scholarly journals Palladium Complexes Based on 2-Hydrazinopyridine Ligand: Synthesis, Spectroscopic Studies, DFT Calculations, and Cytotoxicity

2021 ◽  
Vol 11 (6) ◽  
pp. 14316-14335
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Thermal Studies ◽  
Spectroscopic Studies ◽  
Palladium Complexes ◽  
Geometric Optimization ◽  
Planar Geometry ◽  
Cytotoxic Activities ◽  
Ic50 Values

Three new palladium complexes based on 2-hydrazinopyridine (hzpy) ligand, coupled with oxalate (ox), malonate (ma) and pyrophosphate (pyph) ligands, were prepared; [Pd(hzpy)(ox)], [Pd(hzpy)(ma)] and [Pd(hzpy)(pyph)]. The spectroscopic and thermal studies of the complexes suggested that the complexes were of square planar geometry. The complexes were thermally stable with an overall activation energy of 678, 981, and 633 kJ mol–1 for [Pd(hzpy)(ox)]. [Pd(hzpy)(ma)] and [Pd(hzpy)(pyph)], respectively. Geometric optimization of the three complexes was performed at DFT/B3LYP/SDD level through Gaussian 09. TDDFT and frequency calculations were studied to investigate the electronic and vibrational transitions. The potential in vitro cytotoxic activities of the three complexes was studied. The complexes exhibited a moderate cytotoxic effect against four cancer cell lines; MCF-7 (human breast cancer cell line), HepG-2 (human Hepatocellular carcinoma), PC-3 cells (human prostate carcinoma), and HEP-2 (Larynx carcinoma). The IC50 values of the three complexes exhibited a good performance against PC-3 cell line with low IC50 values reached 2.87 μg/ml for [Pd(hzpy)(ox)] compared to the IC50 of Vinblastine sulfate (42.4 μg/ml).

New Platinum (II) Ternary Complexes of Formamidine and Pyrophosphate: Synthesis, Characterization and DFT Calculations and In vitro Cytotoxicity

2020 ◽  
Vol 23 (7) ◽  
pp. 611-623
Author(s):  
Ahmed A. Soliman ◽  
Fawzy A. Attaby ◽  
Othman I. Alajrawy ◽  
Azza A.A. Abou-hussein ◽  
Wolfgang Linert
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Theoretical Calculations ◽  
Thermal Analyses ◽  
Cancer Cell Line ◽  
Cellular Growth ◽  
Planar Geometry ◽  
Square Planar ◽  
Vis Spectroscopy

Aim and Objective: Platinum (II) and platinum (IV) of pyrophosphate complexes have been prepared and characterized to discover their potential as antitumor drugs. This study was conducted to prepare and characterize new ternary platinum (II) complexes with formamidine and pyrophosphate as an antitumor candidate. Materials and Methods: The complexes have been characterized by mass, infrared, UV-Vis. spectroscopy, elemental analysis, magnetic susceptibility, thermal analyses, and theoretical calculations. They have been tested for their cytotoxicity, which was carried out using the fastcolorimetric assay for cellular growth and survival against MCF-7 (breast cancer cell line), HCT- 116 (colon carcinoma cell line), and HepG-2 (hepatocellular cancer cell line). Results: All complexes are diamagnetic, and the electronic spectral data displayed the bands due to square planar Pt(II) complexes. The optimized complexes structures (1-4) indicated a distorted square planar geometry where O-Pt-O and N-Pt-N bond angles were 82.04°-96.44°, respectively. Conclusion: The complexes showed noticeable cytotoxicity and are considered as promising antitumor candidates for further applications.

IN-SILICO AND IN VITRO ASSESSMENT OF SYNTHESIZED DIAZENYLSULFONAMIDES AS APOPTOSIS INDUCERS AND RADICAL SCAVENGERS

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (06) ◽  
pp. 49-59
Author(s):  
Priyambada Kshiroda Nandini Sarangi ◽  
Jyotirmaya Sahoo ◽  
Chita Ranjan Sahoo ◽  
Sudhir Kumar Paidesetty ◽  
Guru Prasad Mohanta
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Radical Scavenging ◽  
Cancer Cell Line ◽  
Scavenging Effect ◽  
Ic50 Values ◽  
Radical Scavenging Effect ◽  
The Individual ◽  
Mcf 7

A series of eight quinoline-thiazole hybrid-bearing diazenylsulfonamides, 4a-4h, were synthesized and characterized by UV-Vis, FT/IR, 1H NMR and lC-MS. These compounds were formed when two prepared intermediate precursors of Schiff-base compounds, (E)-N-((2-chloroquinolin-3-yl)methylene)-4phenylthiazol-2-amine (3a) and (E)-N-((2-chloroquinolin-3-yl)methylene)-4-chlorophenylthiazol-2-amine (3b) were converted to the corresponding diazenyl compounds 4a-4h by treating and coupling with the individual diazonium salts of sulfa-drugs. The results of in vitro cytotoxic activity of the synthesized compounds in two cancer cell lines MCF 7 (human breast cancer cell line) and K562 (myelogenousleukemia cell line) have shown the IC50 values as given: 4b against MCF 7 19.52 and against K562 20.55µM; 4d against MCF 7 15.96 and against K562 13.05µM. Moreover, the compound 4-(((Z)-(2-chloroquinolin-3yl)(4-phenylthiazol-2-ylimino)methyl)diazenyl)benzenesulfonic acid (4d) induced maximum percentage of apoptosis. Furthermore, the in vitro antioxidant activity study revealed that among all the synthesized compounds, compound 4d has an excellent radical scavenging effect. Molecular docking was additionally performed to investigate the binding affinity of H-bonding interaction of synthesized compounds with a targeted enzyme and to compare it with the anticancer drugs, dasatinib, bosutinib and dacarbazine.

scholarly journals Synthesis of New 1-Aryl-2-(3,5-dimethylpyrazol-1-yl)ethanone Oxime Ether Derivatives and Investigation of Their Cytotoxic Effects

Processes ◽  
2021 ◽  
Vol 9 (11) ◽  
pp. 2019
Author(s):  
Mehmet Abdullah Alagöz ◽  
Arzu Karakurt ◽  
Ceylan Hepokur ◽  
Emine Şalva ◽  
Tijen Önkol ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Cytotoxic Activities ◽  
Oxime Ether ◽  
Cytotoxic Effects ◽  
Healthy Cell ◽  
Cycle Arrest

In this study, 12 new 1-aryl-2-(3,5-dimethylpyrazol-1-yl)ethanone oxime ether derivatives were designed and synthesized to investigate their cytotoxic effects. The in vitro cytotoxic activities of the compounds were evaluated against cervix, colon, breast, glioma, neuroblastoma, and lung cancer cell lines, as well as a healthy cell line using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazo-lium bromide (MTT) assays with 5-fluorouracil (5-FU) as the reference compound. Compound 5f (IC50 = 5.13 µM) was found to be more effective than 5-FU (IC50 = 8.34 µM) in the C6 cancer cell line, and it had no cytotoxic effect on the L929 healthy cell line. Flow cytometry was used to investigate the mechanism of action of compound 5f on the cell cycle of the C6 cell line. The analysis showed that cell death was significantly due to apoptosis. These results indicate that compound 5f induces cell cycle arrest, and may be effective in treating glioma.

In vitro α-amylase and α-glucosidase Inhibition, Antioxidant, Anti- Inflammatory Activity and GC-MS Profiling of Avicennia alba Blume

2020 ◽  
Vol 23 (9) ◽  
pp. 945-954
Author(s):  
Swagat K. Das ◽  
Sagarika Dash ◽  
Hrudayanath Thatoi ◽  
Jayanta K. Patra
Keyword(s):  
Cell Line ◽  
Protein Denaturation ◽  
Cytotoxic Activities ◽  
Mangrove Plant ◽  
Metal Chelating ◽  
Murine Cell Line ◽  
Ic50 Value ◽  
Ic50 Values ◽  
Avicennia Alba

Background: Avicennia alba Blume, is a well-known mangrove plant used in traditional medicinal practices for several human ailments. Objective: The study aimed at evaluation of antidiabetic, antioxidant, anti-inflammatory and cytotoxic activities of A. alba ethanolic leaf (AAL) and bark (AAB) extract along with phytochemical investigation. Methods: In vitro antidiabetic study was done by α-amylase, α-glucosidase enzyme inhibition assay; antioxidant study by DPPH, ABTS, superoxide, and metal chelating assays, antiinflammatory study by protein denaturation assay. The cytotoxicity study was done on TC1 murine cell line. Further, GC-MS analysis was carried out for AAL extracts. Results: AAL exhibited better antidiabetic activities with IC50 values of 1.18 and 0.87 mg/ml against α-amylase and α-glucosidase enzymes respectively. The AAL exhibited better ABTS, superoxide scavenging and metal chelating potential with IC50 values of 0.095, 0.127 and 0.444 mg/ml. However, AAB showed higher DPPH scavenging potential with IC50 value of 0.163 mg/ml. The AAL also exhibited higher protein denaturation potential with IC50 value of 0.370 mg/ml. The bark extract exhibited better cytotoxic activity as compared to leaf extracts on the TC1 murine cell line. The phytochemical study revealed higher total phenol (25.64 mg GAE/g), flavonoid (205.09 mg QE/g), and tannin content (251.17 mg GAE/g) in AAL. The GC-MS analysis revealed the presence of several compounds in AAL extract. Conclusion: The result of the present study highlights the antidiabetic, antioxidant and cytotoxic activities of mangrove plant Avicennia alba.

scholarly journals Cytotoxic activities of Methanolic and Chloroform Extract of Cryptocarya Massoy (Oken) Kosterm. Bark on MCF-7 human breast cancer cell line

2018 ◽  
Vol 9 (1) ◽  
pp. 57-62
Author(s):  
Yuli Widiyastuti ◽  
Ika Yanti M. Sholikhah ◽  
Sari Haryanti
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cancer Cell ◽  
Mtt Assay ◽  
Cancer Cell Line ◽  
Chloroform Extract ◽  
Cytotoxic Activities ◽  
Litsea Cubeba ◽  
Mcf 7

Abstrak Latar Belakang. Krangean [Litsea cubeba (Lour.) Pers.] Adalah salah satu tanaman aromatik purba di Indonesia. Tanaman ini adalah anggota keluarga Lauraceae, tumbuh liar di dataran tinggi Sumatera, Kalimantan, dan pulau Jawa. Aktivitas antikanker tanaman ini belum banyak dieksplorasi. Penelitian ini bertujuan untuk mengetahui kandungan fitokimia dan aktivitas sitotoksik ekstrak buah krangean pada sel kanker manusia secara in vitro. Metode. Kloroform dan metanol digunakan untuk mempererat bubuk buah kering selama 3x24 jam. Senyawa fitokimia utama ditandai dengan KLT (kromatografi lapis tipis). Uji MTT dilakukan untuk mengamati morfologi dan viabilitas kanker serviks HeLa, kanker payudara MCF-7, dan sel HEPG2 hepar. Hasil. Hasil penelitian menunjukkan bahwa karakterisasi KLT ekstrak kloroform dan metanol Litsea cubeba menunjukkan profil yang sama, dengan senyawa utama yang ditemukan adalah terpenoid dan alkaloid. Uji MTT menemukan bahwa kedua ekstrak memiliki penghambatan kuat pada sel HeLa. Ekstrak kloroform menunjukkan aktivitas sitotoksik yang lebih kuat dibandingkan dengan metanol, dengan nilai IC50 masing-masing 33,7 dan 64,8 μg / mL. Kesimpulan. Esktrak kloroform dan ekstrak metanol dari Litsea cubeba memiliki aktivitas yang kuat terhadap sel HeLa dan aktivitas sedang terhadap sel HEPG2 dan MCF-7.  Selanjutnya disarankan untuk dilakukan penelitian lebih lanjut untuk mengathui senyawa aktif L. cubeba (Lour.) Pers. yang memiliki aktivitas antikanker potensial. Kata kunci: Litsea cubeba (Lour.) Pers., sitotoksik, HeLa, MCF-7, HebG2, MTT assay   Abstract Background. Krangean [Litsea cubeba (Lour.) Pers.] is one of ancient aromatic plants in Indonesia. This plant is the member of Lauraceae family, growing wild on the highlands of Sumatera, Kalimantan, and Java island. The anticancer activity of this plant haven’t been explored extensively.This research aimed to investigate phytochemical content and cytotoxic activity of krangean fruits extract on human cancer cell line in vitro. Method. Chloroform and methanol were used to macerate dried fruits powder for 3x24 hours. Major phytochemical compounds was characterized by TLC (thin layer chromatography). MTT assay was done to observe morphology and viability of HeLa cervical cancer, MCF-7 breast cancer, and HepG2 hepar cancer cell line. Result. The results showed that TLC characterization of chloroform and methanolic extracts of Litsea cubeba revealed similar profile, with the major compound found are terpenoid and alkaloid. The MTT assay found that both extracts have strong inhibition on HeLa cell line. Chloroform extract exhibited stronger cytotoxic activities compared to methanol, with the IC50 values of 33,7 and 64,8 μg/mL respectively. While, the both extract have moderate cytotoxic activities to HEPG2 and MCF-7 cancer cell line indicated by IC50value more than 100 mg/mL. Conclusion. Chloroform and methanolic extract of Litsea cubeba have a strong activity againts HeLa cancer cell lines and moderate activity to HEPG2 and MCF-7, thought chloroform extract of Litsea cubeba has stronger effect on cancer cell line viability. It is well recommended for further studies to investigate the active compound of L. cubeba (Lour.) Pers. for potential anticancer activity.   Key words: Litsea cubeba (Lour.) Pers., cytotoxic, HeLa, MCF-7, HebG2, MTT assay

ANTITUMOR EFFECT OF SUNITINIB AND BORTEZOMIB ON BREAST CANCER CELL LINE IN VITRO

2017 ◽  
Vol 63 (1) ◽  
pp. 141-145
Author(s):  
Yuliya Khochenkova ◽  
Eliso Solomko ◽  
Oksana Ryabaya ◽  
Yevgeniya Stepanova ◽  
Dmitriy Khochenkov
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Antitumor Effect ◽  
Cancer Cell Lines ◽  
Breast Cancer Cell Lines ◽  
Actual Problem

The discovery for effective combinations of anticancer drugs for treatment for breast cancer is the actual problem in the experimental chemotherapy. In this paper we conducted a study of antitumor effect of the combination of sunitinib and bortezomib against MDA-MB-231 and SKBR-3 breast cancer cell lines in vitro. We found that bortezomib in non-toxic concentrations can potentiate the antitumor activity of sunitinib. MDA-MB-231 cell line has showed great sensitivity to the combination of bortezomib and sunitinib in vitro. Bortezomib and sunitinib caused reduced expression of receptor tyrosine kinases VEGFR1, VEGFR2, PDGFRa, PDGFRß and c-Kit on HER2- and HER2+ breast cancer cell lines

A Novel Triazole Derivative Drug Presenting In Vitro and In Vivo Anticancer Properties

2018 ◽  
Vol 18 (17) ◽  
pp. 1483-1493
Author(s):  
Ricardo Imbroisi Filho ◽  
Daniel T.G. Gonzaga ◽  
Thainá M. Demaria ◽  
João G.B. Leandro ◽  
Dora C.S. Costa ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Hepatic Function ◽  
Anticancer Properties ◽  
Mcf 7

Background: Cancer is a major cause of death worldwide, despite many different drugs available to treat the disease. This high mortality rate is largely due to the complexity of the disease, which results from several genetic and epigenetic changes. Therefore, researchers are constantly searching for novel drugs that can target different and multiple aspects of cancer. Experimental: After a screening, we selected one novel molecule, out of ninety-four triazole derivatives, that strongly affects the viability and proliferation of the human breast cancer cell line MCF-7, with minimal effects on non-cancer cells. The drug, named DAN94, induced a dose-dependent decrease in MCF-7 cells viability, with an IC50 of 3.2 ± 0.2 µM. Additionally, DAN94 interfered with mitochondria metabolism promoting reactive oxygen species production, triggering apoptosis and arresting the cancer cells on G1/G0 phase of cell cycle, inhibiting cell proliferation. These effects are not observed when the drug was tested in the non-cancer cell line MCF10A. Using a mouse model with xenograft tumor implants, the drug preventing tumor growth presented no toxicity for the animal and without altering biochemical markers of hepatic function. Results and Conclusion: The novel drug DAN94 is selective for cancer cells, targeting the mitochondrial metabolism, which culminates in the cancer cell death. In the end, DAN94 has been shown to be a promising drug for controlling breast cancer with minimal undesirable effects.

Synthesis, Docking Study, Cytotoxicity, Antioxidant, and Anti-microbial Activities of Novel 2,4-Disubstituted Thiazoles Based on Phenothiazine

2020 ◽  
Vol 17 (2) ◽  
pp. 151-159
Author(s):  
Tran Nguyen Minh An ◽  
Pham Thai Phuong ◽  
Nguyen Minh Quang ◽  
Nguyen Van Son ◽  
Nguyen Van Cuong ◽  
...  
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Antimicrobial Activities ◽  
Significant Activity ◽  
Thiazole Derivatives ◽  
Ligand Interaction ◽  
Ic50 Value ◽  
Mcf 7

: A series of novel 1,3-thiazole derivatives (5a-i) with a modified phenothiazine moiety were synthesized and tested against cancer cell line MCF-7 for their cytotoxicity. Most of them (5a-i) were less cytotoxic or had no activity against MCF-7 cancer cell line. Material and Methods: The IC50 value of compound (4) was 33.84 μM. The compounds (5a-i) were also evaluated for antimicrobial activities, but no significant activity was observed. The antioxidant activity was conducted for target compounds (5a-i). The IC50 value of compound (5b) was 0.151mM. Results: The total amount of energy, ACE (atomic contact energy), energy of receptor (PDB: 5G5J), and ligand interaction of structure (4) were found to be 22.448 Kcal.mol-1 , -247.68, and -91.91 Kcal.mol-1, respectively. The structure (4) is well binded with the receptor because the values of binding energy, steric energy, and the number of hydrogen bondings are -91.91, 22.448 kcal.mol-1, and 2, respectively. It shows that structure (4) has good cytotoxicity with MCF-7 in vitro. Conclusion: The increasing of docking ability of structures (5a-i) with the receptor is presented in increasing order as (5f)>(5e)>(5g)>(5a)>(5b)>(5d)>(5c)>(5i)>(5h). The structure bearing substitution as thiosemicarbazone (4), nitrogen heterocyclic (5f), halogen (5e), and azide (5g) showed good cytotoxicity activity in vitro.

Naphthoquinone-based hydrazone hybrids: synthesis and potent activity against cancer cell lines

2020 ◽  
Vol 16 ◽  
Author(s):  
Délis Galvão Guimarães ◽  
Arlan de Assis Gonsalves ◽  
Larissa Araújo Rolim ◽  
Edigênia Cavalcante Araújo ◽  
Victória Laysna dos Anjos Santos ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Biological Activities ◽  
Supporting Electrolyte ◽  
Cancer Cell Lines ◽  
Molecular Structures ◽  
Cytotoxic Activities ◽  
Electrochemical Studies ◽  
Ic50 Values

Background: Natural naphthoquinones have shown diversified biological activities including antibacterial, antifungal, antimalarial, and cytotoxic activities. However, they are also compounds with acute cytotoxicity, immunotoxicity, carcinogenesis, and cardio- and hepatotoxicity, then the modification at their redox center is an interesting strategy to overcome such harmful activity. Objective: In this study, four novel semisynthetic hydrazones, derived from the isomers α- and β-lapachones (α and β, respectively) and coupled with the drugs hydralazine (HDZ) and isoniazid (ACIL), were prepared, evaluated by electrochemical methods and assayed for anticancer activity. Method: The semisynthetic hydrazones were obtained and had their molecular structures established by NMR, IR, and MS. Anticancer activity was evaluated by cell viability determined by reduction of 3-(4,5-dimethyl-2-thiazol)-2,5-diphenyl-2H-tetrazolium bromide (MTT). The electrochemical studies, mainly cyclic voltammetry, were performed, in aprotic and protic media. Result: The study showed that the compounds 2, 3, and 4 were active against at least one of the cancer cell lines evaluated, being compounds 3 and 4 the most cytotoxic. Toward HL-60 cells, compound 3 was 20x more active than β-lapachone, and 3x more cytotoxic than doxorubicin. Furthermore, 3 showed an SI value of 39.62 for HL-60 cells. Compound 4 was active against all cancer cells tested, with IC50 values in the range 2.90–12.40 μM. Electrochemical studies revealed a profile typical of self-protonation and reductive cleavage, dependent on the supporting electrolyte. Conclusion: These results therefore indicate that compounds 3 and 4 are strong candidates as prototypes of new antineoplastic drugs.

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