scholarly journals Investigating the in Vitro Antiproliferative and Apoptosis-Inducing Effects of Pyranochromene Derivatives

2020 ◽  
Vol 11 (3) ◽  
pp. 10987-10995
Keyword(s):  
Cell Lines ◽  
Biological Activities ◽  
Para Position ◽  
Lead Compounds ◽  
Three Component Reaction ◽  
Anti Cancer ◽  
Important Health ◽  
Induced Apoptosis ◽  
Mcf 7

Cancer is one of the important health problems, and researchers continue their efforts to discover new anti-cancer agents. Coumarins (chromene-2-ones), a group of natural metabolites, have shown different biological activities based on their substitutions. In this study, 15 compounds of 1,5-dihydropyrano[2,3-c]chromene were synthesized by three-component reaction and investigated for the antiproliferative activity on the breast (MCF-7), colorectal (SW48 and HT-29), lung (A549), and brain (U-87 MG) cancer cell lines as well as two normal cell lines (3T3 and HUVEC). The apoptosis/necrosis-inducing effect of the selected compounds was determined on the MCF-7 cell line by flow cytometry. The results showed that the compounds bearing a moiety on their phenyl ring's para position had potent cytotoxic effects on the tested cell lines. These compounds induced apoptosis in MCF-7 cells. The compounds were also toxic for 3T3 and HUVECs and did not display a high selectivity for tumor cells. Our results revealed that the compounds having a moiety at the para position of their phenyl ring might be suitable lead compounds for the synthesis of potent anti-cancer agents.

scholarly journals Synthesis and In Vitro Antitumor Activity of Naringenin Oxime and Oxime Ether Derivatives

2019 ◽  
Vol 20 (9) ◽  
pp. 2184 ◽  
Author(s):  
Ahmed Dhahir Latif ◽  
Tímea Gonda ◽  
Máté Vágvölgyi ◽  
Norbert Kúsz ◽  
Ágnes Kulmány ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Antioxidant Activities ◽  
Biological Activities ◽  
Gynecological Cancer ◽  
Human Leukemia ◽  
Oxime Ether ◽  
M Phase ◽  
Induced Apoptosis ◽  
Mcf 7

Naringenin is one of the most abundant dietary flavonoids exerting several beneficial biological activities. Synthetic modification of naringenin is of continuous interest. During this study our aim was to synthesize a compound library of oxime and oxime ether derivatives of naringenin, and to investigate their biological activities. Two oximes and five oxime ether derivatives were prepared; their structure has been elucidated by NMR and high-resolution mass spectroscopy. The antiproliferative activity of the prepared compounds was evaluated by MTT assay against human leukemia (HL-60) and gynecological cancer cell lines isolated from cervical (HeLa, Siha) and breast (MCF-7, MDA-MB-231) cancers. Tert-butyl oxime ether derivative exerted the most potent cell growth inhibitory activity. Moreover, cell cycle analysis suggested that this derivative caused a significant increase in the hypodiploid (subG1) phase and induced apoptosis in Hela and Siha cells, and induced cell cycle arrest at G2/M phase in MCF-7 cells. The proapoptotic potential of the selected compound was confirmed by the activation of caspase-3. Antioxidant activities of the prepared molecules were also evaluated with xanthine oxidase, DPPH and ORAC assays, and the methyl substituted oxime ether exerted the most promising activity.

scholarly journals 3′,4′-Dihydro-2′H-spiro[indoline-3,1′-isoquinolin]-2-ones as potential anti-cancer agents: synthesis and preliminary screening

2020 ◽  
Vol 7 (1) ◽  
pp. 191316 ◽  
Author(s):  
Maloba M. M. Lobe ◽  
Simon M. N. Efange
Keyword(s):  
Cell Proliferation ◽  
Cell Lines ◽  
Biological Activities ◽  
Cell Cancer ◽  
Breast Cancer Cell Lines ◽  
Small Cell Lung ◽  
Preliminary Screening ◽  
Anti Cancer ◽  
Molecular Hybrids

Both tetrahydroisoquinolines (THIQs) and oxindoles (OXs) display a broad range of biological activities including anti-cancer activity, and are therefore recognized as two privileged scaffolds in drug discovery. In the present study, 24 3′,4′-dihydro-2′H-spiro[indoline-3,1′-isoquinolin]-2-ones, designed as molecular hybrids of THIQ and OX, were synthesized and screened in vitro against 59 cell lines in the NCI-60 screen. Twenty compounds displayed weak to moderate inhibition of cell proliferation; among them, three compounds displayed at least 50% inhibition of cell proliferation. The compounds appeared to target primarily renal cell cancer lines; however, leukaemia, melanoma, non-small cell lung cancer, prostate, ovarian and even breast cancer cell lines were also affected. Therefore, this class of spirooxindoles may provide useful leads in the search for new anti-cancer agents.

Do herbal drinks augment the cytotoxic effect against different cancer cells? Are they potent stimulators of innate and acquired immunity?

2020 ◽  
Vol 38 (15_suppl) ◽  
pp. e21657-e21657 ◽  
Author(s):  
Israa Adnan ◽  
Wamidh Talib
Keyword(s):  
Middle East ◽  
Cell Lines ◽  
Biological Activities ◽  
Neutral Red ◽  
Acquired Immunity ◽  
Anticancer Activities ◽  
Anti Cancer ◽  
Wild Thyme ◽  
Phagocytosis Activity ◽  
Mcf 7

e21657 Background: The herbal drinks are highly prevalent in the Middle East and are consumed in large quantities as daily drinks. Few studies have evaluated the biological activities of the herbal drinks produced from some plants.The current study aims to evaluate the anticancer and immunomodulatory activities of five herbal drinks consumed in the Middle East. These drinks are Palestinian Zhourat, Lebanese Zhourat, Lemon and Ginger combination, Wild Thyme, and Marjoram. Methods: The selected herbal drinks as concentrated water extracts were tested separately for: A. Anti-cancer effect on the cell lines (MCF-7, MDA-MB231, HCT-116, A549, and Vero-normal cells) by assessing: - Antiproliferation activities using MTT assay. Apoptosis (using the caspase-3 assay) and vascular endothelial growth factor (VEGF) expression (using ELISA kit) for the most potent antiproliferative extract. B. Immunomodulatory effect by evaluating: - Splenocytes proliferation using the mitogen proliferation assay. Phagocytosis activity using the nitro blue tetrazolium assay. - Pinocytosis function using the neutral red method. Results: The Lemon and Ginger combination was the most potent against MDA-MB231, MCF-7 and A549l cell lines with IC50 3.5,4, 6.5mg/ml, respectively. Lemon and Ginger combination and Wild thyme separately showed high apoptosis induction and angiogenesis suppression on the MDA-MB231cell line at concentrations 3.5 and 4.4 mg/ml for both extracts, respectively. Wild thyme was the most potent stimulant lymphocyte proliferation (with index 4.7), and Marjoram has the highest percentage (314.4%) in phagocytosis activity, while moderate stimulation by Zhourat was noted. Lemon and Ginger combination, Wild thyme, Marjoram, and the Lebanese herbal drink "Zhourat" were the most active extracts in stimulating pinocytosis with absorbance value 0.5745,0.4645,0.461,0.4575 nm, respectively. Meanwhile, the Palestinian herbal drink "Zhourat" had a moderate effect. Conclusions: The consumption ofthe mentioned herbal drinks has various Anti-cancer and immunomodulatory effects. Lemon and ginger combination exhibits the most potent anticancer activities. Wild thyme and marjoram are potent stimulators of innate and acquired immunity. The result achieved in this study is very optimistic and encouraging to be considered for further clinical trials.

scholarly journals Synthesis of Chromene 4 Aldehyde and 6-Phenyl-6h-Chromeno [4,3-B] Quinoline Derivatives as Anticancer and Apoptosis Inducing Agents

2021 ◽  
Vol 9 (10) ◽  
pp. 1764-1772
Author(s):  
Rizuana Sultana
Keyword(s):  
Cell Lines ◽  
Morphological Changes ◽  
Quinoline Derivatives ◽  
Significant Extent ◽  
Diverse Range ◽  
Synthetic Strategy ◽  
Induced Apoptosis ◽  
Apoptosis Inducing Agents ◽  
Mcf 7

Abstract: A series of novel chromene 3-aldehyde and quinoline derivatives have been synthesized using diversely substituted nitroarenes in the presence of In, dil. HCl, H2O (reductive amination) and evaluated for in vitro cytotoxic activity in three different cancer cell lines (MDA-MB-453, MCF-7, A549 and PC3). The synthetic strategy utilized to access these hybrids is operationally simple and works with great substrate scope. Interestingly, compound 6i was induced apoptosis to a significant extent in MDA-MB-453 cell lines. And these selected compounds 6i was led to morphological changes after treatment with MDA-MB-453 cell lines and found clear destabilization of mitochondrial membrane potential behind the observed anticancer activity. This strategy is operationally simple and works with a diverse range of substrates and warrants future investigations for further anticancer drug development.

scholarly journals In vitro anticancer activity of microbial isolates from diverse habitats

2011 ◽  
Vol 47 (2) ◽  
pp. 279-287 ◽  
Author(s):  
Angel Treasa Thomas ◽  
Josyula Venkata Rao ◽  
Volety Mallikarjuna Subrahmanyam ◽  
Hariharapura Raghu Chandrashekhar ◽  
Naseer Maliyakkal ◽  
...  
Keyword(s):  
Cell Lines ◽  
Biological Activities ◽  
Bioactive Molecules ◽  
Nuclear Staining ◽  
Cytotoxic Potential ◽  
Biochemical Tests ◽  
Morphological Studies ◽  
Aspergillus Sp ◽  
Mcf 7

Extracts from natural products, especially microorganisms, have served as a valuable source of diverse molecules in many drug discovery efforts and led to the discovery of several important drugs. Identification of microbial strains having promising biological activities and purifying the bio-molecules responsible for the activities, have led to the discovery of many bioactive molecules. Extracellular, as well as intracellular, extracts of the metabolites of thirty-six bacterial and twenty-four fungal isolates, grown under unusual conditions such as high temperature, high salt and low sugar concentrations, were in vitro tested for their cytotoxic potential on various cancer cell lines. The extracts were screened on HeLa and MCF-7 cell lines to study the cytotoxic potential. Nuclear staining and flow cytometric studies were carried out to assess the potential of the extracts in arresting the cell cycle. The crude ethylacetate extract of isolate F-21 showed promising results by MTT assay with IC50 as low as 20.37±0.36 µg/mL on HeLa, and 44.75±0.81 µg/mL on MCF-7 cells, comparable with Cisplatin. The isolate F-21 was identified as Aspergillus sp. Promising results were also obtained with B-2C and B-4E strains. Morphological studies, biochemical tests and preliminary chemical investigation of the extracts were also carried out.

scholarly journals Synthesis, Characterization and Anti-Cancer Studies of Curcumin Diketimines-Heteropolyacid Composites

2020 ◽  
Vol 32 (7) ◽  
pp. 1534-1542
Author(s):  
BHARATH SAMANNAN ◽  
JOTHI SELVAM ◽  
JEYABALAN THAVASIKANI
Keyword(s):  
13C Nmr ◽  
Hybrid Composites ◽  
Biological Activities ◽  
Spectral Studies ◽  
Keggin Anion ◽  
Round Shape ◽  
Anti Cancer ◽  
Cancer Studies ◽  
Mcf 7

A novel composite of curcumin diketimine (CDK)-heteropolyacid (where HPA = vanadium doped Keggin anion and CDK = curcuminbenzoguanamine) had been synthesized. The hybrid composites were investigated by analytical methods such as elemental analysis, FTIR, 13C NMR, SEM, EDS, XRD, DSC-TGA, ESR spectral studies and biological activities. Encapsulated hybrid composite also studied (in vitro) against MCF-7 cancer cell lines. ESR results showed that the presence of (V4+) ion nitrogen ligation in the composite. 13C NMR of CDK ligand value of 183.37 and 55.06 ppm corresponds to (2=N) and (O-CH3) may be due to the composites. The morphology of molybdovanadate (HPA) showed a structure of self-assembled round shape of a diameter around 1 μm.

scholarly journals Synthesis of novel thiourea-/urea-benzimidazole derivatives as anticancer agents

2021 ◽  
Vol 19 (1) ◽  
pp. 1062-1073
Author(s):  
Lamia A. Siddig ◽  
Mohammad A. Khasawneh ◽  
Abdelouahid Samadi ◽  
Haythem Saadeh ◽  
Nael Abutaha ◽  
...  
Keyword(s):  
Cell Lines ◽  
Anticancer Agents ◽  
Caspase 3 ◽  
Benzimidazole Derivatives ◽  
Spectroscopic Techniques ◽  
Thiourea Derivatives ◽  
Ethidium Bromide Staining ◽  
Induced Apoptosis ◽  
Mcf 7

Abstract A new series of urea and thiourea derivatives containing benzimidazole group as potential anticancer agents have been designed and synthesized. The structures of the synthesized compounds were characterized and confirmed by spectroscopic techniques such as 1H NMR, 13C NMR, and mass spectrometry. In vitro anticancer assay against two breast cancer (BC) cell lines, MDA-MB-231ER(−)/PR(−) and MCF-7ER(+)/PR(+), revealed that the cytotoxicity of 1-(2-(1H-benzo[d]imidazol-2-ylamino)ethyl)-3-p-tolylthiourea (7b) and 4-(1H-benzo[d]imidazol-2-yl)-N-(3-chlorophenyl)piperazine-1-carboxamide (5d) were higher in MCF-7 with IC50 values of 25.8 and 48.3 µM, respectively, as compared with MDA-MB-231 cells. Furthermore, 7b and 5d were assessed for their apoptotic potential using 4′,6-diamidino-2-phenylindole, acridine orange/ethidium bromide staining, and Caspase-3/7. After incubation with MCF-7, the compounds 7b and 5d induced apoptosis through caspase-3/7 activation. In conclusion, the compounds 7b and 5d are potential candidates for inducing apoptosis in different genotypic BC cell lines.

scholarly journals Design, Synthesis, Antibacterial, Antifungal and Anticancer Evaluations of Novel β-Pinene Quaternary Ammonium Salts

2021 ◽  
Vol 22 (20) ◽  
pp. 11299
Author(s):  
Li Zhang ◽  
Xue-Zhen Feng ◽  
Zhuan-Quan Xiao ◽  
Guo-Rong Fan ◽  
Shang-Xing Chen ◽  
...  
Keyword(s):  
Cell Lines ◽  
Anticancer Agents ◽  
Quaternary Ammonium ◽  
Biological Activities ◽  
Cell Membrane Permeability ◽  
Vitro Assay ◽  
Ic50 Values ◽  
Hct 116 ◽  
Mcf 7

β-pinene is a monoterpene isolated from turpentine oil and numerous other plants’ essential oils, which has a broad spectrum of biological activities. In the current work, six novel β-pinene quaternary ammonium (β-PQA) salts were synthesized and evaluated in vitro for their antifungal, antibacterial and anticancer activities. The in vitro assay results revealed that compounds 4a and 4b presented remarkable antimicrobial activity against the tested fungi and bacteria. In particular, compound 4a showed excellent activities against F. oxysporum f.sp. niveum, P. nicotianae var.nicotianae, R. solani, D. pinea and Fusicoccumaesculi, with EC50 values of 4.50, 10.92, 9.45, 10.82 and 6.34 μg/mL, respectively. Moreover, compound 4a showed the best antibacterial action against E. coli, P. aeruginosa, S. aureus and B. subtilis, with MIC at 2.5, 0.625, 1.25 and 1.25 μg/mL, respectively. The anticancer activity results demonstrated that compounds 4a, 4b, 4c and 4f exhibited remarkable activity against HCT-116 and MCF-7 cell lines, with IC50 values ranged from 1.10 to 25.54 μM. Notably, the compound 4c displayed the strongest cytotoxicity against HCT-116 and MCF-7 cell lines, with the IC50 values of 1.10 and 2.46 μM, respectively. Furthermore, preliminary antimicrobial mechanistic studies revealed that compound 4a might cause mycelium abnormalities of microbial, cell membrane permeability changes and inhibition of the activity of ATP. Altogether, these findings open interesting perspectives to the application of β-PQA salts as a novel leading structure for the development of effective antimicrobial and anticancer agents.

Synthesis of New 4-Chloro-6-Methylpyrimidin-2-yl-Aminophosphonates as Potential DU145 and A549 Cancer Cell Inhibitors

2020 ◽  
Vol 17 (4) ◽  
pp. 396-410
Author(s):  
Gajjala Raghavendra Reddy ◽  
Chinta Raveendra Reddy ◽  
Gopireddy Venkata Subba Reddy ◽  
Pasupuleti Visweswara Rao ◽  
Meenakshisundaram Swaminathan ◽  
...  
Keyword(s):  
Cell Lines ◽  
Biological Activities ◽  
Solid Acid Catalyst ◽  
Acid Catalyst ◽  
Sulfated Titania ◽  
Scope For Growth ◽  
Inhibition Of Growth ◽  
Anti Cancer ◽  
High Yields

: A series of new α-aminophosphonates containing potential anticancer active 4-chloro-6- methylpyrimidin-2-amino pharmacophore were synthesized. Background: α-Aminophosphonates are of growing interest to the researchers due to their biological activities. Besides aminophosphoryl functionality, which is responsible for the vital activity, incorporation of a captivating pharmacophore on it will definitely enrich its activity. Objective: Erstwhile many of the reported α-aminophosphonates impregnated with bioactive heterocycles like quinazoline, chromene, pyrazole, furan and thiophene were used as anticancer drugs, and we are intended to enhance the anticancer potentiality of α-aminophosphonates by substituting a new 4-chloro-6-methylpyrimidin-2-yl group into its structure, specifically on nitrogen atom. Methods: Title compounds were synthesized by Kabachnik-Fields reaction by using sulfated Titania, a solid acid catalyst that is encompassed with high density of Lewis acidic reaction sites. The series of synthesized compounds were screened for in vitro anti-cancer activity and their ADMET, QSAR and drug properties studied. Results: Structures of all the title compounds synthesized in high yields were confirmed by spectral & elemental analyses. Their anti-cancer screening studies on various cell lines and evaluation of other properties revealed their potentiality towards the inhibition of growth of DU145 & A549 cell lines. Conclusion: The substitution of 4-chloro-6-methylpyrimidin-2-amino moiety on to the amino functionality of the α-aminophosphonates is a critical task invariably due to the substitutions that are located on α-carbon. As such, this substitution had increased the scope for growth inhibition of DU145 and A549 cancer cells.

Design, Synthesis of novel coumarin conjugated acetamides as promising anticancer agents: An in-silico and in-vitro approach.

2020 ◽  
Vol 20 ◽  
Author(s):  
Mamatha S. V ◽  
S. L. Belagali ◽  
Mahesh Bhat ◽  
Vijay M. Kumbar
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Mtt Assay ◽  
Anticancer Agents ◽  
In Silico ◽  
Active Sites ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Mcf 7

Background: Coumarin and benzophenone possess a vast sphere of biological activities whereas thiazoles display various pharmacological properties. Hence we focused on incorporation of coumarin and thiazole core to the benzophenone skeleton to enhance the bioactivity anticipating their interesting biological properties. Objective: The objective of the current work is synthesis and biological evaluation of a novel series of coumarin fused thiazole derivatives. Methods: A novel series of Coumarin conjugated thiazolyl acetamide hybrid derivatives were synthesized by multistep reaction sequence and were characterized by the FT-IR, LCMS and NMR spectral techniques. The newly synthesized compounds were screened for anticancer activity by in-silico and in-vitro methods. The cytotoxicity of the synthesized unique compounds had been executed for two different cancer cell lines MCF-7 (Breast cancer) and KB (Oral cancer) in comparison with standard paclitaxel by MTT assay. Results: The compound 7f is the potent motif with an acceptable range of IC 50 values for anticancer activity were 63.54 µg/ml and 55.67 µg/ml, against the MCF-7 and KB cell lines, respectively. Molecule docking model revealed that this compound formed three conventional hydrogen bonds with the active sites of the amino acids MET 769, ARG 817 and LYS 721. Conclusion: Compound 7f with two methyl groups on the phenoxy ring and one 4-position methoxy group on the benzoyl ring, showed a significant cytotoxic effect. An advantageous level of low toxicity against normal cell line (L292) by MTT assay was determined.

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