Design, Synthesis and Biological Evaluation of C-8 Modified Curcumol Derivatives as Potential Anticancer Agents

Abstract A series of structural modification of curcumol derivatives at C-8 position were designed and synthesized, which structures were confirmed by 1H NMR,13C NMR and HRMS analysis. The tested compounds were evaluated for in vitro antitumor activity against colorectal cancer cell lines SW620, HCT116 and CaCo2. Many of the tested candidates exhibited higher inhibition efficiency than curcumol. Among them, compound 3l shows the best inhibitory effect on the viability of SW620 with IC50 value of 19.90 mM. The structure-activity relationships (SARs) of these derivatives were discussed, which showed that the introduction of amino or aryl groups tended to increase the anti-cancer activity. In addition, compound 3l may inhibit cancer cell proliferation through triggering cell apoptosis.

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Design, synthesis, and biological evaluation of new series of 2-amido-1,3,4-thiadiazole derivatives as cytotoxic agents

Zeitschrift für Naturforschung B ◽

10.1515/znb-2015-0138 ◽

2016 ◽

Vol 71 (3) ◽

pp. 205-210 ◽

Cited By ~ 3

Author(s):

Ali Almasirad ◽

Loghman Firoozpour ◽

Maliheh Nejati ◽

Najmeh Edraki ◽

Omidreza Firuzi ◽

...

Keyword(s):

Human Tumor ◽

Inhibitory Effect ◽

Biological Evaluation ◽

Cytotoxic Agents ◽

Antitumor Activities ◽

Design Synthesis ◽

Ethidium Bromide Staining ◽

Thiadiazole Derivatives ◽

Synthesis And Biological Evaluation

AbstractA series of novel 1,3,4-thiadiazole derivatives bearing an amide moiety were designed, synthesized, and evaluated for their in vitro antitumor activities against HL-60, SKOV-3 and MOLT-4 human tumor cell lines by MTT assay. Ethyl 2-((5-(4-methoxybenzamido)-1,3,4-thiadiazol-2-yl)thio)acetate (5f) showed the best inhibitory effect against SKOV-3 cells, with an IC50 value of 19.5 μm. In addition, the acridine orange/ethidium bromide staining assay in SKOV-3 cells suggested that the cytotoxic activity of 5f occurs via apoptosis.

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Design, synthesis, and biological evaluation of novel benzodiazepine derivatives as anticancer agents through inhibition of tubulin polymerization in vitro and in vivo

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2019.111670 ◽

2019 ◽

Vol 182 ◽

pp. 111670 ◽

Cited By ~ 2

Author(s):

Yanqing Pang ◽

Haibiao Lin ◽

Caiwen Ou ◽

Yingying Cao ◽

Baijiao An ◽

...

Keyword(s):

Anticancer Agents ◽

Biological Evaluation ◽

Tubulin Polymerization ◽

Design Synthesis ◽

Benzodiazepine Derivatives ◽

Synthesis And Biological Evaluation

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Design, synthesis and biological evaluation of rhein derivatives as anticancer agents

MedChemComm ◽

10.1039/c6md00252h ◽

2016 ◽

Vol 7 (9) ◽

pp. 1812-1818 ◽

Cited By ~ 3

Author(s):

Junkai Huang ◽

Zhuo Zhang ◽

Peng Huang ◽

Liqin He ◽

Yong Ling

Keyword(s):

Tumor Cell ◽

Anticancer Agents ◽

Biological Evaluation ◽

Tumor Cell Lines ◽

Promising Candidate ◽

Design Synthesis ◽

Anti Tumor Activity ◽

Synthesis And Biological Evaluation ◽

Derivatives Of

A series of novel derivatives of rhein were synthesized and evaluated for their in vitro antiproliferative activity against six kinds of tumor cell lines. All derivatives displayed more potent anti-tumor activity than rhein, and most of them were even stronger than 5-FU. Compound 4v was the most promising candidate among the investigated compounds.

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Design, Synthesis and Biological Evaluation of Sunitinib Analogues to Improve Aqueous Solubility

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.749.350 ◽

2013 ◽

Vol 749 ◽

pp. 350-353 ◽

Cited By ~ 1

Author(s):

Ke Tao Chen ◽

Zheng Fang ◽

Zhao Yang ◽

Kai Guo

Keyword(s):

Aqueous Solubility ◽

Positive Control ◽

Biological Evaluation ◽

Antitumor Activities ◽

Design Synthesis ◽

H Nmr ◽

Mtt Method ◽

Antitumor Bioactivity ◽

Synthesis And Biological Evaluation

In order to improve aqueous solubility of Sunitinib, based on the structure-activity relationship, four analogues were designed and synthesized. The obtained structures were identified by1H NMR, MS and elemental analysis.In vitroevaluation of antitumor bioactivity was performed by MTT method. All of synthesized compounds showed antitumor activities, especially, compounds A1, which were better than or equal to the antitumor activity of positive control.

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