scholarly journals SYNTHESIS OF NEW QUINAZOLINONE-BASED CONJUGATES AND IN VITRO CYTOTOXIC EVALUATION

2021 ◽  
Vol 59 (4) ◽  
pp. 489
Author(s):  
Tran khac Vu
Keyword(s):  
Acetic Acid ◽  
Cell Lines ◽  
Cytotoxic Effect ◽  
High Yield ◽  
Step Procedure ◽  
Ic50 Value ◽  
Hydroxyanthranilic Acid

A series of new quinazolione derivatives containing a conjugate sytem 13 a-l were synthesized via a three step-procedure. The first step is the condensation of 5-hydroxyanthranilic acid (10) at 160oC for 2 h to afford the intermediate 11 in high yield. This intermediate was then reacted with n-butylamin in acetic acid at 160oC for 14 h to give 12 in 92%. Finally, the reaction of 12 with different aldehydes in acetic acid at 140oC for 14h furnished new conjugates 13a-l in 62-81%. The bioassay results showed that several compounds displayed cytotoxic effect against two cell lines including HepG-2 and SKLu-1 in which 13h exhibited the strongest cytotoxic effect against SKLu-1 with IC50 value of 5.05 µg/mL.

scholarly journals Synthesis and In vitro Cytotocxic Evaluation of New Quinazolinone Derivatives

2020 ◽  
Vol 36 (3) ◽  
Author(s):  
Tran Dang Thinh ◽  
Tran Khac Vu
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
High Yield ◽  
Ic50 Values ◽  
Hydroxyanthranilic Acid ◽  
Quinazolinone Derivatives ◽  
Bioassay Result ◽  
Mcf 7

The paper presents a simple and efficient synthesis of a series of new quinazolinone derivatives 8a-h. First, the reaction of 5-hydroxyanthranilic acid (6) with acetic anhydride at 160–180oC for 2 h gave the intermediate 7 in high yield. This intermediate was then reacted with amines in acetic acid at 180 oC for 14 h afforded new quinazolinone derivatives 8a-h in 77–92%. Synthesized compounds were structurally confirmed using spectroscopic methods: 1H, 13CNMR and mass spectrum. The bioassay result using three cancer cell lines including SKLU-1 (lung cancer), MCF-7 (breast cancer) and HepG-2 (liver cancer) showed that only compound 8h exhibited significant cytotoxic effect against cancer cell lines tested with IC50 values of 23.09, 27.75 and 30.19 µg/ mL, respectively.

(Substituted)-benzo[b]thiophene-4-carboxamide Synthesis and Antiproliferative Activity Study

2020 ◽  
Vol 17 (5) ◽  
pp. 563-573 ◽  
Author(s):  
Chandrakant Dhondiram Pawar ◽  
Dattatraya Navnath Pansare ◽  
Devanand Baburao Shinde
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Proliferative Activity ◽  
Thiophene Ring ◽  
Amide Group ◽  
Peptide Coupling ◽  
Ic50 Value ◽  
Important Building Block ◽  
Mcf 7

Background: Thiophene ring forms important building block in medicinal chemistry. Literature reveals that thiophene ring in combination with different groups shows different activity. By keeping these things in mind we have designed and synthesized a new series of amide and sulfonamide coupled thiophene. A series of novel substituted 3-sulfamoylbenzo[b]thiophene-4- carboxamide molecules containing sulfonamide and amide group were designed, synthesized and used for anti-proliferative activity study. Methods: The final compounds 16-36 were synthesized by using series of reactions comprising sulfonation, sulfonamide coupling, hydrolysis and peptide coupling. The yields of compounds 16- 36 are in the range of 90-98%. The structures of the synthesized compounds were elucidated and confirmed by 1H NMR, 13C NMR, LCMS and the purity was checked through HPLC analysis. The compounds were further tested for their in vitro anticancer activity against a series of cell lines A549, HeLa, MCF-7 and Du-145. Results: The intermediates 8-13, 15 and final compounds 16-36 were synthesized in good yields. The synthesized compounds were further tested for their anticancer activity and most of compounds showed moderate to good anticancer activity against all four cell lines. Conclusion: We have synthesized 21 compounds and were screened for anticancer activity against MCF-7, HeLa, A-549 and Du-145 cancer cell lines. Most of the compounds were active for tested cell lines with IC50 value in the range of 1.81 to 9.73 μM. The compounds 18, 19, 21, 25, 30, 31 and 33 are most active in cell line data with IC50 value in the range of 1.81 to 2.52 μM.

Cytotoxic Effect of Brassica oleracea Extract on two Tumor Cell Lines in vitro

2013 ◽  
Vol 16 (1) ◽  
pp. 137-142
Author(s):  
Farooq I. Mohammed ◽  
◽  
Farah T. Abdullah ◽  
Shaimaa Y. Abdulfttah ◽  
◽  
...  
Keyword(s):  
Tumor Cell ◽  
Brassica Oleracea ◽  
Cell Lines ◽  
Cytotoxic Effect ◽  
Tumor Cell Lines

scholarly journals In vitro cytotoxic study for partially purified resveratrol extracted from grape skin fruit Vitis vinifera

2009 ◽  
Vol 3 (2) ◽  
pp. 40-47
Author(s):  
Zainab Y. Mohammed ◽  
Essam F. Al-Jumaily ◽  
Nahi Y. Yaseen
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Cytotoxic Effect ◽  
Inhibitory Effect ◽  
Mammary Adenocarcinoma ◽  
Dependent Manner ◽  
Grape Skin ◽  
Grape Fruit ◽  
Glass Column

The partial purified resveratrol was obtained from the skin of black grape fruit cultivated in Iraq using 80% ethanolic solution, then an acid hydrolysis with 10% HCl solution for (10–30) min at 60Cº was carried out. The aglycone moiety was taken with an organic solvent (chloroform), then using an open glass column packed with silica gelG 60 as a stationary phase and a mobile phase of; benzene: methanol: actic acid (20:4:1). The study utilized an in vitro evaluation for the cytotoxic effect of the partially purified resveratrol on some cell lines including, the murine mammary adenocarcinoma (Ahmed –Mohammed –Nahi–2003 -AMN -3) cell line; the human laryngeal carcinoma (Hep -2) cell line and the Rat Embryo Fibroblast (REF) cell line at different concentrations and different exposure time of treatment. The partial purified resveratrol extract concentrations ranging (7.8–4000) µg/ml in a two fold serial dilutions were used to treat the three types of cell lines for 48 and 72 hours intervals. AMN-3 cell lines showed highest sensitivity toward the cytotoxic effect of the paritial purified resveratrol than other cell lines after 48 hours in a dose dependent manner. While Hep-2 cell line showed novel behavior, the lowest concentration of cell treatment gave the most significant (P< 0.01) inhibitory effect. Only the highest concentration gave significant inhibitory effect (P< 0.01) with the transformed Ref cell line.

Synthesis and Biological Evaluation of Novel 4-Phenylaminobenzofuro[2,3-d]pyrimidine Derivatives

2020 ◽  
Vol 42 (4) ◽  
pp. 564-564
Author(s):  
Ju liu Ju liu ◽  
Jun Li Jun Li ◽  
Jian tao Shi Jian tao Shi ◽  
Jie Li Jie Li ◽  
Xue chen Hao Xue chen Hao ◽  
...  
Keyword(s):  
Cell Lines ◽  
A549 Cells ◽  
Positive Control ◽  
Biological Evaluation ◽  
Dependent Manner ◽  
Pyrimidine Derivatives ◽  
Concentration Dependent Manner ◽  
Ic50 Value ◽  
Synthesis And Biological Evaluation

A series of novel 4-phenylaminobenzofuro[2,3-d]pyrimidine derivatives had been prepared and assessed for their in vitro antiproliferative activities against three lung cancer cell lines (A549, H460 and H1975). The bioassay results showed most of the designed compounds exhibited potential antiproliferation activities. Among them, compound 8f exhibited remarkable inhibitory activity against A549 and H460 cell lines with IC50 value of 2.54 μM and 2.68 μM, respectively, which was comparable to that of the positive control sorafenib (IC50 = 2.69 μM for A549 and 3.71 μM for H460). AO/EB staining suggests that compound 8f could induce apoptosis in A549 cells. Furthermore, cell cycle analyses show that compound 8f increased G0/G1 A549 cells arrest in a concentration-dependent manner. The preliminary structure-activity relationships (SARs) studies indicated that mono-electron-withdrawing groups (mono-EWGs) on the phenyl ring are positive on the antitumor activity.

scholarly journals Cytotoxic Effect of Trabectedin In Human Adrenocortical Carcinoma Cell Lines and Primary Cells

Cancers ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 928 ◽  
Author(s):  
Andrea Abate ◽  
Elisa Rossini ◽  
Sara Anna Bonini ◽  
Martina Fragni ◽  
Deborah Cosentini ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cell Cultures ◽  
Adrenocortical Carcinoma ◽  
Cytotoxic Effect ◽  
Alkylating Agents ◽  
Primary Cell ◽  
Primary Cell Cultures ◽  
High Cytotoxicity

Mitotane is the only drug approved for the treatment of adrenocortical carcinoma (ACC). The regimen to be added to mitotane is a chemotherapy including etoposide, doxorubicin, and cisplatin. This pharmacological approach, however, has a limited efficacy and significant toxicity. Evidence indicates that ACC seems to be sensitive to alkylating agents. Trabectedin is an anti-tumor drug that acts as an alkylating agent with a complex mechanism of action. Here, we investigated whether trabectedin could exert a cytotoxic activity in in vitro cell models of ACC. Cell viability was evaluated by MTT assay on ACC cell lines and primary cell cultures. The gene expression was evaluated by q-RT-PCR, while protein expression and localization were studied by Western blot and immunocytochemistry. Combination experiments were performed to evaluate their interaction on ACC cell line viability. Trabectedin demonstrated high cytotoxicity at sub-nanomolar concentrations in ACC cell lines and patient-derived primary cell cultures. The drug was able to reduce /β catenin nuclear localization, although it is unclear whether this effect is involved in the observed cytotoxicity. Trabectedin/mitotane combination exerted a synergic cytotoxic effect in NCI-H295R cells. Trabectedin has antineoplastic activity in ACC cells. The synergistic cytotoxic activity of trabectedin with mitotane provides the rationale for testing this combination in a clinical study.

scholarly journals In VitroCytotoxic Potential of Essential Oils ofEucalyptus benthamiiand Its Related Terpenes on Tumor Cell Lines

2012 ◽  
Vol 2012 ◽  
pp. 1-8 ◽  
Author(s):  
Patrícia Mathias Döll-Boscardin ◽  
Adilson Sartoratto ◽  
Beatriz Helena Lameiro de Noronha Sales Maia ◽  
Josiane Padilha de Paula ◽  
Tomoe Nakashima ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Essential Oils ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cytotoxic Effect ◽  
Herbal Remedy ◽  
Jurkat Cells ◽  
Tumor Cell Lines ◽  
Hela Cell Lines

EucalyptusL. is traditionally used for many medicinal purposes. In particular, someEucalyptusspecies have currently shown cytotoxic properties. Local Brazilian communities have used leaves ofE. benthamiias a herbal remedy for various diseases, including cancer. Considering the lack of available data for supporting this cytotoxic effect, the goal of this paper was to study thein vitrocytotoxic potential of the essential oils from young and adult leaves ofE. benthamiiand some related terpenes (α-pinene, terpinen-4-ol, andγ-terpinene) on Jurkat, J774A.1 and HeLa cells lines. Regarding the cytotoxic activity based on MTT assay, the essential oils showed improved results thanα-pinene andγ-terpinene, particularly for Jurkat and HeLa cell lines. Terpinen-4-ol revealed a cytotoxic effect against Jurkat cells similar to that observed for volatile oils. The results of LDH activity indicated that cytotoxic activity of samples against Jurkat cells probably involved cell death by apoptosis. The decrease of cell DNA content was demonstrated due to inhibition of Jurkat cells proliferation by samples as a result of cytotoxicity. In general, the essential oils from young and adult leaves ofE. benthamiipresented cytotoxicity against the investigated tumor cell lines which confirms their antitumor potential.

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