The Experts below are selected from a list of 162 Experts worldwide ranked by ideXlab platform
Monica Notarbartolo - One of the best experts on this subject based on the ideXlab platform.
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antitumor effects of curcumin and structurally β diketone modified analogs on multidrug resistant cancer cells
Bioorganic & Medicinal Chemistry Letters, 2008Co-Authors: Daniele Simoni, Michele Rizzi, Riccardo Rondanin, Riccardo Baruchello, Paolo Marchetti, Francesco Paolo Invidiata, Manuela Labbozzetta, Paola Poma, Valeria Carina, Monica NotarbartoloAbstract:Abstract Using concepts of bioisostery a series of curcumin analogs were synthesized: the diketonic system of the compound was elaborated into enaminones, Oximes, and the isoxazole heterocycle. The cell growth inhibitory and apoptosis inducing effects of the new analogs were evaluated by in vitro assays in the hepatocellular carcinoma HA22T/VGH cells, as well as in the MCF-7 breast cancer cell line and in its multidrug resistant (MDR) variant MCF-7R. Increased antitumor activity on all cell lines was found with the isoxazole analog and especially with the benzyl Oxime Derivative; in the HA22T/VGH cell model, the latter compound inhibited constitutive NF-κB activation.
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Antitumor effects of curcumin and structurally beta-diketone modified analogs on multidrug resistant cancer cells.
2008Co-Authors: Daniele Simoni, Michele Rizzi, Riccardo Rondanin, Riccardo Baruchello, Paolo Marchetti, Francesco Paolo Invidiata, Manuela Labbozzetta, Paola Poma, Valeria Carina, Monica NotarbartoloAbstract:Using concepts of bioisostery a series of curcumin analogs were synthesized: the diketonic system of the compound was elaborated into enaminones, Oximes, and the isoxazole heterocycle. The cell growth inhibitory and apoptosis inducing effects of the new analogs were evaluated by in vitro assays in the hepatocellular carcinoma HA22T/VGH cells, as well as in the MCF-7 breast cancer cell line and in its multidrug resistant (MDR) variant MCF-7R. Increased antitumor activity on all cell lines was found with the isoxazole analog and especially with the benzyl Oxime Derivative; in the HA22T/VGH cell model, the latter compound inhibited constitutive NF-kappaB activation
Carmen Navarroranninger - One of the best experts on this subject based on the ideXlab platform.
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trans platinum complexes design one novel water soluble Oxime Derivative that contains aliphatic amines in trans configuration
Journal of Inorganic Biochemistry, 2007Co-Authors: Adoracion G Quiroga, Leticia Cubo, Elena De Blas, Patricio Aller, Carmen NavarroranningerAbstract:In an attempt to design new antitumoral drugs based on transplatin complexes, we determined the experimental conditions for the preparation of trans-[Pt((CH(3))(2)CNOH)((CH(3))(2)CHNH(2))Cl(2)], and solved the crystal structure. The cytotoxicity of the novel complex, the cis counterpart, cisplatin, and a trans complex with aliphatic amines, as well as the capacity of some of these complexes to cause either apoptotic or necrotic cell death, was comparatively examined in NRK-52E rat renal tubular cells and HepG2 human hepatoma cells. The results indicate that the Oxime complex with trans geometry, but not the one with cis geometry, causes death by apoptosis, making the complex potentially suitable for therapeutic purposes. However cytotoxicity values are higher in the case of cis geometry than in trans geometry in both tumoral and non-tumoral cell lines.
Daniele Simoni - One of the best experts on this subject based on the ideXlab platform.
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antitumor effects of curcumin and structurally β diketone modified analogs on multidrug resistant cancer cells
Bioorganic & Medicinal Chemistry Letters, 2008Co-Authors: Daniele Simoni, Michele Rizzi, Riccardo Rondanin, Riccardo Baruchello, Paolo Marchetti, Francesco Paolo Invidiata, Manuela Labbozzetta, Paola Poma, Valeria Carina, Monica NotarbartoloAbstract:Abstract Using concepts of bioisostery a series of curcumin analogs were synthesized: the diketonic system of the compound was elaborated into enaminones, Oximes, and the isoxazole heterocycle. The cell growth inhibitory and apoptosis inducing effects of the new analogs were evaluated by in vitro assays in the hepatocellular carcinoma HA22T/VGH cells, as well as in the MCF-7 breast cancer cell line and in its multidrug resistant (MDR) variant MCF-7R. Increased antitumor activity on all cell lines was found with the isoxazole analog and especially with the benzyl Oxime Derivative; in the HA22T/VGH cell model, the latter compound inhibited constitutive NF-κB activation.
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Antitumor effects of curcumin and structurally beta-diketone modified analogs on multidrug resistant cancer cells.
2008Co-Authors: Daniele Simoni, Michele Rizzi, Riccardo Rondanin, Riccardo Baruchello, Paolo Marchetti, Francesco Paolo Invidiata, Manuela Labbozzetta, Paola Poma, Valeria Carina, Monica NotarbartoloAbstract:Using concepts of bioisostery a series of curcumin analogs were synthesized: the diketonic system of the compound was elaborated into enaminones, Oximes, and the isoxazole heterocycle. The cell growth inhibitory and apoptosis inducing effects of the new analogs were evaluated by in vitro assays in the hepatocellular carcinoma HA22T/VGH cells, as well as in the MCF-7 breast cancer cell line and in its multidrug resistant (MDR) variant MCF-7R. Increased antitumor activity on all cell lines was found with the isoxazole analog and especially with the benzyl Oxime Derivative; in the HA22T/VGH cell model, the latter compound inhibited constitutive NF-kappaB activation
Junghoon Yoon - One of the best experts on this subject based on the ideXlab platform.
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5 nitro 5 hydroxy indirubin 3 Oxime agm130 an indirubin 3 Oxime Derivative inhibits tumor growth by inducing apoptosis against non small cell lung cancer in vitro and in vivo
European Journal of Pharmaceutical Sciences, 2015Co-Authors: Meeyoung Ahn, Tae Hyung Kim, Seongmin Kwon, Hyoeun Yoon, Hyung Sik Kim, Jae Il Kim, Yongchul Kim, Keonwook Kang, Sanggun Ahn, Junghoon YoonAbstract:This study examined the anti-tumor effects of AGM130, a novel indirubin-3'-Oxime Derivative in A549 human non-small cell lung cancer cells. AGM130 significantly inhibited the proliferation and arrested the cell cycle of G2/M phase. Induction of apoptosis was detected in AGM130-treated A549 cells. The protein levels of Cytochrome c release, Bax, cleaved caspases and PARP were increased in AGM130 treated cells, whereas Bcl-2 levels were decreased. AGM130 inhibited Insulin-like growth factor 1 receptor (IGF1R), AKT/mTOR signaling and inactivated mitogen-activated protein kinases (MAPK). AGM130 also induced slight autophagy as pro-survival function and autophagy inhibition by chloroquine (CQ) induced necrosis. In vivo tumor xenograft model, AGM130 dose-dependently suppressed transplanted A549 cell tumor growth and induced the expression of proliferative cell nuclear antigen (PCNA). AGM130 also increased TUNEL positive apoptotic cell populations and the induction of glandular differentiation with mucin pool compared with vehicle-treated control in tumor tissue. These results suggest that AGM130 is an effective novel indirubin-3'-Oxime Derivative of anti-cancer drug and may be an attractive candidate for non-small cell lung cancer therapy.
Adoracion G Quiroga - One of the best experts on this subject based on the ideXlab platform.
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trans platinum complexes design one novel water soluble Oxime Derivative that contains aliphatic amines in trans configuration
Journal of Inorganic Biochemistry, 2007Co-Authors: Adoracion G Quiroga, Leticia Cubo, Elena De Blas, Patricio Aller, Carmen NavarroranningerAbstract:In an attempt to design new antitumoral drugs based on transplatin complexes, we determined the experimental conditions for the preparation of trans-[Pt((CH(3))(2)CNOH)((CH(3))(2)CHNH(2))Cl(2)], and solved the crystal structure. The cytotoxicity of the novel complex, the cis counterpart, cisplatin, and a trans complex with aliphatic amines, as well as the capacity of some of these complexes to cause either apoptotic or necrotic cell death, was comparatively examined in NRK-52E rat renal tubular cells and HepG2 human hepatoma cells. The results indicate that the Oxime complex with trans geometry, but not the one with cis geometry, causes death by apoptosis, making the complex potentially suitable for therapeutic purposes. However cytotoxicity values are higher in the case of cis geometry than in trans geometry in both tumoral and non-tumoral cell lines.
