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 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.

scholarly journals Design, Synthesis and Cytotoxic Evaluation of 4-Anilinoquinazoline– triazole–AZT Hybrids as Anticancer Agents

2018 ◽  
Vol 13 (12) ◽  
pp. 1934578X1801301
Author(s):  
Le Nhat Thuy Giang ◽  
Nguyen Thi Nga ◽  
Dinh Thuy Van ◽  
Dang Thi Tuyet Anh ◽  
Hoang Thi Phuong ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Anticancer Activities ◽  
Cytotoxic Potential ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Dilution Assay ◽  
Cancer Activity

A series of 4-anilinoquinazoline–triazole–AZT hybrids were designed and synthesized as anticancer agents. Their cytotoxic potential has been evaluated by means of a micro-dilution assay against three human cancer cell lines (KB, epidermoid carcinoma; HepG2, hepatoma carcinoma; SK-Lu-1, non-small lung cancer). The biological results revealed that compounds 4b and 6d showed good anticancer activities against KB, HepG2, and Lu cell lines (IC50 values ranging from 9 μM to 100 μM). Especially, compounds 4b and 6d exhibited up to 3-fold more potent than reference drugs erlotinib hydrochloride and AZT in term of anti-lung cancer activity.

scholarly journals Design, synthesis and biological evaluation of imidazopyridine–propenone conjugates as potent tubulin inhibitors

MedChemComm ◽  
2017 ◽  
Vol 8 (5) ◽  
pp. 1000-1006 ◽  
Author(s):  
Ibrahim Bin Sayeed ◽  
V. Lakshma Nayak ◽  
Mohd Adil Shareef ◽  
Neeraj Kumar Chouhan ◽  
Ahmed Kamal
Keyword(s):  
Antitumor Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Biological Evaluation ◽  
Human Cancer Cell ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Tubulin Inhibitors ◽  
Synthesis And Biological Evaluation

A library of imidazopyridine–propenone conjugates (8a–8u) were synthesized and evaluated for their antitumor activity against four human cancer cell lines.

scholarly journals Syntheses and Anticancer Activities of Novel Glucosylated (-)-Epigallocatechin-3-Gallate Derivatives Linked via Triazole Rings

2021 ◽  
Author(s):  
Cheng-Ting Zi ◽  
Bo-Ya Shi ◽  
Ze-Hao Wang ◽  
Ning Zhang ◽  
Yin-Rong Xie ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Anticancer Activities ◽  
Glucose Residue ◽  
Human Cancer Cell Lines ◽  
Mtt Assays ◽  
Mcf 7

Abstract Novel glucosylated (-)-epigallocatechin-3-gallate derivatives 10 – 13 having the EGCG analogues conjugated to the D-glucosyl azide were synthesized by carrying out the copper-catalyzed azide-alkyne cycloaddition (CuAAC) reaction, and were evaluated for their cytotoxicities against a panel of five human cancer cell lines (HL-60, SMMC-7721, A-549, MCF-7 and SW480) using MTT assays. Compounds 10 and 11 showed the highest levels of cytotoxicity against the HL-60 cells with IC50 values of 4.57 μM and 3.78 μM, respectively, and showed moderate selectivity towards cancer cell lines. Compound 11 was also shown to induce apoptosis in HL-60 cells. Most notably, inclusion of the perbutyrylated glucose residue in an EGCG derivative was concluded to lead to increased anticancer activity.

scholarly journals The Design, Synthesis, and Evaluation of Hypoxia-Activated Prodrugs of the KDAC Inhibitor Panobinostat

2020 ◽  
Author(s):  
Ewen Calder ◽  
Anna Skwarska ◽  
Deborah Sneddon ◽  
Lisa Folkes ◽  
Ishna N. Mistry ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Parent Drug ◽  
Human Cancer Cell ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Design And Synthesis ◽  
Initial Validation

The design and synthesis of four hypoxia-activated prodrugs of the KDAC inhibitor panobinostat is described. Initial validation of these compounds using isolated enzymes, and in two human cancer cell lines, reveals that the nitroimidazole-based prodrug (NI-Pano, CH-03) undergoes efficient bioreduction and fragmentation to release the parent drug, panobinostat. NI-Pano was identified as the optimum compound for use in further studies in cells, spheroid tumor models, and <i>in vivo</i>.

Design, Synthesis, and Cytotoxic Activity of New Tubulysin Analogues

Synlett ◽  
2021 ◽  
Author(s):  
Anh Tuan Tran ◽  
Chien Van Tran ◽  
Hai Van Le ◽  
Loc Van Tran ◽  
Thao Thi Phuong Tran ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Cytotoxic Activities ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Ht 29

AbstractSynthesis of tubulysin analogues, containing an N-methyl substituent on tubuvaline-amide together with the replacement of either the hydrophobic N-terminal N-methyl pipecolic acid (Mep) or at both N- and C- terminal peptides with available heteroaromatic acids and an unsaturated tubuphenylalanine moiety, respectively, were described. The in vitro cytotoxic activity by SRB assay on five cancer cell lines for sixteen tubulysins was evaluated. Among them, five analogues exhibited strong cytotoxic activities against five human cancer cell lines, including human breast carcinoma (MCF7), human colorectal adenocarcinoma (HT-29), HL-60, SW-480, human lung adenocarcinoma (A459). Interestingly, one analogue showed the strongest cytotoxicity on all five tested cell lines even much higher toxicity than the reference compound ellipticine.

scholarly journals Bauhinia variegataLeaf Extracts Exhibit Considerable Antibacterial, Antioxidant, and Anticancer Activities

2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Amita Mishra ◽  
Amit Kumar Sharma ◽  
Shashank Kumar ◽  
Ajit K. Saxena ◽  
Abhay K. Pandey
Keyword(s):  
Cell Lines ◽  
Metal Ion ◽  
Human Cancer ◽  
Reducing Power ◽  
Ethanol Extract ◽  
Anticancer Activities ◽  
Leaf Extracts ◽  
Human Cancer Cell Lines ◽  
Polar Extracts ◽  
Mcf 7

The present study reports the phytochemical profiling, antimicrobial, antioxidant, and anticancer activities ofBauhinia variegataleaf extracts. The reducing sugar, anthraquinone, and saponins were observed in polar extracts, while terpenoids and alkaloids were present in nonpolar and ethanol extracts. Total flavonoid contents in various extracts were found in the range of 11–222.67 mg QE/g. In disc diffusion assays, petroleum ether and chloroform fractions exhibited considerable inhibition againstKlebsiella pneumoniae. Several other extracts also showed antibacterial activity against pathogenic strains ofE. coli,Proteusspp. andPseudomonasspp. Minimum bactericidal concentration (MBC) values of potential extracts were found between 3.5 and 28.40 mg/mL. The lowest MBC (3.5 mg/mL) was recorded for ethanol extract againstPseudomonasspp. The antioxidant activity of the extracts was compared with standard antioxidants. Dose dependent response was observed in reducing power of extracts. Polar extracts demonstrated appreciable metal ion chelating activity at lower concentrations (10–40 μg/mL). Many extracts showed significant antioxidant response in beta carotene bleaching assay. AQ fraction ofB. variegatashowed pronounced cytotoxic effect against DU-145, HOP-62, IGR-OV-1, MCF-7, and THP-1 human cancer cell lines with 90–99% cell growth inhibitory activity. Ethyl acetate fraction also produced considerable cytotoxicity against MCF-7 and THP-1 cell lines. The study demonstrates notable antibacterial, antioxidant, and anticancer activities inB. variegataleaf extracts.

scholarly journals Aaptamines from the Marine SpongeAaptossp. Display Anticancer Activities in Human Cancer Cell Lines and Modulate AP-1-, NF-κB-, and p53-Dependent Transcriptional Activity in Mouse JB6 Cl41 Cells

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Sergey A. Dyshlovoy ◽  
Sergey N. Fedorov ◽  
Larisa K. Shubina ◽  
Alexandra S. Kuzmich ◽  
Carsten Bokemeyer ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Cellular Response ◽  
Transcriptional Activity ◽  
Human Cancer ◽  
Cell Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Anticancer Activities ◽  
Human Cancer Cell Lines

Aaptamine (8,9-dimethoxy-1H-benzo[de][1,6]naphthyridine) is a marine natural compound possessing antioxidative, antimicrobial, antifungal, and antiretroviral activity. Earlier, we have found that aaptamine and its derivatives demonstrate equal anticancer effects against the human germ cell cancer cell lines NT2 and NT2-R and cause some changes in the proteome of these cells. In order to explore further the mechanism of action of aaptamine and its derivatives, we studied the effects of aaptamine (1), demethyl(oxy)aaptamine (2), and isoaaptamine (3) on human cancer cell lines and on AP-1-, NF-κB-, and p53-dependent transcriptional activity in murine JB6 Cl41 cells. We showed that compounds1–3demonstrate anticancer activity in THP-1, HeLa, SNU-C4, SK-MEL-28, and MDA-MB-231 human cancer cell lines. Additionally, all compounds were found to prevent EGF-induced neoplastic transformation of murine JB6 Cl41 cells. Nuclear factors AP-1, NF-κB, and p53 are involved in the cellular response to high and nontoxic concentrations of aaptamine alkaloids1–3. Furthermore, inhibition of EGF-induced JB6 cell transformation, which is exerted by the compounds1–3at low nontoxic concentrations of 0.7–2.1 μM, cannot be explained by activation of AP-1 and NF-κB.

Recent development of tetrahydro-quinoline/isoquinoline based compounds as anticancer agents

2021 ◽  
Vol 21 ◽  
Author(s):  
Pratik Yadav ◽  
Ashish Kumar ◽  
Ismail Althagafi ◽  
Vishal Nemaysh ◽  
Reeta Rai ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Biological Activities ◽  
Cancer Cell Lines ◽  
New Drugs ◽  
Anticancer Activities ◽  
Human Cancer Cell Lines ◽  
Anticancer Properties

: Tetrahydroquinoline and isoquinoline scaffolds are important class heterocyclic compounds, which is implied for the development of new drugs and diagnostic for therapeutic function. Naturally occurring as well as synthetic tetrahydroquinolines/isoquinolines possess many different biological activities and have been testified as remarkable cytotoxic and potency in human cancer cell lines. Tetrahydroquinoline/isoquinolines based compounds displayed a key role in the development of anticancer drugs or lead molecules and acting through various mechanisms such as cell proliferation, apoptosis, DNA fragmentation, inhibition of tubulin polymerization, induced cell cycle arrest, interruption of cell migration, and modulation. The number of tetrahydroquinoline/isoquinoline derivatives has been reported as potent anticancer agents. Due to promising anticancer activities and wide-ranging properties of these molecules, we have compiled the literature for the synthesis and anticancer properties of various tetrahydroquinolines and isoquinolines. We have reported the synthesis of potent tetrahydroquinoline/isoquinoline molecules of the last 10 years with their anticancer properties in various cancer cell lines and stated their half-maximal inhibitory concentration (IC50). In addition, we also considered the discussion of molecular docking and structural activity relationship wherever provided to understand the possible mode of activity a target involved and structural feature responsible for the better activity, so the reader can directly find the detail for designing new anticancer agents.

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