Quinone-Fused Pyrazoles through 1,3-Dipolar Cycloadditions: Synthesis of Tricyclic Scaffolds and in vitro Cytotoxic Activity Evaluation on Glioblastoma Cancer Cells

ChemMedChem ◽  
2018 ◽  
Vol 13 (17) ◽  
pp. 1744-1750 ◽  
Author(s):  
Giulio Bertuzzi ◽  
Simone Crotti ◽  
Pierpaolo Calandro ◽  
Bianca Flavia Bonini ◽  
Ilaria Monaco ◽  
...  
2019 ◽  
Vol 121 ◽  
pp. 267-273 ◽  
Author(s):  
Ana Cláudia Nogueira da Silva ◽  
Renato Malveira Carreiro do Nascimento ◽  
Débora Caroline do Nascimento Rodrigues ◽  
Paulo Michel Pinheiro Ferreira ◽  
Cláudia Pessoa ◽  
...  

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4984
Author(s):  
Didi Nurhadi Illian ◽  
Ihsanul Hafiz ◽  
Okpri Meila ◽  
Ahmad Rusdan Handoyo Utomo ◽  
Arif Nuryawan ◽  
...  

In 2020, an estimated 19.3 million new cancer cases and nearly 10 million cancer deaths have occurred worldwide, with colorectal cancer ranking as the third most frequently diagnosed (10.0%). Several attempts have been conducted against cancer, including surgery, radiation, monoclonal antibodies, and chemotherapy. Many people choose natural products as alternatives against cancer. These products will not only help in human life preservation but also work as a source of up-to-date information, leading people away from incorrect information. We discuss the current status, distribution, and future implications of protecting populations with natural products as an alternative against colorectal cancer in Indonesia. Thirty-eight studies were included in this review for data extraction. The distribution of natural products in Indonesia that have potential activity against colorectal cancer cells was predominated by terpenoids, followed by phytosterols, phenolics, alkaloids, and polyisoprenoids. The type of cell line utilized in the cytotoxic activity analysis of natural products was the WiDr cell line, followed by HT-29 cells and HCT-116 cells. This review showed that MTT in vitro assay is a general method used to analyze the cytotoxic activity of a natural product against colorectal cancer cells, followed by other in vitro and in vivo methods. The systematic review provided predictions for several secondary metabolites to be utilized as an alternative treatment against colorectal cancer in Indonesia. It also might be a candidate for a future co-chemotherapy agent in safety, quality, and standardization. In addition, computational methods are being developed to predict the drug-likeness of compounds, thus, drug discovery is already on the road towards electronic research and development.


2013 ◽  
Vol 8 (1) ◽  
pp. 1934578X1300800
Author(s):  
Yu-Chang Su ◽  
Chen-Lung Ho

This study investigated the chemical composition and in-vitro cytotoxic activities of the essential oil isolated from the leaf of Beilschmiedia erythrophloia. The essential oil was isolated using hydrodistillation in a Clevenger-type apparatus, and characterized by GC-FID and GC-MS. Fifty-five compounds were identified, representing 100% of the oil. The main components identified were β-caryophyllene (22.6%), α-humulene (21.9%), terpinen-4-ol (5.3%), cis-β-ocimene (5.1%), sabinene (5.0%) and limonene (4.5%). The anticancer activities of oil were evaluated. The results showed that the oil exhibited cytotoxic activity against human oral, liver, lung, colon, melanoma, and leukemic cancer cells.


Author(s):  
Mohsen Vosooghi ◽  
Hoda Yahyavi ◽  
Kouros Divsalar ◽  
Hashem Shamsa ◽  
Asma Kheirollahi ◽  
...  

2020 ◽  
Vol 44 (47) ◽  
pp. 20574-20583
Author(s):  
Kandoth Kandy Jesna ◽  
Malaichamy Ilanchelian

In the present work, we have synthesized cetyltrimethyl ammonium bromide (CTAB) capped gold nanorods (Au NRs) to evaluate apparent binding affinities for the adsorption of trypsin (TRP).


MedChemComm ◽  
2014 ◽  
Vol 5 (1) ◽  
pp. 25-31 ◽  
Author(s):  
Peng Du ◽  
Uma M. Viswanathan ◽  
Khairan Khairan ◽  
Tomislav Buric ◽  
Nathaniel E. B. Saidu ◽  
...  

2012 ◽  
Vol 65 (12) ◽  
pp. 1625 ◽  
Author(s):  
Vasilis I. Balas ◽  
Christina N. Banti ◽  
Nikolaos Kourkoumelis ◽  
Sotiris K. Hadjikakou ◽  
George D. Geromichalos ◽  
...  

Crystals of Ph3SnCl (1) were grown from a methanol/acetonitrile solution. Compounds [Ph3SnOH]n (2) and [(Ph2Sn)4Cl2O2(OH)2] (3) were crystallized from diethyl ether/methanol/acetonitrile and hot acetone/water solutions respectively, of the white precipitation, formed by adding KOH to solutions of 1 and [Ph2SnCl2] in 1 : 1 and 1 : 2 molar ratios respectively. Complex 1 was characterized by X-ray crystallography. X-ray structure determination of compounds 2 and 3 confirmed the previously reported identities. The molecular structure of 1, reported here, is a new polymorphic form of the known one for Ph3SnCl. Four independent [Ph3SnCl] molecules constitute the crystal structure of 1. The moieties are packed in two pairs in a tail-to-tail arrangement. Complexes 1–3 were evaluated for their in vitro cytotoxic activity (cell viability) against human cancer cell lines: HeLa (human cervical), MCF-7 (breast, estrogen receptor (ER) positive), MDA-MB-231 (breast, ER negative), A549 (lung), Caki-1 (kidney carcinoma), 786-O (renal adenocarcinoma), K1 (thyroid carcinoma), and the normal human lung cell line MRC-5 (normal human fetal lung fibroblast cells) versus, the normal immortalized human mammary gland epithelial cell line MTSV17 with a sulforhodamine B (SRB) assay. The results show potent cytotoxic activity of the complexes against all cell lines used, which was superior to that of cisplatin (CDDP). Compounds 1–3 showed higher activity against breast cancer cells MCF-7 (ER positive) than against of MDA-MB-231 (ER negative). These findings prompted us to search for possible interaction of these complexes with other cellular elements of fundamental importance in cell proliferation. The influence of these complexes 1–3 upon the catalytic peroxidation of linoleic acid to hydroperoxylinoleic acid by the enzyme lipoxygenase (LOX), as well as their binding affinity towards calf thymus-DNA, were kinetically and theoretically studied.


2020 ◽  
Vol 20 (1) ◽  
Author(s):  
Sista Werdyani ◽  
Annisa Fitria ◽  
Sari Rakhmawati

Cancer remains one of the diseases with increasing number of sufferers, but research on compounds that act as anti-cancer is also ongoing. Terpenoids have been known as a compound that can inhibit the proliferation of cancer cells. One of the medical plants that produce terpenoids is Jarak cina (Jatropha multifida Linn.). Therefore, the possibility of Jarak cina (Jatropha multifida Linn.) to have an cytotoxic activity on cancer cell proliferation is reasonably high. This study was conducted to determine the cytotoxic activity of Jarak cina (Jatropha multifida Linn.) bark extracts against cancer cell MCF-7. Jarak cina bark was extracted using the multilevel soxhlet extraction method with n-hexane, ethyl acetate, and ethanol as the solvents. All the three extracts were then tested against MCF-7 cancer cells using MTT (3-(4,5-dimethylthiazol-2-yl) - 2,5-diphenyltetrazolium bromide) method. Data analysis was performed for IC50 (ppm) parameter. The results showed that the IC50 of n-hexane extract was 313.21 ppm, while the ethyl acetate extract reached 258.38 ppm of IC50, and the IC50 of ethanol extract was 418.51 ppm. The highest potential of cytotoxicity was found in the ethyl acetate extract, so further testing would be required to optimize the proliferation inhibitory activity.


Sign in / Sign up

Export Citation Format

Share Document