Synthesis and biological evaluation of novel pyrano[3,2-c]carbazole derivatives as anti-tumor agents inducing apoptosis via tubulin polymerization inhibition

2015 ◽  
Vol 13 (5) ◽  
pp. 1404-1414 ◽  
Author(s):  
Pannala Padmaja ◽  
Garikapati Koteswara Rao ◽  
Adisherla Indrasena ◽  
Basireddy V. Subba Reddy ◽  
Nibedita Patel ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Cancer Cell Lines ◽  
Biological Evaluation ◽  
Tubulin Polymerization ◽  
Carbazole Derivatives ◽  
Synthesis And Biological Evaluation

A series of novel pyrano[3,2-c]carbazole derivatives have been synthesized and antiproliferative activity of the derivatives were investigated on various cancer cell lines.

scholarly journals Synthesis and biological evaluation of phosphatidylcholines with cinnamic and 3-methoxycinnamic acids with potent antiproliferative activity

RSC Advances ◽  
2018 ◽  
Vol 8 (62) ◽  
pp. 35744-35752 ◽  
Author(s):  
Marta Czarnecka ◽  
Marta Świtalska ◽  
Joanna Wietrzyk ◽  
Gabriela Maciejewska ◽  
Anna Gliszczyńska
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Cancer Cell Lines ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

A series of eight novel phosphatidylcholines containing CA or 3-OMe-CA acids (3a-b, 5a-b, 9a-b, 10a-b) at sn-1 and/or sn-2 positions were synthesized and tested for their antiproliferative activity against selected cancer cell lines.

scholarly journals Synthesis and Biological Evaluation of New Antitubulin Agents Containing 2-(3′,4′,5′-trimethoxyanilino)-3,6-disubstituted-4,5,6,7-tetrahydrothieno[2,3-c]pyridine Scaffold

Molecules ◽  
2020 ◽  
Vol 25 (7) ◽  
pp. 1690
Author(s):  
Romeo Romagnoli ◽  
Filippo Prencipe ◽  
Paola Oliva ◽  
Barbara Cacciari ◽  
Jan Balzarini ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Cell Death ◽  
Cell Lines ◽  
Cancer Cell ◽  
Mononuclear Cells ◽  
Cancer Cell Lines ◽  
Biological Evaluation ◽  
Pyridine Derivative ◽  
Tubulin Polymerization ◽  
Dependent Manner

Two novel series of compounds based on the 4,5,6,7-tetrahydrothieno[2,3-c]pyridine and 4,5,6,7-tetrahydrobenzo[b]thiophene molecular skeleton, characterized by the presence of a 3′,4′,5′-trimethoxyanilino moiety and a cyano or an alkoxycarbonyl group at its 2- or 3-position, respectively, were designed, synthesized, and evaluated for antiproliferative activity on a panel of cancer cell lines and for selected highly active compounds, inhibition of tubulin polymerization, and cell cycle effects. We have identified the 2-(3′,4′,5′-trimethoxyanilino)-3-cyano-6-methoxycarbonyl-4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivative 3a and its 6-ethoxycarbonyl homologue 3b as new antiproliferative agents that inhibit cancer cell growth with IC50 values ranging from 1.1 to 4.7 μM against a panel of three cancer cell lines. Their interaction with tubulin at micromolar levels leads to the accumulation of cells in the G2/M phase of the cell cycle and to an apoptotic cell death. The cell apoptosis study found that compounds 3a and 3b were very effective in the induction of apoptosis in a dose-dependent manner. These two derivatives did not induce cell death in normal human peripheral blood mononuclear cells, suggesting that they may be selective against cancer cells. Molecular docking studies confirmed that the inhibitory activity of these molecules on tubulin polymerization derived from binding to the colchicine site.

Pyrazole–oxadiazole conjugates: synthesis, antiproliferative activity and inhibition of tubulin polymerization

2014 ◽  
Vol 12 (40) ◽  
pp. 7993-8007 ◽  
Author(s):  
Ahmed Kamal ◽  
Anver Basha Shaik ◽  
Sowjanya Polepalli ◽  
Vangala Santosh Reddy ◽  
G. Bharath Kumar ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Tubulin Polymerization ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

A library of pyrazole–oxadiazole conjugates were synthesized and investigated for their antiproliferative activity in human cancer cell lines.

Synthesis and biological evaluation of bivalent β-carbolines as potential anticancer agents

MedChemComm ◽  
2016 ◽  
Vol 7 (4) ◽  
pp. 636-645 ◽  
Author(s):  
Hongtao Du ◽  
Hongling Gu ◽  
Na Li ◽  
Junru Wang
Keyword(s):  
Cell Cycle ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Cancer Cell Lines ◽  
Biological Evaluation ◽  
Apoptosis Induction ◽  
Synthesis And Biological Evaluation

A series of novel bivalent β-carbolines were synthesized and evaluated for their anti-proliferative activities on a panel of cancer cell lines, apoptosis induction and cell cycle effects.

Design, Synthesis and Biological Evaluation of 4, 6-Coumarin Derivatives as Anti-Cancer and Apoptosis-Inducing Agents

2021 ◽  
Vol 21 ◽  
Author(s):  
Guoyi Yan ◽  
Jiang Luo ◽  
Xuan Han ◽  
Wenjuan Zhang ◽  
Chunlan Pu ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Biological Evaluation ◽  
Cancer Drug ◽  
Dependent Manner ◽  
Coumarin Derivatives ◽  
In Silico Admet ◽  
Anti Cancer ◽  
Synthesis And Biological Evaluation

BACKGROUND: : Coumarin structures were widely employed in anti-cancer drug design. Herein we focused on the modifications of C4 and C6 positions on coumarin scaffold to get novel anti-cancer agents. OBJECTIVE: The objective of the current work was the synthesis and biological evaluation of a series of 4, 6-coumarin derivatives to get novel anticancer agents. METHODS: Thirty-seven coumarin derivatives were designed and synthesized, the antiproliferative activity of the compounds were evaluated against human cancer cell lines and non-cancerous cells by MTT assay. The bioactivities and underling mechanisms of active molecules were studied and the ADMET characters were predicted. RESULTS: Among the compounds, 4-phydroxy phenol-6-pinacol borane coumarin (25) exhibited a promising anti-cancer activity to cancer cell lines in dose-dependent manner and the toxicity to normal cells was low. The mechanism of action was observed through inducing G2/M phase arrest and apoptosis which was further confirmed via western blot. In silico ADMET prediction revealed that compound 25 is a drug-like small molecule with a favorable safety profile. CONCLUSION: The findings in this work may give vital information for further development of 6-pinacol borane coumarin derivatives as novel anti-cancer agents.

SAR study of tyrosine–chlorambucil hybrid regioisomers; synthesis and biological evaluation against breast cancer cell lines

Amino Acids ◽  
2011 ◽  
Vol 43 (2) ◽  
pp. 923-935 ◽  
Author(s):  
Caroline Descôteaux ◽  
Kevin Brasseur ◽  
Valérie Leblanc ◽  
Sophie Parent ◽  
Éric Asselin ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Cancer Cell Lines ◽  
Biological Evaluation ◽  
Breast Cancer Cell Lines ◽  
Sar Study ◽  
Synthesis And Biological Evaluation
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