ChemInform Abstract: Efficient Microwave Irradiation Enhanced Stereoselective Synthesis and Antitumor Activity of Indolylchalcones and Their Pyrazoline Analogues.

Zahran, M. A.; Salama, Hanan F.; Abdin, Yasmin G.; Gamal‐Eldeen, Amira M.

doi:10.1002/chin.201049108

Cited by 5 publications

(5 citation statements)

References 1 publication

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Based on our previous studies which involved the synthesis and evaluation of novel thalidomide analogs as anticancer and antiangiogenic agents and the diversity of biological activities of indole derivatives, the current study aimed to synthesize and evaluate novel phthalimide–indole hybrids as antimicrobial, antitumor, and anti‐hepatic fibrosis agents.…”

Section: Introductionmentioning

confidence: 99%

Design, synthesis, biological evaluations, molecular docking, and in vivo studies of novel phthalimide analogs

Zahran

El‐Aarag

Mehany

et al. 2018

Archiv der Pharmazie

Self Cite

View full text Add to dashboard Cite

A series of novel phthalimide analogs containing an indole or brominated indole moiety were synthesized and their antimicrobial activity was evaluated. Compound 8 showed a broad spectrum activity, revealing 53-67% of erythromycin activity on the tested bacteria and 60-70% of miconazole activity on the tested fungi. Anticancer activity was evaluated on the cell lines HepG2, MCF-7, A549, H1299, and Caco2. The results revealed that the new phthalimide analog 8 has broad-spectrum anticancer activity toward all the tested cancer cell lines, followed by compound 11, which showed good activity toward all the tested cell lines except for MCF-7. The ability of the promising analogs 5, 8, and 11 to bind to topoisomerase II DNA gyrase was investigated. Caspase-3 activation and Bcl-2 assay of the best active derivatives 8, 11 in addition to compound 5 were evaluated. The antifibrotic activity was studied in an in vivo model and the histopathological studies revealed that treatment with the new compound 8 improved the fibrotic liver tissues to normality.

show abstract

Section: Introductionmentioning

confidence: 99%

Design, synthesis, biological evaluations, molecular docking, and in vivo studies of novel phthalimide analogs

Zahran

El‐Aarag

Mehany

et al. 2018

Archiv der Pharmazie

Self Cite

View full text Add to dashboard Cite

show abstract

“…[22][23][24][25] Microwave assisted organic synthesis (MAOS) has become increasingly popular in recent years to improve the yields and shorten reaction time in a variety of reactions. 26,27 Hence, in continuation of our interest on indole derivatives, 28 the utility of microwave irradiation in organic synthesis and the evaluation of different classes of heterocyclic nucleus as anti cancer bioactive compounds, 29,30 we presented in this context an efficient and facile microwave N-alkylation of indole-3-carbaldehyde derivatives and their ClaisenSchmidt condensation with 1-biphenyl-4-yl-ethanone to afford novel indolylchalcones and investigation of their antitumor activity as well as their binding capability to genomic DNA extracted from bacteria.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and cellular cytotoxicities of new N-substituted indole-3-carbaldehyde and their indolylchalcones

Zahran

Ibrahim

2009

J Chem Sci

Self Cite

View full text Add to dashboard Cite

A simple and efficient method for N-alkylation of indole-3-carbaldehyde derivatives using a mixture of different bases in DMF under conventional and microwave irradiation conditions to afford N-substituted indole-3-carbaldehyde derivatives 3a-o is reported. These derivatives which undergo Claisen-Schmidt condensation with 1-biphenyl-4-yl-ethanone yielded the corresponding indolylchalcone derivatives 5a-h. A comparative study showed that the microwave irradiation condition afforded excellent yield and shorten reaction time of all the synthesized indole derivatives which possess promising antitumor activity as well as interchelation bioactivity of indolylchalcones 5a-h with DNA.

show abstract

“…Our research interest is still existing in development of TH analogs and potential antitumor compounds [8][9][10][11][12][13][14][20][21][22]. So, we herein describe the design, synthesis and biological evaluation of novel dithiocarbamate analogs connected either through methylene or ethylene bridges to phthalimide pharmacophoric core.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and biological evaluation of phthalimide dithiocarbamate and dithioate derivatives as anti-proliferative and anti-angiogenic agents-I

et al. 2017

View full text Add to dashboard Cite

A facile synthesis of new phthalimide dithiocarbamate and dithioate analogs 8a-j, 9a-e and 9g-j were achieved by the reaction of N-chloromethyl and N-bromoethylphthalimide with carbon disulfide (CS2) and various amines. The structures of the synthesized analogs were elucidated by spectroscopic methods, including IR, 1 H NMR and 13 C NMR, and ESI-HRMS techniques. The antiproliferative activity of the newly synthesized compounds was also evaluated against various human cancer cell lines. The compound 9e and 9i exhibited the highest activity against human breast adenocarcinoma MCF-7 and hepatocellular carcinoma HepG2 cells. Compound 8f showed better antiproliferative effect against colon carcinoma HCT-116 and cervical carcinoma HeLa compared to thalidomide. The binding affinity to vascular endothelial growth factor receptor (VEGFR) of some compounds was assessed in addition to molecular docking study. Compounds 9e and 9i showed high docking score values and they significantly declined the concentration of VEGFR. KEYWORDS

show abstract

ChemInform Abstract: Efficient Microwave Irradiation Enhanced Stereoselective Synthesis and Antitumor Activity of Indolylchalcones and Their Pyrazoline Analogues.

Cited by 5 publications

References 1 publication

Design, synthesis, biological evaluations, molecular docking, and in vivo studies of novel phthalimide analogs

Design, synthesis, biological evaluations, molecular docking, and in vivo studies of novel phthalimide analogs

Synthesis and cellular cytotoxicities of new N-substituted indole-3-carbaldehyde and their indolylchalcones

Synthesis and biological evaluation of phthalimide dithiocarbamate and dithioate derivatives as anti-proliferative and anti-angiogenic agents-I

Contact Info

Product

Resources

About