[2,3-d]pyrimidinone derivative as a starting material, which was prepared from cyclization of ethyl ester derivative with formamide. Treatment of with ethyl- chloroacetate gave thienopyrimidinone -ethylacetate , which was reacted with hydrazine hydrate or anthranilic acid to afford acetohydrazide and benzo[d][1,]oxazin-4-one respectively. Condensation of with aromatic aldehydes or phenylisothiocyanate yielded Schiff base derivatives , and thiosemicarbazise , which were treated with 2-mercaptoacetic acid or chloroacetic acid to give the corresponding thiazolidinones , and phenylimino-thiazolidinone , respectively. Treatment of with ethylacetoacetate or acetic acid/acetic anhydride gave pyrazole and acetyl acetohydrazide derivatives, respectively. The latter compound was reacted with ethyl cycno-acetate or malononitrile to give and , respectively. In this work, we have studied the anti-cancer activity of the synthesized thienopyrimidinone derivatives against MCF-7 and MCF-10A cancer cells. Furthermore, in vivo experiments showed that the synthesized compounds significantly reduced tumor growth up to the 8 day of treatment in comparison to control animal models. Additionally, the synthesized derivatives showed potential inhibitory effects against pim-1 kinase activities.
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http://dx.doi.org/10.3390/molecules24122255DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6631792PMC
June 2019

Potent Anti-Ovarian Cancer with Inhibitor Activities on both Topoisomerase II and BRAF of Synthesized Substituted Estrone Candidates.

Molecules 2019 May 29;24(11). Epub 2019 May 29.

Atos Pharma, Elkatyba Land, Belbis 44621, El Sharkya, Egypt.

A series of 16-(α-alkoxyalkane)-17-hydrazino-estra-1(10),2,4-trien[17,16-c]-3-ol (-) and estra-1(10),2,4-trien-[17,16-c]pyrazoline-3-ol derivatives (-) were synthesized from corresponding arylidines which was prepared from estrone as starting material. Condensation of 1 with aldehydes gave the corresponding arylidine derivatives which were treated with hydrazine derivatives in alcohols to give the corresponding derivatives -, respectively. Additionally, treatment of with methyl- or phenylhydrazine in ethanolic potassium hydroxide afforded the corresponding N-substituted pyrazoline derivatives -, respectively. All these derivatives showed potent anti-ovarian cancer both in vitro and in vivo The mechanism of anti-ovarian cancer was suggested to process via topoisomerase II and BRAF inhibition.
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http://dx.doi.org/10.3390/molecules24112054DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6600292PMC
May 2019

Synthesis and antimicrobial activity of some new substituted pyrido[3',2':4,5]thieno[3,2-d]-pyrimidinone derivatives.

Bioorg Khim 2014 May-Jun;40(3):335-40

A series of new 3-substituted-7-(2-chloro-6-ethoxypyridin-4-yl)-9-(2,4-dichlorophenyl)-2-methylpyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4(3H)-one derivatives were synthesized as antimicrobial agents using 7-(2-chloro-6-ethoxypyridin-4-yl)-9-(2,4-dichlorophenyl)-2-methyl-4H-pyrido[3',2':4,5]thieno[3,2-d]-[1,3]oxazin-4-one as a starting compound. Its condensation with substituted aniline derivatives or phenyl hydrazine gave the corresponding N-substituted derivatives. Treatment of the starting compound with hydrazine hydrate afforded the corresponding N-amino derivative, which was reacted with substituted phenylisocyanate and phenylisothiocyanate derivatives to give the corresponding semicarbazides and thiosemicarbazide derivatives. All the newly synthesized compounds were evaluated for their antimicrobial activities in comparison to streptomycin and fusidic acid as positive controls. The structure assignments of the new compounds are based on chemical and spectroscopic evidence.
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June 2015

Androgen receptor antagonists and anti-prostate cancer activities of some newly synthesized substituted fused pyrazolo-, triazolo- and thiazolo-pyrimidine derivatives.

Int J Mol Sci 2014 Nov 24;15(11):21587-602. Epub 2014 Nov 24.

Pharmacology and Toxicology Department, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.

A series of substituted pyrazole, triazole and thiazole derivatives (2-13) were synthesized from 1-(naphtho[1,2-d]thiazol-2-yl)hydrazine as starting material and evaluated as androgen receptor antagonists and anti-prostate cancer agents. The newly synthesized compounds showed potent androgen receptor antagonists and anti-prostate cancer activities with low toxicity (lethal dose 50 (LD50)) comparable to Bicalutamide as reference drug. The structures of newly synthesized compounds were confirmed by IR, 1H-NMR, 13C-NMR, and MS spectral data and elemental analysis. The detailed synthesis, spectroscopic data, LD50 values and pharmacological activities of the synthesized compounds are reported.
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http://dx.doi.org/10.3390/ijms151121587DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4264242PMC
November 2014

Synthesis and pharmacological activities of some new triazolo- and tetrazolopyrimidine derivatives.

Molecules 2013 Dec 6;18(12):15051-63. Epub 2013 Dec 6.

Pharmacology and Toxicology Department, College of Pharmacy, Taibah University, Al-Madinah Al-Munawara 3893, Saudi Arabia.

A new series of fused triazolo- and tetrazolopyrimidine derivatives 2-14 were synthesized and their anti-inflammatory and ulcerogenic activities were evaluated. The pharmacological screening showed that many of these obtained compounds have good anti-inflammatory activities, comparable to the reference drug. The toxicity of the compounds was also assayed via the determination of their LD50 values. The structures of newly synthesized compounds were confirmed by IR, 1H-NMR, MS spectral data and elemental analysis.
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http://dx.doi.org/10.3390/molecules181215051DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6269734PMC
December 2013

Anti-parkinsonism, hypoglycemic and anti-microbial activities of new poly fused ring heterocyclic candidates.

Int J Biol Macromol 2013 Jun 15;57:165-73. Epub 2013 Mar 15.

Pharmacology and Toxicology Department, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.

A new series of poly fused pyrazolothienopyrimidine derivatives (2-14) were synthesized and their anti-parkinsonism, hypoglycemic and anti-microbial activities were evaluated. Some of the newly synthesized compounds exhibited better pharmacological and biological activities than the reference controls with low concentrations. The structures of newly synthesized compounds were confirmed by chemical, elemental and spectroscopic evidences. The detailed synthesis, spectroscopic data, and pharmacological activities were reported.
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http://dx.doi.org/10.1016/j.ijbiomac.2013.03.019DOI Listing
June 2013

Synthesis of new macrocyclic polyamides as antimicrobial agent candidates.

Molecules 2012 Dec 6;17(12):14510-21. Epub 2012 Dec 6.

Applied Organic Chemistry Department, National Research Center, Dokki 12622, Cairo, Egypt.

A series of macrocyclic imides and Schiff-bases have been prepared via the cyclocondensation of pyridine-2,6-dicarbonyl dichloride (1) with L-ornithine methyl ester to give the corresponding macrocyclic bisester 2. Treatment of 2 with hydrazine hydrate gave macrocyclic bisacid hydrazide 3, which was used as starting material. Condensation of bishydrazide 3 with diacid anhydrides or aromatic aldehydes in refluxing acetic acid or ethanol gave the corresponding macrocyclic bisimides 4, 5a,b and macrocyclic bis- hydrazones 6a-j, respectively. The structure assignments of the new compounds were based on chemical and spectroscopic evidence. The antimicrobial screening showed that many of these newly synthesized compounds have good antimicrobial activities, comparable to ampicillin and ketaconazole used as reference drugs.
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http://dx.doi.org/10.3390/molecules171214510DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268893PMC
December 2012

Pharmacological activities of some new polycyclic triazolopyrazolopyridazine derivatives.

Int J Biol Macromol 2012 Jul-Aug;51(1-2):7-17. Epub 2012 May 8.

Pharmacy Department, College of Medical Rehabilitation Sciences, Taibah University, Madinah Munawara, Saudi Arabia.

In continuation of our previous work, a novel series of polycyclic derivatives were synthesized and their anti-inflammatory, analgesic and antimicrobial activities were evaluated. Initially the acute toxicity of the compounds was assayed via the determination of their LD(50). Some of the newly compounds exhibited better biological and pharmacological activities than the reference controls with low toxicity (LD(50)). The structure of the new compounds has been established on the bases of chemical and spectroscopic evidences. The detailed synthesis, spectroscopic data, LD(50) and pharmacological activities of the synthesized compounds were reported.
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http://dx.doi.org/10.1016/j.ijbiomac.2012.05.002DOI Listing
October 2012
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