Antiproliferative Activity and Mechanism of Action of Fatty Acid Derivatives of Gemcitabine in Leukemia and Solid Tumor Cell Lines and in Human Xenografts

ChemInform ◽  
2005 ◽  
Vol 36 (10) ◽  
Author(s):  
A. M. Bergman ◽  
et al. et al.
ChemInform ◽  
2005 ◽  
Vol 36 (12) ◽  
Author(s):  
A. M. Bergmann ◽  
C. M. Kuiper ◽  
F. Myhren ◽  
M. L. Sandvold ◽  
H. R. Hendriks ◽  
...  

2010 ◽  
Vol 20 (5) ◽  
pp. 1504-1506 ◽  
Author(s):  
Simonas Rudys ◽  
Carla Ríos-Luci ◽  
Eduardo Pérez-Roth ◽  
Inga Cikotiene ◽  
José M. Padrón

2021 ◽  
Author(s):  
Exequiel O. J. Porta ◽  
María Sol Ballari ◽  
José M. Padrón ◽  
Guillermo R. Labadie

Aim: We proposed to determine the antiproliferative activity of a series of synthetic salirasib analogs, presenting or not a 1,2,3-triazole linker, against five different cancer cell lines. Results: Bioassay, cheminformatic, and in silico ADME-Tox allowed the identification of new potent analogs. SAR analysis allowed the identification of structural and physicochemical features that benefit the antiproliferative activity. Conclusion: Isoprenyl R chains with three or more isoprene units, or long aliphatic R chains are the preferred ones within the active compounds. Likewise, we have identified three compounds with better activity profiles than salirasib against all the cell lines tested.


2007 ◽  
Vol 17 (10) ◽  
pp. 2681-2684 ◽  
Author(s):  
Leticia G. León ◽  
Rubén M. Carballo ◽  
María C. Vega-Hernández ◽  
Víctor S. Martín ◽  
Juan I. Padrón ◽  
...  

2007 ◽  
Vol 85 (11) ◽  
pp. 938-944 ◽  
Author(s):  
Liping Deng ◽  
Li Shen ◽  
Jing Zhang ◽  
Bo Yang ◽  
Qiaojun He ◽  
...  

A series of norcantharidin (NCTD) analogues have been synthesized by [3+2]1,3-dipolar cycloaddition reaction of norcantharidin derivatives of substituted aromatic amines with four nitrile oximes. All analogues have been screened for their antiproliferative activity in vitro against a panel of tumor cell lines: KB, SGC-7901, HL60, Bel-7402, HO-8910, and ECA109, producing IC50 values from 0.36 µmol/L to >100 µmol/L. Compound 9d showed potency for the treatment of hepatoma, with IC50 value to Bel-7402 cell line comparable to that of norcantharidin.Key words: norcantharidin analogues, isoxazoline, growth inhibition.


MedChemComm ◽  
2015 ◽  
Vol 6 (2) ◽  
pp. 334-338 ◽  
Author(s):  
Peng Huang ◽  
Zhong Hu ◽  
Liqin He ◽  
Xiaoshan Wang ◽  
Yaxian Wu

A series of novel derivatives of gambogenic acid (GNA) were synthesized and evaluated for their in vitro antiproliferative activity against four kinds of tumor cell lines. These compounds displayed potent antiproliferative activity. In particular, compound 3f exhibited superior antiproliferative activity against these tumor cell lines than GNA.


ChemInform ◽  
2010 ◽  
Vol 41 (30) ◽  
pp. no-no
Author(s):  
Simonas Rudys ◽  
Carla Rios-Luci ◽  
Eduardo Perez-Roth ◽  
Inga Cikotiene ◽  
Jose M. Padron

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