Novel thalidomide analogs: Anti-angiogenic and apoptotic effects on Hep-G2 and MCF-7 cancer cell lines

Talaat, Roba M.; Elsayed, Waheba; Agwa, Hussein S.; Gamal‐Eldeen, Amira M.; Moawia, Shaden; Zahran, M. A.

doi:10.1016/j.biomag.2014.03.002

Cited by 23 publications

(15 citation statements)

References 95 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Cell viability for all groups were measured by (3-(4,5-Dimethylthiazol)-2,5-Diphenyltetrazolium bromide) MTT assay as previously described (Talaat et al 2014). Cell suspension (200μl) adjusted at 5×10 4 cells/well were seeded in triplicates into flat-bottom 96-well tissue culture plates (Griener Labortechnik, Kremsmunster, Austria).…”

Section: Cytotoxicity Assaymentioning

confidence: 99%

“…Levels of VEGF and PDGF were quantified by ELISA using commercially available matched paired antibodies (R and D Systems Inc., Minneapolis, MN) as previously described (Talaat et al 2014). The intensity of the developed color was measured by reading optical absorbance at 450nm using a microplate ELISA reader (FLUOstar OPTIMA).…”

Section: Determination Of Vegf and Pdgf By Sandwich Enzymelinked Immumentioning

confidence: 99%

See 1 more Smart Citation

Combined Hyperthermia and Radiation Therapy for Treatment of Hepatocellular Carcinoma

Talaat

Abo-Zeid

Abo-Elfadl

et al. 2019

Asian Pac J Cancer Prev

View full text Add to dashboard Cite

Background:There is no doubt that hyperthermia is one of the powerful radiosensitizers. Finding a proper mechanism working in hyperthermia/radiation combination is still pronounced challenge.Objectives:This study is focusing on the anti-cancer activities (anti-proliferative, anti-angiogenic and antiapoptotic) of thermoradiotherapy. Materials and Methods:Liver cancer cell line (HepG2) was treated by 37oC, 40oC and 43oC hyperthermia degrees combined with three radiation doses (2 Gy, 4 Gy and 8 Gy) for 24, 48 and 72 hrs. Cell viability, apoptotic/necrotic cell screening, apoptotic (BAX and FasL) and antiapoptotic (BCL-2 and GRP78) genes, and pro-angiogenic mediators [vascular endothelial- (VEGF) and Platelet derived-growth factors (PDGF) ware investigated. Results:Our data showed that 40oC temperature combined with 4 Gy radiation gives a significant decrease (p<0.05) in cell viability. Maximum cytotoxicity was reported 48 hr post-treatment followed by slight restoration of cell viability after 72 hr. Compared with untreated cells, only 5% of viable cells with a high percentage of apoptotic (31%) and necrotic (63%) cells were demonstrated in 40oC/4 Gy/48 hr group. Expression of pro-apoptotic genes (BAX and FasL) were increased after hyperthermia with apparent elevation in 40oC/4 Gy/48 hr group coincides with moderate expression of antiapoptotic BCL-2 and GRP78 genes. A significant reduction (p<0.001; p<0.05) in VEGF and PDGF levels; respectively was shown at 40oC/4 Gy/48 hr group. Conclusions:This pilot study proposed 40oC mild temperature hyperthermia as a favorable hyperthermal condition with 4 Gy radiotherapy in HCC treatment. A further research has to be performed considering an application of more than one session of radiothermal therapy at 40oC/4 Gy for total abrogation of cancer cells.

show abstract

Section: Cytotoxicity Assaymentioning

confidence: 99%

Section: Determination Of Vegf and Pdgf By Sandwich Enzymelinked Immumentioning

confidence: 99%

Combined Hyperthermia and Radiation Therapy for Treatment of Hepatocellular Carcinoma

Talaat

Abo-Zeid

Abo-Elfadl

et al. 2019

Asian Pac J Cancer Prev

View full text Add to dashboard Cite

show abstract

“…Based on these results and assumption, new series of phthalimide derivatives were synthesized and evaluated as potential antitumor drug candidates [6,7]. Recently, our group reported the potency of the thalidomide dithiocarbamate analogs as novel antitumor derivatives [8][9][10][11][12][13][14]. On the other hand, dithiocarbamic acid esters have drawn a great attention due to their cancer chemopreventive and antitumor activities [15,16].…”

Section: Introductionmentioning

confidence: 99%

“…On the other hand, dithiocarbamic acid esters have drawn a great attention due to their cancer chemopreventive and antitumor activities [15,16]. Some molecules that incorporated dithiocarbamic acid ester functionality, as a linker between different pharmacophores, showed significant anticancer activities, such as TH derivatives [8][9][10][11][12][13][14], chromones [17], quinazolinones [18] and naphthalimide derivatives [19].…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

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

et al. 2017

Self Cite

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

Synthesis and Evaluation of Thalidomide and Phthalimide Esters as Antitumor Agents

Zahran

Abdin

Osman

et al. 2014

Archiv der Pharmazie

View full text Add to dashboard Cite

A series of thalidomide and phthalimide ester analogs were efficiently synthesized from N-chloromethylthalidomide, N-chloromethylphthalimide, and N-(2-bromoethyl)phthalimide derivatives with various biologically important carboxylic acids. The synthesized compounds were purified and characterized by various chromatographic and spectroscopic techniques. The antitumor activity of all the synthesized compounds was screened against human liver and breast cancer cells, which showed that phthalimide ester 6a was the best cytotoxic compound against MCF7 cells, while all of the tested compounds showed a non-cytotoxic effect against HepG2 cells. Compounds 5a, 6a, and 7a possess immunosuppressant effect, while compounds 5c, 5d, 6c, 6d, 7c, and 7d showed an immunostimmulatory effect. Meanwhile, estimation of the binding affinity for all the synthesized compounds toward the vascular endothelial growth factor receptor (VEGFR) showed that compounds 5a, 5b, and 7d were the most potent inhibitors.

show abstract

Novel thalidomide analogs: Anti-angiogenic and apoptotic effects on Hep-G2 and MCF-7 cancer cell lines

Cited by 23 publications

References 95 publications

Combined Hyperthermia and Radiation Therapy for Treatment of Hepatocellular Carcinoma

Combined Hyperthermia and Radiation Therapy for Treatment of Hepatocellular Carcinoma

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

Synthesis and Evaluation of Thalidomide and Phthalimide Esters as Antitumor Agents

Contact Info

Product

Resources

About