One-pot synthesis of fused benzoxazino[1,2,3]triazolyl[4,5-c]quinolinone derivatives and their anticancer activity

RSC Advances ◽  
2016 ◽  
Vol 6 (78) ◽  
pp. 74332-74339 ◽  
Author(s):  
Sirassu Narsimha ◽  
Kumara Swamy Battula ◽  
Satheesh Kumar Nukala ◽  
Ramesh Gondru ◽  
Yellu Narasimha Reddy ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Human Cancer Cell ◽  
One Pot ◽  
Human Cancer Cell Lines ◽  
One Pot Synthesis ◽  
Mcf 7

Cu/Pd catalyzed one pot synthesis of fused benzoxazino[1,2,3]triazolyl[4,5-c]quinolinone hybrids and their cytotoxic activity against human cancer cell lines MCF-7, HeLa and A-549 is described.

scholarly journals Alkaloids From Zanthoxylum nitidum and Their Cytotoxic Activity

2019 ◽  
Vol 14 (5) ◽  
pp. 1934578X1984413
Author(s):  
Thi Hong Van Nguyen ◽  
Thi Tuyen Tran ◽  
Thi Inh Cam ◽  
Minh Quan Pham ◽  
Quoc Long Pham ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Spectroscopy Data ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Zanthoxylum Nitidum ◽  
Mcf 7

Zanthoxylum nitidum (Roxb.) DC (Rutaceae) is a traditional medicine used for the treatment of various diseases like toothache, gingivitis, fever, colic vomiting, diarrhea, and cholera. Three new alkaloids, zanthocadinanine C (1), 7-methoxy-8-demethoxynitidine (2), and zanthonitiside I (3) were isolated from the stems and twigs of Z. nitidum. Their structures were determined on the basis of extensive spectroscopic, including 1-dimensional and 2-dimensional nuclear magnetic resonance and mass spectroscopy data. Compounds 1–3 were evaluated for cytotoxic activity against 5 human cancer cell lines, KB, MCF-7, LNCaP, HepG-2, and LU-1. Compound 2 showed significant cytotoxic activity against all tested human cancer cell lines with IC50 values ranging from 10.3 to 12.6 µM.

Synthesis of imidazo[2,1-b][1,3,4]thiadiazole–chalcones as apoptosis inducing anticancer agents

MedChemComm ◽  
2014 ◽  
Vol 5 (11) ◽  
pp. 1718-1723 ◽  
Author(s):  
Ahmed Kamal ◽  
Vangala Santhosh Reddy ◽  
Karnewar Santosh ◽  
G. Bharath Kumar ◽  
Anver Basha Shaik ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

A library of imidazothiadiazole–chalcone conjugates were synthesised and investigated for their cytotoxic activity against various human cancer cell lines. Some of the tested compounds like 7a, 7b, 11a and 11b exhibited promising anticancer activity.

One-Pot Synthesis of New (1,3-Thiazolo[5,4-b]pyridin-2-yl)benzenediols and Their Antiproliferative Activities against Human Cancer Cell Lines

2012 ◽  
Vol 9 (1) ◽  
pp. 48-57 ◽  
Author(s):  
Joanna Matysiak ◽  
Monika M. Karpińska ◽  
Andrzej Niewiadomy ◽  
Joanna Wietrzyk ◽  
Dagmara Kłopotowska
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
One Pot ◽  
Human Cancer Cell Lines ◽  
One Pot Synthesis ◽  
Antiproliferative Activities

scholarly journals Damarane-type Saponins from Gynostemma Longipes and their Cytotoxic Activity

2015 ◽  
Vol 10 (8) ◽  
pp. 1934578X1501000
Author(s):  
Pham Tuan Anh ◽  
Pham Thanh Ky ◽  
Nguyen Thi Cuc ◽  
Nguyen Xuan Nhiem ◽  
Pham Hai Yen ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
2D Nmr ◽  
Moderate Activity ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Ht 29 ◽  
Mcf 7

Two new damarane- type saponins, named gylongiposides II-III (1 and 2), along with one known compound, (23 S)-3β,20ζ,21ζ-trihydroxy-19-oxo-21,23-epoxydammar-24-ene 3- O-α-L-rhamnopyranosyl-(1→2)-[β-D-xylopyranosyl-(1→3)]-α-L-arabinopyranoside, were isolated from the leaves of Gynostemma longipes C.Y.Wu. Their structures were determined by 1D- and 2D-NMR and HR-ESI-MS spectra. Compounds 1–3 exhibited moderate activity against four human cancer cell lines, A-549, HT-29, OVCAR, and MCF-7, with IC50 values ranging from 9.8 ± 2.1 to 49.6 ± 2.6 μM.

Design and Synthesis of Indole Pyrimidine Scaffolds as Potential KSP Inhibitors and Anticancer Agents

2019 ◽  
Vol 15 (1) ◽  
pp. 28-35
Author(s):  
Radhika Chelamalla ◽  
Ajitha Makula
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Cytotoxic Agents ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Antimitotic Activity ◽  
Mcf 7

Background: Several biological activities like anticancer, anti-inflammatory, analgesic, antitubercular activities are reported for pyrimidine scaffolds. Extensive work on pyrimidine indole scaffolds is required for antimitotic activity. Objective: To synthesize a novel Indole Pyrimidine scaffold via an efficient synthetic method and to evaluate cytotoxic activity using various human cancer cell lines. Methods: 4,4-(3-substituted phenyl)-6-methyl-N-[(Z)-(5-methyl-2-oxo-indolin-3-ylidene)amino]-2- oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide derivatives were designed, synthesized and evaluated for cytotoxic activity. The structures were confirmed by IR, 1H NMR, C13NMR and Mass spectroscopy. The antiproliferative activities of the synthesized compounds were evaluated in vitro against human cancer cell lines including HeLa and MCF-7. Results: The results revealed that most of the compounds possessed moderate to excellent potency. Three among 10 molecules, showed more than 70% growth inhibition against all tested cancer cells. The nature of the substituent group (R) on the indole ring affected significantly the anti-proliferative activity of the molecules. The IC50 values of the most promising compound 4h are 76.4µM and 88.2µM against HeLa and MCF-7 respectively, which are closer to the standard compound doxorubicin. Conclusion: Molecular docking analysis demonstrated that 4b and 4d interact and bind efficiently with KSP binding site. The preliminary results made us investigate for further development of potent indole-pyrimidine scaffolds as cytotoxic agents

scholarly journals In vitro anticancer activity of N-benzyl 1,10-phenanthroline derivatives on human cancer cell lines and their selectivity

2018 ◽  
Vol 23 (2) ◽  
pp. 68
Author(s):  
Eti Nurwening Sholikhah ◽  
Jumina Jumina ◽  
Sitarina Widyarini ◽  
Ruslin Hadanu ◽  
Mustofa Mustofa
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Vero Cell Line ◽  
Mcf 7

This research was conducted to evaluate the anticancer activity of new compounds of benzyl-1,10- phenanthroline derivatives and their selectivity. In vitro anticancer activity of 11 benzyl-1,10-phenanthroline derivatives were conducted on three human cancer cell lines, cervical cancer (HeLa), myeloma (NS-1), and breast cancer (MCF-7) using MTT-based cytotoxicity assay. The cytotoxicity of each compound was assessed to normal Vero cell line by the same method. The in vitro anticancer activity and cytotoxicity was expressed by the concentration inhibiting 50% of the cell growth (IC50), and the selectivity index (SI) was determined by calculating ratio of the IC50 on Vero cell line and the human cancer cell lines. The results showed that among the 11 compounds tested, the (1)-N-(4-butoxybenzyl)-1,10-phenanthrolinium bromide exhibited the best in vitro anticancer activity with an IC50 27.60 ± 2.76 µM on HeLa, 6.42 ± 5.53 µM on NS-1 and 9.44 ± 2.17 µM on MCF-7 cell lines. Its SI were 377.65 ± 39.97 on HeLa, 6158.72 ± 5306.34 on NS-1 and 1140.11 ± 261.85 on MCF-7 cell lines. This study demonstrated that (1)-N-(4-butoxybenzyl)-1,10-phenanthrolinium bromide possessed a potential in vitro anticancer activity on cancer cell lines with high selectivity

Design, Synthesis and Biological Evaluation of 3-(3,4,5-Trimethoxyphenyl)- 5-(2-(5-arylbenzo[b]thiophen-3-yl)oxazol-5-yl)isoxazole Derivatives as Anticancer Agents

2020 ◽  
Vol 17 (5) ◽  
pp. 345-351
Author(s):  
Syndla Premalatha ◽  
G. Rambabu ◽  
Islavathu Hatti ◽  
Dittakavi Ramachandran
Keyword(s):  
Breast Cancer ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Biological Evaluation ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Isoxazole Derivatives

A new series of 3-(3,4,5-trimethoxyphenyl)-5-(2-(5-arylbenzo[b]thiophen-3-yl)oxa zol-5- yl)isoxazole derivatives were designed and synthesized. All these derivatives were evaluated for their anticancer activity against various human cancer cell lines such as MCF-7 (breast cancer), A549 (lung cancer), DU-145 (prostate cancer) and MDA MB-231 (breast cancer)-four human cancer cell lines by using MTT assay. Here, etoposide was used as a standard reference drug and most of the compounds were exhibited good anticancer activity with respect to cell lines. Among all compounds, five compounds 11b, 11c, 11f, 11i and 11j showed more potent activity than standard drug, in which, compound 11f was the most promising compound.

scholarly journals Discovery of New Pyrazolopyridine, Furopyridine, and Pyridine Derivatives as CDK2 Inhibitors: Design, Synthesis, Docking Studies, and Anti-Proliferative Activity

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3923
Author(s):  
Adel A.-H. Abdel-Rahman ◽  
Amira K. F. Shaban ◽  
Ibrahim F. Nassar ◽  
Dina S. EL-Kady ◽  
Nasser S. M. Ismail ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Molecular Docking Study ◽  
Human Cancer Cell Lines ◽  
Hct 116 ◽  
Mcf 7

New pyridine, pyrazoloyridine, and furopyridine derivatives substituted with naphthyl and thienyl moieties were designed and synthesized starting from 6-(naphthalen-2-yl)-2-oxo-4-(thiophen-2-yl)-1,2-dihydropyridine-3-carbonitrile (1). The chloro, methoxy, cholroacetoxy, imidazolyl, azide, and arylamino derivatives were prepared to obtain the pyridine-−C2 functionalized derivatives. The derived pyrazolpyridine-N-glycosides were synthesized via heterocyclization of the C2-thioxopyridine derivative followed by glycosylation using glucose and galactose. The furopyridine derivative 14 and the tricyclic pyrido[3′,2′:4,5]furo[3,2-d]pyrimidine 15 were prepared via heterocyclization of the ester derivative followed by a reaction with formamide. The newly synthesized compounds were evaluated for their ability to in vitro inhibit the CDK2 enzyme. In addition, the cytotoxicity of the compounds was tested against four different human cancer cell lines (HCT-116, MCF-7, HepG2, and A549). The CDK2/cyclin A2 enzyme inhibitory results revealed that pyridone 1, 2-chloro-6-(naphthalen-2-yl)-4-(thiophen-2-yl)nicotinonitrile (4), 6-(naphthalen-2-yl)-4-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-amine (8), S-(3-cyano-6-(naphthaen-2-yl)-4-(thiophen-2-yl)pyridin-2-yl) 2-chloroethanethioate (11), and ethyl 3-amino-6-(naphthalen-2-yl)-4-(thiophen-2-yl)furo[2,3-b]pyridine-2-carboxylate (14) are among the most active inhibitors with IC50 values of 0.57, 0.24, 0.65, 0.50, and 0.93 µM, respectively, compared to roscovitine (IC50 0.394 μM). Most compounds showed significant inhibition on different human cancer cell lines (HCT-116, MCF-7, HepG2, and A549) with IC50 ranges of 31.3–49.0, 19.3–55.5, 22.7–44.8, and 36.8–70.7 μM, respectively compared to doxorubicin (IC50 40.0, 64.8, 24.7 and 58.1 µM, respectively). Furthermore, a molecular docking study suggests that most of the target compounds have a similar binding mode as a reference compound in the active site of the CDK2 enzyme. The structural requirements controlling the CDK2 inhibitory activity were determined through the generation of a statistically significant 2D-QSAR model.

Uptake Studies of Free and Liposomal Sclareol by Mcf-7 and H-460 Human Cancer Cell Lines

2007 ◽  
pp. 125-133
Author(s):  
Agnes Paradissis ◽  
Sophia Hatziantoniou ◽  
Aristidis Georgopoulos ◽  
Konstantinos Dimas ◽  
Costas Demetzos
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Uptake Studies ◽  
Mcf 7
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