scholarly journals Synthesis and potential cytotoxic activity of some new benzoxazoles, imidazoles, benzimidazoles and tetrazoles

2013 ◽  
Vol 63 (2) ◽  
pp. 253-264 ◽  
Author(s):  
Subramaniyan Arulmurugan ◽  
Helen P. Kavitha
Keyword(s):  
Breast Cancer ◽  
Mass Spectrometry ◽  
Colon Cancer ◽  
Heterocyclic Compounds ◽  
Human Cancer ◽  
Assay Method ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Ht 29 ◽  
Mcf 7

2 The present work deals with the synthesis of some novel heterocyclic compounds such as benzoxazoles , 7, 13 and 19, imidazoles 3, 8, 14 and 20, benzimidazoles 4, 9, 15 and 21, and tetrazoles 10, 16, and 22. The synthesized compounds were characterized by IR, 1H NMR, mass spectrometry and elemental analysis. The compounds were evaluated for cytotoxicity against human cancer cell lines such as MCF-7 (breast cancer) and HT-29 (colon cancer) by the MTT assay method. Among the tested compounds, 4,4’-sulfonylbis(N-(2-(1H-benzo[d]imidazol- -2-yl)ethyl)aniline (9), N-bis(2-(benzo[d]oxazol-2-yl)-ethyl)- 6-phenyl-1,3,5-triazine-2,4-diamine (13), N-bis(2-(1H-benzo[ d]imidazol-2-yl)ethyl)-6-phenyl-1,3,5-triazine-2,4-diamine (15) and N-tris(2-1H-benzo[d]imidazol-2-yl)ethyl)- 1,3,5-triazine-2,4,6-triamine (21) showed potent cytotoxicity.

Design, Synthesis and Anticancer Evaluation of 1,2,4-Oxadiazole Bearing Isoxazole-Pyrazole Derivatives

2020 ◽  
Vol 17 (5) ◽  
pp. 352-359 ◽  
Author(s):  
Bhukya Ravinaik ◽  
Dittakavi Ramachandran ◽  
Mandava Venkata Basaveswara Rao
Keyword(s):  
Breast Cancer ◽  
Cell Lines ◽  
Human Cancer ◽  
Pyrazole Derivatives ◽  
Human Cancer Cell ◽  
Design Synthesis ◽  
Standard Drug ◽  
Human Cancer Cell Lines ◽  
A549 Lung ◽  
Mcf 7

A novel library of 1,2,4-oxadiazole bearing isoxazole-pyrazole derivatives (13a-j) were designed, synthesized and evaluated for their anticancer activity towards MCF-7 (breast cancer), A549 (lung cancer), DU-145 (prostate cancer) and MDA MB-231 (breast cancer) human cancer cell lines by MTT assay. Here etoposide used as standard drug. Among them, five compounds (13b, 13c, 13d, 13h and 13i) were exhibited more potent activity. In which compound 13h was the most promising compound against all cell lines MCF-7, A549, DU-145 and MDA MB-231.

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.

scholarly journals Two New Taxane Diterpenoids From Taxus baccata

2020 ◽  
Vol 15 (9) ◽  
pp. 1934578X2095328
Author(s):  
Qi Ding ◽  
Dong-Mei Fang ◽  
Xiao-Huan Li ◽  
Feng Gao
Keyword(s):  
Mass Spectrometry ◽  
Human Cancer ◽  
Ionization Mass ◽  
Taxus Baccata ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Nuclear Magnetic Resonance Spectra ◽  
Taxane Diterpenoids ◽  
Taxane Diterpenoid ◽  
Mcf 7

Two new diterpenoids named 13-oxo-wollifoliane-10,15-olide (1) and 19-acetoxy-7,9,10-deacetyl-baccatin VI (2), along with 14 known taxanes (3-16), were isolated from Taxus baccata. The structures of these compounds were elucidated by 1-dimensional and 2-dimensional nuclear magnetic resonance spectra, high-resolution electrospray ionization-mass spectrometry, and infrared spectroscopy. Structurally, 13-oxo-wollifoliane-10,15-olide (1) is the first taxane diterpenoid possessing an unusual carbonyl group at the C-13 position of the 11(15→1),11(10→9)bis- abeo-taxane structure (5/6/6/6/4 skeleton), and 19-acetoxy-7,9,10-deacetyl-baccatin VI (2) is a new compound containing an acetoxy group at the C-19 position of 6/8/6/4-taxane. Among the 14 known taxane compounds 3-16, compounds 7 and 9 were first isolated and reported from T. baccata. Several compounds (3-16) were evaluated for cytotoxicity against MCF-7 and HCT116 human cancer cell lines, but none of them showed considerable cytotoxic activity.

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 ◽  
2016 ◽  
Vol 6 (19) ◽  
pp. 15286-15297 ◽  
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.

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.

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

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.

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

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

Molecules ◽  
2019 ◽  
Vol 24 (15) ◽  
pp. 2772 ◽  
Author(s):  
Balkrishna ◽  
Das ◽  
Pokhrel ◽  
Joshi ◽  
Laxmi ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Human Cancer ◽  
Cell Cytotoxicity ◽  
Human Cancer Cell ◽  
Gloriosa Superba ◽  
Human Cancer Cell Lines ◽  
Insight Into ◽  
Mb231 Cell ◽  
Mcf 7

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.

Sign in / Sign up

Export Citation Format

Share Document