Colchicine: Isolation, LC–MS QTof Screening, and Anticancer Activity Study of Gloriosa superba Seeds

Colchicine was extracted from Gloriosa superba seeds using the Super Critical Fluid (CO2) Extraction (SCFE) technology. The seeds were purified upto 99.82% using column chromatography. Colchicine affinity was further investigated for anticancer activity in six human cancer cell lines, i.e., A549, MCF-7, MDA-MB231, PANC-1, HCT116, and SiHa. Purified colchicine showed the least cell cytotoxicity and antiproliferation and caused no G2/M arrest at clinically acceptable concentrations. Mitotic arrest was observed in only A549 and MDA-MB231 cell lines at 60nM concentration. Our finding indicated the possible use of colchicine at a clinically acceptable dose and provided insight into the science behind microtubule destabilization. However, more studies need to be conducted beforethese findings could be established.

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

Indonesian Journal of Biotechnology ◽

10.22146/ijbiotech.33997 ◽

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

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

RSC Advances ◽

10.1039/c6ra12285j ◽

2016 ◽

Vol 6 (78) ◽

pp. 74332-74339 ◽

Cited By ~ 14

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.

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Synthesis of novel N-9 substituted 6-(4-(4-propoxyphenyl)piperazin-1-yl)-9H-purine derivatives as inducers of apoptosis in MCF-7 breast cancer cells

RSC Advances ◽

10.1039/c5ra23242b ◽

2016 ◽

Vol 6 (19) ◽

pp. 15286-15297 ◽

Cited By ~ 8

Author(s):

Manjunath G. Sunagar ◽

Supreet Gaonkar ◽

Santosh G. Sunagar ◽

Narahari Deshapande ◽

Ningaraddi S. Belavagi ◽

...

Keyword(s):

Breast Cancer ◽

Anticancer Activity ◽

Cancer Cells ◽

Cell Lines ◽

Breast Cancer Cells ◽

Human Cancer ◽

Human Cancer Cell ◽

Purine Derivatives ◽

Human Cancer Cell Lines ◽

Mcf 7

A series of N-9 substituted 6-(4-(4-propoxyphenyl)piperazin-1-yl)-9H-purine derivatives (PP05–PP21) were prepared and evaluated for their anticancer activity against a panel of human cancer cell lines.

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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

Letters in Organic Chemistry ◽

10.2174/1570178616666191004105445 ◽

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.

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

Molecules ◽

10.3390/molecules26133923 ◽

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.

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Synthesis of novel amide and Schiff’s base functionalized novel pyrido[1,2-a] pyrimidin-4-one derivatives and their anticancer activity studies.

Letters in Organic Chemistry ◽

10.2174/1570178618666210512021950 ◽

2021 ◽

Vol 18 ◽

Author(s):

Sailu Betala ◽

Chiranjeevi Abba ◽

Hanumandlu Racha

Keyword(s):

Anticancer Activity ◽

Hydrazine Hydrate ◽

Human Cancer ◽

Aromatic Aldehydes ◽

Human Cancer Cell ◽

Hep G2 ◽

Schiff’S Base ◽

Human Cancer Cell Lines ◽

Amide Derivatives ◽

Mcf 7

Abstract: A series of novel amide and Schiffs base functionalized novel pyrido[1,2-a]pyrimidin-4-one derivatives were prepared starting from 6-(thiophene-2-yl)/phenyl-4-(trifluoromethyl) pyridin-2-amine 1a and 1b. These compounds on reaction with EMME, to afford compounds 2a and 2b, followed by cyclization to afford compounds 3a and 3b. Treatment of compound 3a and 3b with hydrazine hydrate to get compounds 4a and 4b, compounds 4a and 4b on reaction with different substituted aromatic aldehydes to get Schiff’s base derivatives 5a-j, in another way compounds 3a, 3b on reaction with aliphatic amines to get amide derivatives 6a-f. All the compounds 5a-j and 6a-f were screened against four human cancer cell lines (HeLa, COLO205, Hep G2, and MCF 7), among all the derivatives, compounds 5c, 5e, 6a, and 6b showed promising anticancer activity.

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

Nanomaterials and Nanosystems for Biomedical Applications ◽

10.1007/978-1-4020-6289-6_8 ◽

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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Alkaloids From Zanthoxylum nitidum and Their Cytotoxic Activity

Natural Product Communications ◽

10.1177/1934578x19844133 ◽

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.

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