scholarly journals Syntheses and Structure–Activity Relationships in Growth Inhibition Activity against Human Cancer Cell Lines of 12 Substituted Berberine Derivatives

Molecules ◽  
2020 ◽  
Vol 25 (8) ◽  
pp. 1871 ◽  
Author(s):  
Bo Wang ◽  
An-Jun Deng ◽  
Zhi-Hong Li ◽  
Nan Wang ◽  
Hai-Lin Qin
Keyword(s):  
Growth Inhibition ◽  
Cell Lines ◽  
Human Cancer ◽  
Carbon Chain ◽  
Human Cancer Cell ◽  
Inhibition Activity ◽  
Human Cancer Cell Lines ◽  
Structure Activity ◽  
Amine Structure ◽  
Growth Inhibition Activity

In this study, quaternary berberine chloride is used as a lead compound to design and synthesize a series of berberine-12-amine derivatives to evaluate the growth inhibition activity against human cancer cell lines. Forty-two compounds of several series were obtained. The quaternary berberine-12-N,N-di-n-alkylamine chlorides showed the targeted activities with the IC50 values of most active compounds being dozens of times those of the positive control. A significant structure–activity relationship (SAR) was observed. The activities of quaternary berberine-12-N,N-di-n-alkylamine chlorides are significantly stronger than those of the reduced counterparts. In the range of about 6-8 carbon atoms, the activities increase with the elongation of n-alkyl carbon chain of 12-N,N-di-n-alkylamino, and when the carbon atom numbers are more than 6-8, the activities decrease with the elongation of n-alkyl carbon chain. The activities of the tertiary amine structure are significantly higher than that of the secondary amine structure.

The Effect of 5-Substitution on the Cytotoxicity of 2-(p-Methoxyphenyl)-1H-Benzimidazoles in Human Cancer Cell Lines

2005 ◽  
Vol 277-279 ◽  
pp. 23-27 ◽  
Author(s):  
Min Jin Kwon ◽  
Hwan Mook Kim ◽  
Dae Duk Kim ◽  
Jung Sun Kim
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Inhibition Activity ◽  
A549 Cell Line ◽  
Human Cancer Cell Lines ◽  
Structure Activity ◽  
Relationship Study

A series of 5-substituted 2-(p-methoxyphenyl)-1H-benzimidazoles was synthesized and evaluated for cytotoxicity against 4 human cancer cell lines, HCT 15, PC-3, A549, and ACHN. Except for the 5-chloro analogue, most of the 5-substituted compounds showed significant cytotoxicities in these cell lines. However, the structure activity relationship study revealed that neither the electronic nor the lipophilic parameters of the 5-substituents were related to cytotoxicity. Moreover, none of the analogues showed significant NF к-β inhibition activity implying that cytotoxicity was not related to this mechanism. The 5-methyl analogue was the most potent compound in this series with a GI50 of 0.9 µM in the A549 cell line.

Comparative studies of adriamycin and 28-Deacetyl sendanin onin vitro growth inhibition of human cancer cell lines

1994 ◽  
Vol 17 (2) ◽  
pp. 100-103 ◽  
Author(s):  
Hwan Mook Kim ◽  
Goo Taeg Oh ◽  
Sang Bae Han ◽  
Dong Ho Hong ◽  
Bang Yeon Hwang ◽  
...  
Keyword(s):  
Growth Inhibition ◽  
Cell Lines ◽  
Cancer Cell ◽  
Comparative Studies ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

scholarly journals Human cancer cell lines growth inhibition by GTn oligodeoxyribonucleotides recognizing single-stranded DNA-binding proteins

1998 ◽  
Vol 252 (2) ◽  
pp. 207-215 ◽  
Author(s):  
Bruna Scaggiante ◽  
Carla Morassutti ◽  
Barbara Dapas ◽  
Giuseppe Tolazzi ◽  
Franca Ustulin ◽  
...  
Keyword(s):  
Dna Binding ◽  
Growth Inhibition ◽  
Cell Lines ◽  
Cancer Cell ◽  
Binding Proteins ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Dna Binding Proteins ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

scholarly journals Design, Synthesis, Molecular Modelling and Anticancer Activities of New Fused Phenanthrolines

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 527 ◽  
Author(s):  
Cristina Maria Al Matarneh ◽  
Roxana Maria Amarandi ◽  
Anda Mihaela Craciun ◽  
Ionel I. Mangalagiu ◽  
Gheorghita Zbancioc ◽  
...  
Keyword(s):  
Cell Lines ◽  
Human Cancer ◽  
Docking Studies ◽  
Inhibition Activity ◽  
Anticancer Activities ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Colchicine Binding Site ◽  
Growth Inhibition Activity ◽  
Significant Growth Inhibition

Three series of fused pyrrolophenanthroline derivatives were designed as analogues of phenstatin and synthesized in two steps starting with 1,7-phenanthroline, 4,7-phenanthroline and 1,10-phenanthroline, respectively. Two (Compounds 8a and 11c) of the four compounds tested against a panel of sixty human cancer cell lines of the National Cancer Institute (NCI) exhibited significant growth inhibition activity on several cell lines. Compound 11c showed a broad spectrum in terms of antiproliferative efficacy with GI50 values in the range of 0.296 to 250 μM. Molecular docking studies indicated that Compounds 8a and 11c are accommodated in the colchicine binding site of tubulin in two different ways.

scholarly journals Modulating the activity of short arginine-tryptophan containing antibacterial peptides with N-terminal metallocenoyl groups

2012 ◽  
Vol 8 ◽  
pp. 1753-1764 ◽  
Author(s):  
H Bauke Albada ◽  
Alina-Iulia Chiriac ◽  
Michaela Wenzel ◽  
Maya Penkova ◽  
Julia E Bandow ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Growth Inhibition ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Inhibition Studies ◽  
Kinetics Of

A series of small synthetic arginine and tryptophan containing peptides was prepared and analyzed for their antibacterial activity. The effect of N-terminal substitution with metallocenoyl groups such as ferrocene (FcCO) and ruthenocene (RcCO) was investigated. Antibacterial activity in different media, growth inhibition, and killing kinetics of the most active peptides were determined. The toxicity of selected derivatives was determined against erythrocytes and three human cancer cell lines. It was shown that the replacement of an N-terminal arginine residue with a metallocenoyl moiety modulates the activity of WRWRW-peptides against Gram-positive and Gram-negative bacteria. MIC values of 2–6 µM for RcCO-W(RW)2 and 1–11 µM for (RW)3 were determined. Interestingly, W(RW)2-peptides derivatized with ferrocene were significantly less active than those derivatized with ruthenocene which have similar structural but different electronic properties, suggesting a major influence of the latter. The high activities observed for the RcCO-W(RW)2- and (RW)3-peptides led to an investigation of the origin of activity of these peptides using several important activity-related parameters. Firstly, killing kinetics of the RcCO-W(RW)2-peptide versus killing kinetics of the (RW)3 derivative showed faster reduction of the colony forming units for the RcCO-W(RW)2-peptide, although MIC values indicated higher activity for the (RW)3-peptide. This was confirmed by growth inhibition studies. Secondly, hemolysis studies revealed that both peptides did not lead to significant destruction of erythrocytes, even up to 500 µg/mL for (RW)3 and 250 µg/mL for RcCO-W(RW)2. In addition, toxicity against three human cancer cell lines (HepG2, HT29, MCF7) showed that the (RW)3-peptide had an IC50 value of ~140 µM and the RcW(RW)2 one of ~90 µM, indicating a potentially interesting therapeutic window. Both the killing kinetics and growth inhibition studies presented in this work point to a membrane-based mode of action for these two peptides, each having different kinetic parameters.

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