scholarly journals Evaluation of New Naphthalimides as Potential Anticancer Agents against Breast Cancer MCF-7, Pancreatic Cancer BxPC-3 and Colon Cancer HCT- 15 Cell Lines

2015 ◽  
Vol 04 (03) ◽  
Author(s):  
Noro J ◽  
Maciel J
Keyword(s):  
Breast Cancer ◽  
Pancreatic Cancer ◽  
Colon Cancer ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Mcf 7

The In Vitro Anticancer Activity and Potential Mechanism of Action of 1-[(1R,2S)-2-fluorocyclopropyl]Ciprofloxacin-(4-methyl/phenyl/benzyl-3- aryl)-1,2,4-triazole-5(4H)-thione Hybrids

2020 ◽  
Vol 20 (16) ◽  
pp. 1493-1498
Author(s):  
Ya-Zhou Zhang ◽  
Hai-Lin Liu ◽  
Qian-Song He ◽  
Zhi Xu
Keyword(s):  
Breast Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Topoisomerase Ii ◽  
Cancer Cell Lines ◽  
Breast Cancer Cell Lines ◽  
Drug Resistant ◽  
Mcf 7

Aims: Development of 1-[(1R, 2S)-2-fluorocyclopropyl]ciprofloxacin-1,2,4-triazole-5(4H)- thione hybrids as potential dual-acting mechanism anticancer agent to overcome the drug resistance. Background: Chemotherapy is an essential tool for the treatment of lung and female breast cancers, and numerous anticancer agents have been launched for this purpose. However, the clinical outcomes of chemotherapy are usually far from satisfactory due to the side effects and resistance to chemotherapeutic drugs. Thus, it is urgent to develop novel anti-lung and anti-breast cancer agents. Background: Chemotherapy is an essential tool for the treatment of lung and female breast cancers, and numerous anticancer agents have been launched for this purpose. However, the clinical outcomes of chemotherapy are usually far from satisfactory due to the side effects and resistance to chemotherapeutic drugs. Thus, it is urgent to develop novel anti-lung and anti-breast cancer agents. Objective: The primary objective of this study was to evaluate the potential of bis-isatin scaffolds with alkyl/ether linkers between the two isatin moieties against different human breast cancer cell lines including A549, MCF-7 and their drug-resistant counterparts A549/CDDP, MCF-7/ADM cells. Methods: The 1-[(1R, 2S)-2-fluorocyclopropyl]ciprofloxacin-(4-methyl/phenyl/benzyl-3-aryl)-1,2,4- triazole-5(4H)-thione hybrids were screened for their in vitro activity against drug-sensitive lung (A549), breast (MCF-7) and their drug-resistant counterparts A549/CDDP (cisplatin-resistant), MCF- 7/ADM (doxorubicin-resistant) cancer cell lines by MTT assay. The inhibitory activity of these hybrids against topoisomerase II and EGFR was also evaluated to investigate the potential mechanism of action of these hybrids. Result: The most prominent hybrid 7k (IC50: 37.28-49.05 µM) was comparable to Vorinostat against A549 and A549/CDDP lung cancer cells, and was 2.79-2.94 times more active than Vorinostat against MCF-7 and MCF-7/ADM breast cancer cell lines. Moreover, hybrid 7k (IC50: 8.6 and 16.4 µM) also demonstrated dual inhibition against topoisomerase II and EGFR. Conclusion: The 1-[(1R, 2S)-2-fluorocyclopropyl]ciprofloxacin-1,2,4-triazole-5(4H)-thione hybrids possess equally activity against both drug-sensitive cancer cells and their drug-resistant counterparts, and the majority of them were no inferior to the reference Vorinostat. The mechanistic study revealed that these hybrids could inhibit both topoisomerase II and EGFR, so these hybrids can be developed as dual-acting mechanism anticancer agents.

scholarly journals Anti-Proliferation Effects of Benzimidazole Derivatives on HCT-116 Colon Cancer and MCF-7 Breast Cancer Cell Lines

2012 ◽  
Vol 13 (8) ◽  
pp. 4075-4079 ◽  
Author(s):  
Mohammed Hadi Al-Douh ◽  
Hayder B. Sahib ◽  
Hasnah Osman ◽  
Shafida Abd Hamid ◽  
Salizawati M. Salhimi
Keyword(s):  
Breast Cancer ◽  
Colon Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Cancer Cell Lines ◽  
Breast Cancer Cell Lines ◽  
Benzimidazole Derivatives ◽  
Hct 116 ◽  
Mcf 7

Cytotoxicity , docking study of new fluorinated fused pyrimidine scaffold: Thermal and microwave irradiation synthesis

2019 ◽  
Vol 16 ◽  
Author(s):  
Alaa M. Abo Alnaja ◽  
Thoraya. A. Farghaly ◽  
Heba S. A. El-zahabi ◽  
Mohamed R. Shaaban
Keyword(s):  
Breast Cancer ◽  
Colon Cancer ◽  
Microwave Irradiation ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Hepatic Cancer ◽  
Hct 116 ◽  
Mcf 7

Background: Azolopyrimidines are imposed on the arena of drugs treated for cancer. The urgent need to discover new selective anticancer agents, paved the way to explore the antitumor significance of such fused systems. From synthetic point of view, Microwave- facilitated technique for synthesis is very strongly associated with green method in chemistry field. Aim: Our aim is to synthesis of bioactive compounds and using docking simulation run by MOE program to explore the binding mode of the most active enzyme inhibitor among the target compounds. Method: In addition to the use of conventional heating, the MARS system of CEM utilized for Microwave irradiation that is equipped with a multi-mode platform with a magnetic stirring plate and a rotor that allows the parallel processing of many vessels per batch. All the synthesized compounds were tested for their anticancer activity against hepatic cancer (HePG-2), breast cancer (MCF-7) and colon cancer (HCT-116). Screening against the cancer cell lines was performed, using doxorubicin as a reference drug. Docking studies were conducted using MOE software. Result: A novel series of fluorinated fused-pyrimidine namely, pyrazolopyrimidine, triazolopyrimidine and pyrimidobenzimidazole were designed and synthesized conventionally and under microwave irradiations The mechanistic pathways as well as the structure of all products were debated and demonstrated based on all possible spectral data. In-vitro examination of the novel prepared derivatives versus the three different human cancer cell lines [hepatic cancer (HePG-2), breast cancer (MCF-7) and colon cancer (HCT-116)] was evaluated to estimate their actual activity. Conclusion: We have developed a simple, facile, and efficient procedure for the formation of new series of azolopyrimidines. All spectra of all products were investigated deliberately to confirm their structures. The anti-cancer activity has been examined against three cancer cell lines e.g. HepG-2, MCF-7 and HCT116. Molecular modeling study was carried out in order to rationalize the in vitro anti-tumor results.

scholarly journals Synthesis, X-Ray Crystal Structures, and Preliminary Antiproliferative Activities of New s-Triazine-hydroxybenzylidene Hydrazone Derivatives

2019 ◽  
Vol 2019 ◽  
pp. 1-10 ◽  
Author(s):  
Assem Barakat ◽  
Fardous F. El-Senduny ◽  
Zainab Almarhoon ◽  
Hessa H. Al-Rasheed ◽  
Farid A. Badria ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Hydroxyl Group ◽  
X Ray ◽  
Synthetic Strategy ◽  
Weak Activity ◽  
Hct 116 ◽  
Antiproliferative Activities ◽  
Mcf 7

We herein report a new small library of Schiff-base compounds that encompasses s-triazine and (2 or 4)-hydroxylbenzylidene derivatives. These compounds were synthesized through a hydrazone linkage connecting both the s-triazine and hydroxybenzylidene derivatives. The synthetic strategy adopted allowed the synthesis of the target compounds with excellent yields and purities as observed from their NMR (1H and 13C) and elemental analysis. Furthermore, 4f, 5b, and 5f were further confirmed by X-ray single crystal diffraction technique. The preliminary antiproliferative activities for the synthesized compounds were tested against two different cancer cell lines including breast cancer (MCF-7) and colon cancer (HCT-116). From the eighteen compounds, which have been examined, only two derivatives having piperidine moiety showed more selectivity against the two cell lines MCF-7 and HCT-116, while the others showed very weak activity. The position of the hydroxyl group in the benzylidine ring and the substituent on the s-triazine moiety has great effect on the activity of the prepared compounds. The IC50 values for the two derivatives 4a and 5a evaluated against breast cancer cells, very close to those for the chemotherapeutic drug cisplatin, are 27 µM (13.3 µg/mL), 17 µM (8.4 µg/mL), and 20 µM (6 µg/mL) for 4a, 5a, and cisplatin, respectively. These results propose the preliminary antiproliferative activity of these two derivatives may deserve further consideration for development of new derivatives as potent anticancer agents.

scholarly journals Novel dermacozine-1-carboxamides as promising anticancer agents with tubulin polymerization inhibitory activity

RSC Advances ◽  
2019 ◽  
Vol 9 (32) ◽  
pp. 18670-18677 ◽  
Author(s):  
Venkata Rao Ghanta ◽  
Nagaraju Madala ◽  
Aparna Pasula ◽  
Sai Kiran S. S. Pindiprolu ◽  
Kumara Swamy Battula ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Prostate Cancer ◽  
Lung Cancer ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Inhibitory Activity ◽  
Tubulin Polymerization ◽  
Mcf 7

In the present study, novel dermacozine-1-carboxamides (8a–8n) were synthesized and screened for their in vitro cytotoxic activity against three different cancer cell lines: MCF-7 (breast cancer), A-549 (lung cancer) and DU145 (prostate cancer).

scholarly journals Evaluation of the effects of pigments produced by environmental bacteria on cancer cells

2021 ◽  
Author(s):  
Aliakbar Rezaei ◽  
Nazanin Hashemi bani ◽  
Elham moazamian
Keyword(s):  
Colon Cancer ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Complementary Therapy ◽  
Accurate Identification ◽  
Cytotoxic Effects ◽  
Arthrobacter Agilis ◽  
Colony Color ◽  
Mcf 7 ◽  
Bacterial Pigments

Abstract Cancers are a collection of incapacitating diseases in which cells initiate to divide and spread to adjacent tissues in an uncontrolled manner. Many researches demonstrated the potential of bacterial pigments as promising anticancer agents Therefore, in this study, the cytotoxic effects of bacterial pigments were evaluated in breast and colon cancer cell lines. In this study, a total of 90 samples were collected from air, water, and soil from 28 different geographical areas of Iran. Forty isolates were selected based on differences in colony color and geographic regions. The MTT assay was used to evaluate the effect of pigment on MCF-7 and SW-48 cells. Bacteria whose pigment had the highest cytotoxic effect on cell lines were selected. Accurate identification was performed using PCR, and their relative purity was measured using TLC. Bacteria isolated from any three ecosystems are capable of producing pigments. Pigment-producing bacteria are more abundant in the soil than air and water. Among pigment-producing bacteria, 3 isolates had the highest cytotoxicity on MCF-7 cells, and 3 isolates had the greatest effect on SW-48 cells. The results of sequencing of isolates at the BLAST site showed that 6 isolates with cytotoxic effects were identified (Micrococcus xinjiangensis, Dietzia, Arthrobacter agilis, Exigubacterium mexicanum, Bacillus beijingensis). Chromatography shows that these pigmented bacteria have different pigment components.Pigment extraction from bacteria can be used as a complementary therapy or other therapies for breast and colon cancer in the future.

scholarly journals Synthesis and Anticancer Activity ofN-Aryl-5-substituted-1,3,4-oxadiazol-2-amine Analogues

2014 ◽  
Vol 2014 ◽  
pp. 1-9 ◽  
Author(s):  
Mohamed Jawed Ahsan ◽  
Jyotika Sharma ◽  
Monika Singh ◽  
Surender Singh Jadav ◽  
Sabina Yasmin
Keyword(s):  
Breast Cancer ◽  
Colon Cancer ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Melanoma Cell Line ◽  
Maximum Activity ◽  
Colon Cancer Cell ◽  
Breast Cancers ◽  
Colon Cancer Cell Lines

In continuance of our search for anticancer agents, we report herein the synthesis and anticancer activity of some novel oxadiazole analogues. The compounds were screened for anticancer activity as per National Cancer Institute (NCI US) protocol on leukemia, melanoma, lung, colon, CNS, ovarian, renal, prostate, and breast cancers cell lines.N-(2,4-Dimethylphenyl)-5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-amine (4s) showed maximum activity with mean growth percent (GP) of 62.61 and was found to be the most sensitive on MDA-MB-435 (melanoma), K-562 (leukemia), T-47D (breast cancer), and HCT-15 (colon cancer) cell lines with GP of 15.43, 18.22, 34.27, and 39.77, respectively. Maximum GP was observed on MDA-MB-435 (melanoma) cell line (GP=6.82) by compoundN-(2,4-dimethylphenyl)-5-(4-hydroxyphenyl)-1,3,4-oxadiazol-2-amine (4u).

Synthesis of the first 2-hydroxyanthraquinone substituted cyclotriphosphazenes and their cytotoxic properties

2020 ◽  
Vol 44 (39) ◽  
pp. 16733-16740
Author(s):  
Gönül Yenilmez Çiftçi ◽  
Nagihan Bayık ◽  
Esra Tanrıverdi Eçik ◽  
Elif Şenkuytu ◽  
Maşuk Akşahin ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Colon Cancer ◽  
Cell Lines ◽  
Normal Breast ◽  
Normal Colon ◽  
Breast Epithelium ◽  
Normal Breast Epithelium ◽  
Cytotoxic Effects ◽  
Epithelium Cell ◽  
Mcf 7

New 2-hydroxyanthraquinone based cyclotriphosphazenes were prepared and their cytotoxic effects were investigated in MCF-7 (breast cancer), MCF-12A (normal breast epithelium), DLD-1 (colon cancer), and CD-18Co (normal colon epithelium) cell lines.

Cytotoxic activity and anti-cancer potential of Ontario grown onion extracts against breast cancer cell lines

2018 ◽  
Vol 8 (3) ◽  
pp. 159 ◽  
Author(s):  
Meghan Fragis ◽  
Abdulmonem I. Murayyan ◽  
Suresh Neethirajan
Keyword(s):  
Breast Cancer ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Cancer Cell Lines ◽  
Breast Cancer Cell Lines ◽  
Cytotoxic Activities ◽  
Cancer Line ◽  
Mcf 7

Background: Breast cancer is the most commonly diagnosed cancer and the second leading cause of cancer deaths among Canadian women. Cancer management through changes in lifestyle, such as increased intake of foods rich in dietary flavonoids, have been shown to decrease the risk associated with breast, liver, colorectal, and upper-digestive cancers in epidemiologic studies. Onions are high in flavonoid content and one of the most common vegetables. Additionally, onions are used in most Canadian cuisines.Methods: We investigated the effect of five prominent Ontario grown onion (Stanley, Ruby Ring, LaSalle, Fortress, and Safrane) extracts on two subtypes of breast cancer cell lines: a triple negative breast cancer line MDA-MB-231 and an ER+ breast cancer line MCF-7.Results: These onion extracts elicited strong anti-proliferative, anti-migratory, and cytotoxic activities on both the cancer cell lines. Flavonoids present in these onion extracts induced apoptosis, cell cycle arrest in the G2/M phase, and a reduction in mitochondrial membrane potential at dose-dependent concentrations. Onion extracts were more effective against MDA-MB-231 compared to the MCF-7 cell line. Conclusion: In this study, we investigated the extracts synthesized from Ontario-grown onion varieties in inducing anti-migratory, cytostatic, and cytotoxic activities in two sub-types of human breast cancer cell lines. Anti-tumor activity of these extracts depends upon the varietal and can be formulated into nutraceuticals and functional foods for the wellbeing of cancer patients. Overall, the results suggest that onion extracts are a good source of flavonoids with anti-cancerous properties.Keywords: onion extracts; flavonoids; anti-proliferative; breast cancer; cytotoxic activity

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