Synthesis of Scutellarein Derivatives with a Long Aliphatic Chain and Their Biological Evaluation against Human Cancer Cells

Five new meroterpenoids, zizhines P-S and U (1−4,7), together with two known meroterpenoids (5 and 6) were isolated from Ganoderma sinensis. Their structures including absolute configurations were assigned by using spectroscopic, computational, and chemical methods. Racemics zizhines P and Q were purified by HPLC on chiral phase. Biological evaluation found that 4, 5 and 6 are cytotoxic toward human cancer cells (A549, BGC-823, Kyse30) with IC50 values in the range of 63.43–80.83 μM towards A549, 59.2 ± 2.73 μM and 64.25 ± 0.37 μM towards BGC-823, 76.28 ± 1.93 μM and 85.42 ± 2.82 μM towards Kyse30.

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Synthesis and biological evaluation of novel artemisone–piperazine–tetronamide hybrids

RSC Advances ◽

10.1039/d1ra00750e ◽

2021 ◽

Vol 11 (30) ◽

pp. 18333-18341

Author(s):

Meng-Xue Wei ◽

Jia-Ying Yu ◽

Xin-Xin Liu ◽

Xue-Qiang Li ◽

Jin-Hui Yang ◽

...

Keyword(s):

Cancer Cells ◽

Human Cancer ◽

Biological Evaluation ◽

Human Cancer Cells ◽

Synthesis And Biological Evaluation

Six novel artemisone–piperazine–tetronamide hybrids were efficiently synthesised and investigated for their cytotoxicity against some human cancer cells.

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Design, synthesis and biological evaluation of novel carbamodithioates as anti-proliferative agents against human cancer cells

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2018.07.038 ◽

2018 ◽

Vol 157 ◽

pp. 1526-1540 ◽

Cited By ~ 1

Author(s):

Xia Liu ◽

Zhijun Wang ◽

Rui Xie ◽

Pingwah Tang ◽

Qipeng Yuan

Keyword(s):

Cancer Cells ◽

Human Cancer ◽

Biological Evaluation ◽

Design Synthesis ◽

Human Cancer Cells ◽

Synthesis And Biological Evaluation

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Unsymmetric dihydropyridines bearing 2-pyridyl methyl carboxylate as modulators of P-glycoprotein; synthesis and biological evaluation in resistant and non-resistant cancer cells

Canadian Journal of Chemistry ◽

10.1139/cjc-2018-0351 ◽

2019 ◽

Vol 97 (8) ◽

pp. 603-614

Author(s):

Maryam Nejati ◽

Hossein Sadeghpour ◽

Sara Ranjbar ◽

Katayoun Javidnia ◽

Najmeh Edraki ◽

...

Keyword(s):

Cancer Cells ◽

Human Cancer ◽

Binding Mode ◽

Biological Evaluation ◽

Multi Drug Resistance ◽

Glycoprotein P ◽

Glycoprotein Synthesis ◽

Human Cancer Cells ◽

P Glycoprotein ◽

Mdr Reversal

Multi-drug resistance (MDR) in cancer cells is often associated with overexpression of P-glycoprotein (P-gp or ABCB1 or MDR1); therefore, modulators of this transporter might be helpful in overcoming MDR. In this study, 16 novel unsymmetrical dihydropyridine (DHP) derivatives bearing 2-pyridyl methyl carboxylate at C3 and a nitroimidazole or nitrophenyl ring at C4 positions of the DHP ring were synthesized. Their cytotoxicity was tested against four human cancer cells by MTT assay. The reversal capacity of MDR was examined in P-gp overexpressing cells (MES-SA/DX5) by measuring the alteration of doxorubicin’s IC50 and performing flow cytometric determination of intracellular rhodamine 123 accumulation. The calcium channel blocking (CCB) activity, as a side effect of DHPs, was tested on the ileum of a guinea pig. Molecular docking was performed to explain the binding mode of compounds. Two derivatives, 4a and 4c, containing 4-nitrophenyl at C4 and possessing methyl (4a) and iso-propyl (4c) carboxylates at the C5 position of DHP core demonstrated superior cytotoxic and MDR reversal activities and lower CCB effect. Docking analysis confirmed the importance of the 4-nitrophenyl ring for P-gp inhibitory activity. Some of the synthesized DHP derivatives with considerable MDR reversal capacity could be promising compounds for further discovery of useful agents for management of drug resistant cancer.

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