Synthesis, Characterization and Antitumor Activities of Cis-gallic acid[(1R,2R)-1,2-cyclohexanediamine] Platinum(II)

2012 ◽  
Vol 554-556 ◽  
pp. 1645-1649 ◽  
Author(s):  
Qing Kun Wang ◽  
Shao Ping Pu ◽  
Yong Nian Li ◽  
Jian He ◽  
Li Min Zhou ◽  
...  

Abstract. In order to obtain a gallic acid platinum complex, the title compound was synthesed from potassium tetrachloroplatinate by the reaction potassium iodide, (1R,2R)-1,2-cyclohexanediamine, silver nitrate and gallic acid respectively. The complex structure and component were characterized by elemental analysis, ESI-MS, 1H-NMR and IR and the anticancer activity was measured by MTT method. The result showed that its structure was consistent with the title compound and had inhibiting effect on the growth of tumor cell lines in vitro.

2012 ◽  
Vol 581-582 ◽  
pp. 210-213
Author(s):  
Qing Kun Wang ◽  
Shao Ping Pu ◽  
Yong Nian Li ◽  
Jian He ◽  
Li Min Zhou ◽  
...  

In order to obtain a gallic acid platinum complex, the title compound was synthesed from cis-[Pt(Cyclohexylamine)]2I2 by the reaction with NH3, silver nitrate and gallic acid respectively. The complex structure and component were characterized by elemental analysis, ESI-MS, 1H-NMR and IR and the anticancer activity was measured by MTT method. The result showed that its structure was consistent with the title compound and had inhibiting effect on the growth of tumor cell lines in vitro.


2014 ◽  
Vol 884-885 ◽  
pp. 593-597
Author(s):  
Jian He ◽  
Qing Kun Wang ◽  
Xue Jie Li ◽  
Shao Ping Pu

Abstract. In order to obtain a chlorogenic acid platinum complex, The intermediate Pt(C6H14N2)(H2O)2(NO3)2 solution was synthesized from Pt(C6H14N2)I2 and AgNO3, and it was treated with the anion exchange resin to give the key intermediate Pt(C6H14N2)(OH)2. The key intermediate was subsequently reacted with chlorogenic acid in butyl alcohol. The complex structure and component were characterized by elemental analysis, ESI-MS, 1H-NMR and IR and the anticancer activity was measured by MTT method. The result showed that its structure was consistent with the title compound and had inhibiting effect on the growth of tumor cell lines in vitro.


2013 ◽  
Vol 803 ◽  
pp. 145-148 ◽  
Author(s):  
Qing Kun Wang ◽  
Shao Ping Pu ◽  
Yong Nian Li ◽  
Jian He ◽  
Jie Jin ◽  
...  

In order to obtain the mixed isobutylamine /cyclopentylamine platinum complexes with chloride and oxalic acid ions as leaving groups. The title compounds were synthetised from potassiumtetrachloroplatinate(II) by the reaction with potassium iodide, cyclopentylamine, isobutylamine, silver nitrate, potassium chloride, potassium oxalate monohydrate. The complexes structure and component were characterized by elemental analysis, ESI-MS, 1H-NMR and IR and the anticancer activity were measured by MTT method. The results showed that its structure was consistent with the title compound and had inhibiting effect on the growth of tumor cell lines in vitro.


2008 ◽  
Vol 63 (1) ◽  
pp. 83-89 ◽  
Author(s):  
Yaseen A. Al-Soud ◽  
Haitham H. Al-Sa’doni ◽  
Houssain A. S. Amajaour ◽  
Kifah S. M. Salih ◽  
Mohammad S. Mubarakb ◽  
...  

A new series of coumarin and benzofuran derivatives were synthesized as potential non-nucleoside reverse transcriptase inhibitors (NNRTIs) by reacting, separately, 4-bromomethylcoumarins, their sulphonyl chlorides, and ethyl 3-(bromomethyl)-6-methoxy-1-benzofuran-2-carboxylate with different imidazoles and their benzo analogs. The antiviral (HIV-1, HIV-2) properties of the newly synthesized compounds were investigated in vitro and all compounds were found to be inactive, except 10 which showed inhibition of HIV-2 with EC50 > 0.51 μgmL−1. The in vitro cytotoxicity of 17 and 19 was assayed against a panel of tumor cell lines consisting of CD4 human T-cells.


2019 ◽  
Vol 43 (9-10) ◽  
pp. 437-442 ◽  
Author(s):  
Shou De Xu ◽  
Xiang Hua Wu

A series of bimetallic dppfM(II) (dppf = 1,1’-bis (diphenyphosphino) ferrocene; M = Pt and Pd) dithiocarbamate complexes is synthesized and characterized by spectroscopic methods and single-crystal X-ray diffraction. Their antitumor activities in vitro are investigated by MTT assays against four cancer cell lines. The anticancer studies indicate most of the complexes display good to excellent antitumor activity. Remarkably, the platinum complex with a pyrrolidinyl substituent (3b) was identified as the most promising candidate due to its high potency and broad spectrum of activity.


2013 ◽  
Vol 78 (9) ◽  
pp. 1301-1308 ◽  
Author(s):  
Lin Luo ◽  
Jiang-Ke Qin ◽  
Zhi-Kai Dai ◽  
Shi-Hua Gao

Nine novel aminoalkoxy substituted benzoxanthones (3a-3i) were synthesized. Their antitumor activities were evaluated in five human solid tumor cell lines including Hep-G2, BEL-7402, HeLa, MGC-803 and CNE by MTT method. The results showed that most of the compounds displayed moderate to good inhibitory activities on the tested cancer cell lines in vitro, among them compounds 3a and 3h showed higher antitumor activity than other tested compounds against most cell lines. The influence of two kinds of structural factors including the terminal amino group and length of carbon spacers on the anticancer activities were explored to discuss the preliminary structure-activity relationships.


2010 ◽  
Vol 5 (10) ◽  
pp. 1934578X1000501
Author(s):  
Ning Li ◽  
Wan Xiao ◽  
Bailing Hou ◽  
Xian Li

Two new cycloartane glycosides were isolated from the whole herbs of Camptosorus sibiricus Rupr. By means of chemical and spectroscopic methods (1D and 2D NMR, HRMS, ESIMS), the structures were established as (24 R)-3β,7β,24,25,30-pentahydroxycycloartane-30- O-coumaroyl-3- O-β-D-glucopyranosyl-24- O-β-D-glucopyranosyl-(1→6)-β-D-glucopyranoside (1) and (24 R)-3β,7β,24,25,30-pentahydroxy-1-ene-cycloartane 24- O-β-D-glucopyranoside (2). The two new compounds were inactive in vitro against A375-S2 and Hela human tumor cell lines using the MTT method.


2008 ◽  
Vol 3 (6) ◽  
pp. 1934578X0800300
Author(s):  
Peng Zhang ◽  
Yiyu Cheng ◽  
Zhongjun Ma

Two new cycloartane glycosides were isolated from the whole herbs of Camptosorus sibiricus Rupr.. By means of chemical and spectroscopic methods (IR, 1D- and 2D- NMR, HRMS, ESI-MS), the structures were established as (24 R)-3β,7β,24,25,30-pentahydroxycycloartane 3- O-β-D-glucopyranosyl-24- O-β-D-glucopyranosyl-30- O-β-D-glucopyranoside (1), and (24 R)-3β,7β,24,25,30-pentahydroxycycloartane 3- O-β-D-glucopyranosyl-(1→2)-β-D-glucopyranosyl-24- O-β-D-xylopyranosyl-(1→2)-β-D-glucopyranoside (2). The two new compounds were tested for their cytotoxicity in vitro against human tumor cell lines (A375-S2, Hela) using the MTT method, but both compounds were inactive.


2020 ◽  
Vol 17 (5) ◽  
pp. 520-525
Author(s):  
Rui Cai ◽  
Li Zhu ◽  
Pengfei Wang ◽  
Yu Zhao

Background: Natural occurring β-Carbolines alkaloids are abundant in the plant kingdom or other organisms, and they were found to possess good antitumor activity through multiple mechanisms. Based on previous summarized SARs of β-carboline derivatives, the modification on pyridine ring would have a great impact on their antitumor activities. Therefore, we plan to synthesized arylated β-carboline-3-amides to find more valuable β-Carbolines derivatives. Methods: A novel bimetallic Pd(OAc)2/AgOAc catalyst system was developed for the amidation of aryl iodides under acid condition. A series of N-arylated β-carbolines derivatives were synthesized using this method. The structures of these compounds were confirmed by 1H NMR, 13C NMR and HRMS, and their in vitro antiproliferative activity was investigated against HepG2 and Hela tumor cell lines by MTT assay. Results: Eleven N-arylated β-carboline-3-amides were synthesized using this bimetallic catalyzed method in 58-98% yields. These synthesized N-arylated compounds showed no antiproliferative activity at 20 μM. Conclusion: We have discovered an efficient and bimetallic catalytic system allowing the Narylation of secondary acyclic amides. This is the first report that N-arylation of aliphatic secondary acyclic amides under acid condition.


2013 ◽  
Vol 634-638 ◽  
pp. 922-925
Author(s):  
Zhao Yang ◽  
Zhi Xiang Wang ◽  
Zheng Fang ◽  
Kai Guo

Sixteen 3-arylurea-5-fluoroindolin-2-one derivatives were designed according to the principle of fragment based drug discovery and synthesized with 5-fluoroisatin as the starting material. The obtained structures were identified by 1H NMR, MS and elemental analysis. In vitro evaluation of antitumor bioactivity was performed by MTT method. Most of synthesized compounds showed antitumor activities, especially, activities of 6a, 6h, and 6j in tumor inhibition were better than others.


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