Publications by authors named "Said A S Ghozlan"

4 Publications

  • Page 1 of 1

Recent Synthetic Approaches and Biological Evaluations of Amino Hexahydroquinolines and Their Spirocyclic Structures.

Anticancer Agents Med Chem 2019 ;19(7):875-915

Chemistry Department, Faculty of Science, Cairo University, Giza, Egypt.

In this review, the recent synthetic approaches of amino hexahydroquinolines and their spirocyclic structures were highlighted. The synthetic routes include, two-components, three-components or fourcomponents reactions. The two-component [3+3] atom combination reaction represents the simplest method. It involves Michael addition of the electron rich β-carbon of β-enaminones to the activated double bond of cinnamonitriles followed by cyclization to yield hexahydroquinoline compounds. The bioactivity profiles and SAR studies of these compounds were also reviewed with emphasis to the utility of these substances as antimicrobial, anticancer and antitubercular agents, as well as calcium channel modulators.
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http://dx.doi.org/10.2174/1871520619666190131140436DOI Listing
February 2020

Expression of Reactive Oxygen Species-Related Transcripts in Egyptian Children With Autism.

Biomark Insights 2017 23;12:1177271917691035. Epub 2017 Feb 23.

Microbial Biotechnology Department, Genetic Engineering Division, National Research Centre, Giza, Egypt.

The molecular basis of the pathophysiological role of oxidative stress in autism is understudied. Herein, we used polymerase chain reaction (PCR) array to analyze transcriptional pattern of 84 oxidative stress genes in peripheral blood mononuclear cell pools isolated from 32 autistic patients (16 mild/moderate and 16 severe) and 16 healthy subjects (each sample is a pool from 4 autistic patients or 4 controls). The PCR array data were further validated by quantitative real-time PCR in 80 autistic children (55 mild/moderate and 25 severe) and 60 healthy subjects. Our data revealed downregulation in , and transcripts (1.5, 3.8, 1.2, 1.7, and 2.2, respectively; < .05 for all) in autistic group compared with controls. In addition, and exhibited 1.4- and 1.7-fold downregulation, respectively, in severe autistic patients when compared with mild/moderate group ( = .005 and .0008, respectively). This study helps in a better understanding of the underlying biology and related genetic factors of autism, and most importantly, it presents suggested candidate biomarkers for diagnosis and prognosis purposes as well as targets for therapeutic intervention.
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http://dx.doi.org/10.1177/1177271917691035DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5391985PMC
February 2017

Cytotoxic and antimicrobial evaluations of novel apoptotic and anti-angiogenic spiro cyclic 2-oxindole derivatives of 2-amino-tetrahydroquinolin-5-one.

Arch Pharm (Weinheim) 2015 Feb;348(2):113-24

Department of Chemistry, Faculty of Science, Cairo University, Giza, Egypt.

A novel series of cyclic 2-oxindole derivatives incorporating 2-amino-tetrahydroquinolin-5-one were prepared. The structures of the prepared compounds were elucidated using different spectral tools. The regio-orientation of the reaction products was elucidated through NOE difference experiments and through using substituents on the ortho position to affect further cyclization. Antitumor and antimicrobial evaluations were performed on the prepared compounds. Most of these compounds exhibited high to moderate antimicrobial activity. With respect to the antitumor activity, the compounds showed more potent cytotoxic effect only toward the human breast cancer cell line MCF-7. Also, we found that derivatives containing an ester group (8c, 11b, 14b, and 15b) are more active than those containing a cyanide group (8a, 11a, 14a, and 15a). Moreover, compounds 15b and 8b are the most active derivatives in this group. These two compounds showed apoptotic inhibition of the proliferation of human breast adenocarcinoma MCF-7 cells through DNA fragmentation, induction of the tumor suppressor protein p53, induction of caspase-9, and finally the inhibition of angiogenesis by decreasing vascular endothelial growth factor expression and secretion.
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http://dx.doi.org/10.1002/ardp.201400304DOI Listing
February 2015

An easy synthesis of 5-functionally substituted ethyl 4-amino-1-aryl- pyrazolo-3-carboxylates: interesting precursors to sildenafil analogues.

Beilstein J Org Chem 2007 May 1;3:15. Epub 2007 May 1.

Department of Chemistry, Faculty of Science, Cairo University, Giza, A. R. Egypt.

3-Oxo-2-arylhydrazononitriles 1a-c react readily with chloroacetonitrile, ethyl chloroacetate, and with phenacyl chloride to give 4-aminopyrazoles 4a-e. The pyrazolo[4,3-d]pyrimidine derivatives 7 and 10 are synthesized via reaction of the aminopyrazole 4b with phenylisothiocyanate and DMFDMA/NH4OAc respectively.
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http://dx.doi.org/10.1186/1860-5397-3-15DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1885264PMC
May 2007
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