scholarly journals Novel quinolines carrying pyridine, thienopyridine, isoquinoline, thiazolidine, thiazole and thiophene moieties as potential anticancer agents

2016 ◽  
Vol 66 (2) ◽  
pp. 155-171 ◽  
Author(s):  
Mostafa M. Ghorab ◽  
Mansour S. Alsaid ◽  
Mohammed S. Al-Dosari ◽  
Fatma A. Ragab ◽  
Abdullah A. Al-Mishari ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cytotoxic Activity ◽  
Cell Line ◽  
Spectral Data ◽  
Anticancer Agents ◽  
Breast Cancer Cell Line ◽  
Cancer Cell Line ◽  
Biologically Active ◽  
Moderate Activity ◽  
Elemental Analyses

Abstract As a part of ongoing studies in developing new anticancer agents, novel 1,2-dihydropyridine 4, thienopyridine 5, isoquinolines 6–20, acrylamide 21, thiazolidine 22, thiazoles 23–29 and thiophenes 33–35 bearing a biologically active quinoline nucleus were synthesized. The structure of newly synthesized compounds was confirmed on the basis of elemental analyses and spectral data. All the newly synthesized compounds were evaluated for their cytotoxic activity against the breast cancer cell line MCF7. 2,3-Dihydrothiazole-5-carboxamides 27, 25, 4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide (34), 1,2-dihydroisoquinoline-7-carbonitrile (7), 5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide (35), 1,2-dihydroisoquinoline-7-carbonitrile (6), 2-cyano-3-(dimethylamino)-N-(quinolin-3-yl)acrylamide (21), 1,2-dihydroisoquinoline-7-carbonitriles (11) and (8) exhibited higher activity (IC50 values of 27–45 μmol L–1) compared to doxorubicin (IC50 47.9 μmol L–1). LQ quinolin-3-yl)-1,2-dihydroisoquinoline-7-carbonitrile (12), 2-thioxo-2,3-dihydrothiazole-5-carboxamide (28) and quinolin-3-yl)-1,2-dihydroisoquinoline-7-carbonitrile (15) show activity comparable to doxorubicin, while (quinolin-3-yl)-1,2-dihydroisoquinoline-7-carbonitrile (9), 2,3-dihydrothiazole-5-carboxamide (24), thieno [3,4-c] pyridine-4(5H)-one (5), cyclopenta[b]thiophene-3-carboxamide (33) and (quinolin-3-yl)-6-stryl-1,2-dihydroisoquinoline-7-carbonitrile (10) exhibited moderate activity, lower than doxorubicin.

CYTOTOXIC EFFECT OF HEPCIDIN (TH1-5) ON HUMAN BREAST CANCER CELL LINE (MCF7)

2015 ◽  
Vol 77 (3) ◽  
Author(s):  
Mohammed Al-kassim Hassan ◽  
Wan-Atirah Azemin ◽  
Saravanan Dharmaraj ◽  
Khamsah Suryati Mohd
Keyword(s):  
Breast Cancer ◽  
Cytotoxic Activity ◽  
Cell Line ◽  
Cancer Cell ◽  
Breast Cancer Cell Line ◽  
Human Breast Cancer ◽  
Cancer Cell Line ◽  
Human Breast Cancer Cell ◽  
Human Breast ◽  
Nih 3T3

Hepcidin (TH1-5) is a cysteine-rich antimicrobial peptide originally isolated from the freshwater fish Oreochromis mossambicus. A synthesized form of the peptide has been reported to exhibit cytotoxic activity against few human cancer cell lines. This study investigated the potential cytotoxicity of the peptide against human breast cancer cell line and normal mouse embryonic fibroblast cell line (NIH/3T3) using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Morphological changes by acridine orange and propidium iodide (AO/PI) double staining were also studied to determine apoptotic evidences. Hepcidin (TH1-5) showed cytotoxic activity against MCF7 with an IC50 of 20 mg/mL but no significant effect against NIH/3T3. This outcome indicates hepcidin (TH1-5) to be a promising cytotoxic peptide that warrants further studies as a potential anticancer agent for breast cancer therapy.

scholarly journals Flavonoid Constituents of Carduncellus Mareoticus (Del.) Hanelt and their Biological Activities

2008 ◽  
Vol 3 (5) ◽  
pp. 1934578X0800300
Author(s):  
Marwan M. Shabana ◽  
Moshera M. El-Sherei ◽  
Mohamed Y. Moussa ◽  
Amany A. Sleem ◽  
Hosam M. Abdallah
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cancer Cell ◽  
Breast Cancer Cell Line ◽  
Biological Activities ◽  
Cancer Cell Line ◽  
Ethanolic Extract ◽  
Ethyl Acetate Fraction ◽  
Moderate Activity ◽  
First Time

The total ethanolic extract (TEE) of Carduncellus mareoticus (Del.) Hanelt showed antioxidant and antihyperlipidemic activities, which were attributed to the ethyl acetate fraction (EAF). Also TEE showed potent cytotoxic activity against a cervix cancer cell line (IC50 = 5 μg/mL) and moderate activity against a breast cancer cell line. Chemical investigation of EAF led to the isolation of a new flavonoid, 8-hydroxy-5-methoxyluteolin 7- O-β-D-glucopyranoside (11), along with ten known metabolites (1–10). Three of these compounds, isorhamnetin 3- O-β-D-glucopyranoside (7), luteolin 3′- O-β-D-glucopyranoside (8), and eriodictyol 7- O-β-D-glucopyranoside (9) are reported for the first time from the genus Carduncellus, and two compounds, chrysoeriol 7- O-β-D-glucopyranoside (6), and luteolin 7- O-β-D-glucopyranoside (10), for the first time from C. mareoticus. The rest of the isolated compounds, chrysoeriol (1), luteolin (2), quercetin (3), kaempferol 3- O-α-L-arabinopyranoside (4), and kaempferol 3- O-β-D-glucopyranoside (5) have been previously reported from the genus.

Sign in / Sign up

Export Citation Format

Share Document