scholarly journals Synthesis of the 6-Substituted Imidazo[1,2-a]Pyridine-3-yl-2- Phosphonopropionic Acids as Potential Inhibitors of Rab Geranylgeranyl Transferase

2021 ◽  
Vol 8 ◽  
Author(s):  
Damian Kusy ◽  
Aleksandra Marchwicka ◽  
Joanna Małolepsza ◽  
Katarzyna Justyna ◽  
Edyta Gendaszewska-Darmach ◽  
...  
Keyword(s):  
Carboxylic Acid ◽  
Hela Cell ◽  
Cell Line ◽  
Cervical Carcinoma ◽  
Pyridine Ring ◽  
Hela Cell Line ◽  
Human Cervical Carcinoma ◽  
Geranylgeranyl Transferase ◽  
Potential Inhibitors ◽  
Inactive Analog

Twelve phosphonopropionates derived from 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid (3-IPEHPC) were synthesized and evaluated for their activity as inhibitors of protein geranylgeranylation. The nature of the substituent in the C6 position of imidazo[1,2-a]pyridine ring was responsible for the compound's activity against Rab geranylgeranyl transferase (RGGT). The most active inhibitors disrupted Rab11A prenylation in the human cervical carcinoma HeLa cell line. The esterification of carboxylic acid in the phosphonopropionate moiety turned the inhibitor into an inactive analog.

scholarly journals Oridonin induces apoptosis via PI3K/Akt pathway in cervical carcinoma HeLa cell line

2007 ◽  
Vol 28 (11) ◽  
pp. 1819-1826 ◽  
Author(s):  
Hong-zhen Hu ◽  
Yue-bo Yang ◽  
Xiang-dong Xu ◽  
Hong-wei Shen ◽  
Yi-min Shu ◽  
...  
Keyword(s):  
Hela Cell ◽  
Cell Line ◽  
Cervical Carcinoma ◽  
Akt Pathway ◽  
Hela Cell Line

scholarly journals ANTICANCER ACTIVITY OF CALANONE ON HeLa CELL LINE

2010 ◽  
Vol 10 (2) ◽  
pp. 240-244 ◽  
Author(s):  
Heny Ekowati ◽  
Indwiani Astuti ◽  
Mustofa Mustofa
Keyword(s):  
Hela Cell ◽  
Cytotoxic Activity ◽  
Anticancer Activity ◽  
Cell Line ◽  
Cervical Carcinoma ◽  
Carcinoma Cell ◽  
Suppressor Gene ◽  
Positive Control ◽  
Hela Cell Line ◽  
P53 Expression

Calanone (coumarin derivate compound), isolated from Calophyllum sp. had been shown to have cytotoxic activity on leukemia L1210 cell line with IC50 = 59.40 mg/mL. Calanone presumed have anticancer activity on HeLa cervical carcinoma cell. This study was conducted to investigate the cytotoxic and apoptotic activity of calanone and its effect to p53 and p21 expression on HeLa cervical carcinoma cell. Cytotoxic assay of calanone was performed on HeLa cell line, using MTT assay. Apoptotic assay was performed on HeLa cell line incubated with calanone for 24 h, by immunofluororescence method, using fluorochromes ethidium bromide and acridine orange. Expression of p53 was examined on HeLa cell line, by PCR with p53 wild-type primer. Expression of p21 was examined on HeLa cell line, by immunohistochemistry method. 5-fluorourasil was used as positive control in cytotoxic, apoptotic assay, and p53 expression. The result showed that calanone has cytotoxic activity on HeLa cell line, with IC50 = 22.887 mg/mL, caused cytotoxicity through apoptotic mechanism, increase p53 tumor suppressor gene expression, while the p21 expression test showed a negative result.   Keywords: Calanone, cytotoxic, HeLa cell line

Identification and Expression Analysis of CD73 Inhibitors in Cervical Cancer

2020 ◽  
Vol 16 ◽  
Author(s):  
Jamshed Iqbal ◽  
Ayesha Basharat ◽  
Sehrish Bano ◽  
Syed Mobasher Ali Abid ◽  
Julie Pelletier ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Cervical Cancer ◽  
Western Blot ◽  
Hela Cell ◽  
Cell Line ◽  
Cell Apoptosis ◽  
Immunofluorescence Staining ◽  
Cell Cycle Analysis ◽  
Hela Cell Line ◽  
Cell Line Hela

Aims: The present study was conducted to examine the inhibitory effects of synthesized sulfonylhydrazones on the expression of CD73 (ecto-5′-NT). Background: CD73 (ecto-5′-NT) represents the most significant class of ecto-nucleotidases which are mainly responsible for dephosphorylation of adenosine monophosphate to adenosine. Inhibition of CD73 played an important role in the treatment of cancer, autoimmune disorders, precancerous syndromes, and some other diseases associated with CD73 activity. Objective: Keeping in view the significance of CD73 inhibitor in the treatment of cervical cancer, a series of sulfonylhydrazones (3a-3i) derivatives synthesized from 3-formylchromones were evaluated. Methods: All sulfonylhydrazones (3a-3i) were evaluated for their inhibitory activity towards CD73 (ecto-5′-NT) by the malachite green assay and their cytotoxic effect was investigated on HeLa cell line using MTT assay. Secondly, most potent compound was selected for cell apoptosis, immunofluorescence staining and cell cycle analysis. After that, CD73 mRNA and protein expression were analyzed by real-time PCR and Western blot. Results: Among all compounds, 3h, 3e, 3b, and 3c were found the most active against rat-ecto-5′-NT (CD73) enzyme with IC50 (µM) values of 0.70 ± 0.06 µM, 0.87 ± 0.05 µM, 0.39 ± 0.02 µM and 0.33 ± 0.03 µM, respectively. These derivatives were further evaluated for their cytotoxic potential against cancer cell line (HeLa). Compound 3h and 3c showed the cytotoxicity at IC50 value of 30.20 ± 3.11 µM and 86.02 ± 7.11 µM, respectively. Furthermore, compound 3h was selected for cell apoptosis, immunofluorescence staining and cell cycle analysis which showed promising apoptotic effect in HeLa cells. Additionally, compound 3h was further investigated for its effect on expression of CD73 using qRT-PCR and western blot. Conclusion: Among all synthesized compounds (3a-3i), Compound 3h (E)-N'-((6-ethyl-4-oxo-4H-chromen-3-yl) methylene)-4-methylbenzenesulfonohydrazide was identified as most potent compound. Additional expression studies conducted on HeLa cell line proved that this compound successfully decreased the expression level of CD73 and thus inhibiting the growth and proliferation of cancer cells.

Molecular events after antisense inhibition of hMSH2 in a HeLa cell line

1998 ◽  
Vol 418 (2-3) ◽  
pp. 61-71 ◽  
Author(s):  
Ying Qian ◽  
Yingnian Yu ◽  
Xingruo Cheng ◽  
Jianhong Luo ◽  
Haiyang Xie ◽  
...  
Keyword(s):  
Hela Cell ◽  
Cell Line ◽  
Antisense Inhibition ◽  
Hela Cell Line ◽  
Molecular Events
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