• Title/Summary/Keyword: Antitumor agents

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Preparation of $\etha$-N-[(2-Chloroethyl) nitrosocarbamoyl]-L-lysine ($\etha$-N-[(2-Chloroethyl) nitrosocarbamoyl]-L-lysine의 합성)

  • 김정균;조인섭
    • YAKHAK HOEJI
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    • v.27 no.2
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    • pp.177-179
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    • 1983
  • A copper complex of $\epsilon$-N-[(2-chloroethyl)carbamoyl]-L-lysine was prepared by the treatment of the L-lysine copper complex with 2-chloroethyl isocyanate in cold water. Within the L-lysine copper complex molecule, the $\alpha-amino$ and carboxyl groups are bounded to $Cu^{2+}$ but the $\epsilon-amino$ group is free and can react with carbamoylating agents. A potential antitumor agent, $\epsilon-N-[(2-chloroethyl)$ nitrosocarbamoyl]-L-lysine was synthesized by nitrosation of this copper complex with Na $NO_{2}$ in anhydrous formic acid, followed by the passage of $H_{2}$S gas.

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Synthesis and In Vitro Cytotoxicity of 1,3-Dioxoindan-2-Carboxylic Acid Arylamides

  • Jung, Jae-Kyung;Ryu, Jin-Hyeong;Yang, Sung-Il;Cho, Jung-Sook;Lee , Hee-Soon
    • Archives of Pharmacal Research
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    • v.27 no.10
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    • pp.997-1000
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    • 2004
  • A series of 1,3-dioxoindan-2-carboxylic acid arylamides were synthesized and evaluated for in vitro cytotoxicity against four human cancer cell lines (HOP62, SK-OV-3, MD-MB-468 and T- 47D). The most active was compound 3e (1.2 ${\mu}M$ against SK-OV-3 cell line) bearing a 4- methyl substituent.

Stereoselective synthesis of novel 4′$\alpha$-C-methyl branched novel carbocyclic nucleosides

  • Kim, Ji-Hee;Ko, Ok-Hyun;Hong, Joon-Hee
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.345.2-345.2
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    • 2002
  • Recently. 4'${\alpha}$-C homologated furanose nucleosides. especially alkyl branches. are molecules of considerable current interest. One of reasons for this prominence arises from the notable biological activities as antiviral and antitumor agents. as shown in 4'${\alpha}$-C-methyl-2-deoxythymidine (EC$_{50}$ = 7.2$\mu$M against HIV in MT-4 cell), 4'${\alpha}$-C-fluoromethyl-2-deoxycytidine. 4'${\alpha}$-C-hydroxymethylthymidine and 4'${\alpha}$- -C-azidomethyl-thymidine. (omitted)omitted)

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Flexible docking of novel antitumor agents into human topoisomerase I-DNA complex with FlexiDock

  • Woo , Su-Na;Kim, Choon-Mi
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.314.2-314.2
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    • 2002
  • DNA topoisomerases catalyze changes in DNA topology through cycles of transient DNA strand breakage and religation. During this process. the active site tyrosine in human DNA topoisomerase Ⅰ(Top Ⅰ) becomes covalently linked to the 3'-ends of a single-stranded nick in the DNA duplex, Stabilization of the Top Ⅰ-DNA cleavable complex is the common initial event leading to the cytotoxicity of top 1 inhibitors. (omitted)

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Treatment of Rhus vernifciflua STOKES decoction to colorectal cancer patient (stage IV):single case report (옻나무 전탕추출물을 활용한 대장암 4기 환자치험 1례)

  • Kim, Bo-Geun;Park, Sang-Chae
    • Journal of Korean Traditional Oncology
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    • v.15 no.1
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    • pp.111-117
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    • 2010
  • Background & Objectives: Colorectal Cancer is 10% of all cancer incidence and the motality from colorectal cancer is nearly 450,000 a year. Since chemopreventive agents from Herbal medicine is hot issue recently, to prove antitumor effecicacy of Rhus vernifciflua STOKES decoction (Chijong-dan), clinical study was carried out. Here we report one patient with colorectal cancer of stage IV. The patient had a colorectal cancer (Stage IV, T4N2M1), lymph node metastases and underwent chemotherapy. Methods: The patient visited Hana oriental medicine Clinic in 2009 and was treated using Chijong-dan for 1 year at Hana Oriental Clinic. Results: Chijongdan showed no side effect during its treatment and tumor size was retarded based on CT scanning. Overall, this case report suggests that Rhus vernifciflua STOKES decoction can be a potent cancer preventive agents for colorectal cancer but it is still required to verify the scientific and clinical evidences for Rhus vernifciflua STOKES decoction (Chijong-dan).

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Structure-activity Relationship Study of Fluoro-Neplanocin A as Potential Antiviral and Antitumor Agents

  • Shin, Dae-Hong;Moon, Hyung-Ryong;Choi, Won-Jun;Lee, Kang-Man;Lee, Sang-Kook;Jeong, Lak-Shin
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.245.3-246
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    • 2003
  • S-Adenosylhomocysteine hydrolase (SAH) catalyzes the hydrolysis of S-adenosylhomocysteine to adenosine and L-homocysteine and has been an attractive target for the development of broad spectrum antiviral agents. Based on the potent inhibitory activity of neplanocin A against SAH, we have reported the synthesis and novel mechanism of action of fluoro-neplanocin A. (omitted)

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Natural Products Targeting Wnt/β-catenin Signaling Pathway

  • Kim, Donghwa;Lee, Sang Kook
    • Natural Product Sciences
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    • v.26 no.2
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    • pp.109-117
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    • 2020
  • The canonical Wnt/β-catenin signaling pathways play an important role in the embryonic development, cell proliferation, differentiation, and adhesion. Therefore, the abnormal activation and repression have been associated with uncontrolled homeostasis in human tissues. In particular, the activation of Wnt signaling is highly correlated with a diverse of diseases including cancer. On this regard, a strategy for targeting Wnt/β-catenin signaling has been employed in the discovery and development of antitumor agents. Herein, the evolution of Wnt signaling and the Wnt inhibitors derived from natural products were briefly summarized in the drug discovery of anticancer agents.

Ar-turmerone and $\beta-atlantone$ induce internucleosomal DNA fragmentation associated with programmed cell death in human myeloid leukemia HL-60 cells

  • Paek, Sang-Hyun;Kim, Geon-Joo;Han, Seung-Jeong;Yum, Sung-Kwan
    • Archives of Pharmacal Research
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    • v.19 no.2
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    • pp.91-94
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    • 1996
  • In the course of a search for antitumor agents, we found that the extract of Curcuma longa was effective in inducing apoptosis or programmed cell death (PCD) in human myeloid leukemia cells (HL-60). Active compounds for PCD were isolated from the hexanic extraction of the rhizome of Curcuma longa. With the several chromatographies, and spectral data, they were identified as ar-turmerone and $\beta-atlantone$. The present results demonstrate that the exposure of human myeloid leukemia HL-60 cells to clinically achievable concentrations of arturmerone (TU) or .$\beta-atlantone$(AT) produced internucleosomal DNA fragmentation of approximately 200 base-pair multiples, and the morphological changes characteristic of cells undergoing apoptosis or PCD. This findings suggest that these agents may exert their antitumoral activity, in part, through induction of apoptosis(PCD).

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Effect of ginseng and ginsenosides on melanogenesis and their mechanism of action

  • Kim, Kwangmi
    • Journal of Ginseng Research
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    • v.39 no.1
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    • pp.1-6
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    • 2015
  • Abnormal changes in skin color induce significant cosmetic problems and affect quality of life. There are two groups of abnormal change in skin color; hyperpigmentation and hypopigmentation. Hyperpigmentation, darkening skin color by excessive pigmentation, is a major concern for Asian people with yellowe-brown skin. A variety of hypopigmenting agents have been used, but treating the hyperpigmented condition is still challenging and the results are often discouraging. Panax ginseng has been used traditionally in eastern Asia to treat various diseases, due to its immunomodulatory, neuroprotective, antioxidative, and antitumor activities. Recently, several reports have shown that extract, powder, or some constituents of ginseng could inhibit melanogenesis in vivo or in vitro. The underlying mechanisms of antimelanogenic properties in ginseng or its components include the direct inhibition of key enzymes of melanogenesis, inhibition of transcription factors or signaling pathways involved in melanogenesis, decreasing production of inducers of melanogenesis, and enhancing production of antimelanogenic factor. Although there still remain some controversial issues surrounding the antimelanogenic activity of ginseng, especially in its effect on production of proinflammatory cytokines and nitric oxide, these recent findings suggest that ginseng and its constituents might be potential candidates for novel skin whitening agents.

Investigation of Antitumor Effects of Sorafenib and Lapatinib Alone and in Combination on MCF-7 Breast Cancer Cells

  • Kacan, Turgut;Altun, Ahmet;Altun, Gulsah Gultekin;Kacan, Selen Baloglu;Sarac, Bulent;Seker, Mehmet Metin;Bahceci, Aykut;Babacan, Nalan
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.7
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    • pp.3185-3189
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    • 2014
  • Background: Breast cancer evolution and tumor progression are controlled by complex interactions between steroid receptors and growth factor receptor signaling. Aberrant growth factor receptor signaling can augment or suppress estrogen receptor function in hormone-dependent breast cancer cells. Thus, we aimed to investigate antitumor effects of sorafenib and lapatinib alone and in combination on MCF-7 breast cancer cells. Materials and Methods: Cytotoxicity of the sorafenib and lapatinib was tested in MCF-7 cells by XTT assays. 50, 25, 12.5 and $6.25{\mu}M$ concentrations of sorafenib and 200, 100, 50 and $25{\mu}M$ concentrations of lapatinib were administered alone and in combination. Results were evaluated as absorbance at 450nM and $IC_{50}$ values are calculated according to the absorbance data Results: Both sorafenib and lapatinib showed concentration dependent cytotoxic effects on MCF-7 cells. Sorafenib exerted cytotoxic effects with an $IC_{50}$ value of $32.0{\mu}M$; in contrast with lapatinib the $IC_{50}$ was $136.6{\mu}M$. When sorafenib and lapatinib combined, lapatinib increased cytotoxic effects of sorafenib at its ineffective concentrations. Also at the concentrations where both drugs had cytotoxic effects, combination show strong anticancer effects and killed approximately 70 percent of breast cancer cells. Conclusions: Combinations of tyrosine kinase inhibitors and cytotoxic agents or molecular targeted therapy has been successful for many types of cancer. The present study shows that both sorafenib and lapatinib alone are effective in the treatment of breast cancer. Also a combination of these two agents may be a promising therapeutic option in treatment of breast cancer.