• 제목/요약/키워드: sorafenib

검색결과 55건 처리시간 0.024초

새로운 Aminoisoquinolinylamide 유도체의 합성 및 흑색종 저해 효능 (Synthesis and Melanoma Inhibitory Activity of New Aminoisoquinolinylamide Derivatives)

  • 유경호;조혜정
    • 한국응용과학기술학회지
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    • 제26권2호
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    • pp.161-170
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    • 2009
  • In this work, a novel series of aminoisoquinolinylamide derivatives 1a-c and 2a-f were synthesized via several reaction steps, starting from 2-methyl-4-nitrobenzonitrile (3) and 1-chloro-5-nitroquinoline (8). And their antiproliferative activities were screened against A375 human melanoma cell line compared to Sorafenib as a reference compound. Among them, compound 1b and 1c exhibited meaningful inhibitory activities. These results demonstrated that aminoisoquinolinylamide scaffold possesses the possibility as the treatment for melanoma.

Quinazolinylmethoxybenzene 유도체 합성 및 흑색종 세포증식 저해효능 (Synthesis and Antiproliferative Activity of Quinazolinylmethoxybenzene Derivatives against Melanoma Cell Line)

  • 이준상;유경호
    • 한국응용과학기술학회지
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    • 제27권1호
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    • pp.20-28
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    • 2010
  • Melanoma is the most aggressive form of skin cancer and is the fastest growing type of cancer in the United States. We report here the synthesis of a novel series of quinazolinylmethoxybenzene derivatives 1a-c and their antiproliferative activities against A375 human melanoma cell line. Among them, urea compound 1a ($IC_{50}\;=\;4.8\;{\mu}M$) having 4-chloro-3-trifluoromethylphenyl moiety showed superior antiproliferative activity to Sorafenib ($IC_{50}\;=\;5.5\;{\mu}M$) as a reference compound. These results will helpful for designing structure of a therapeutic agent for the treatment of melanoma.

A patient who has survived for a long period with repeated radiotherapies for multifocal extrahepatic metastases from hepatocellular carcinoma

  • Jo, Sunmi;Shim, Hye Kyung
    • Radiation Oncology Journal
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    • 제31권4호
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    • pp.267-272
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    • 2013
  • Although significant advances in the treatment of intrahepatic lesions, it is reported that the prognosis for patients with hepatocellular carcinoma (HCC) who have extrahepatic metastasis remains poor. We report a patient with lung, liver, brain, bone and subcutaneous metastasis from HCC who has survived more than 7 years maintaining relatively good performance status as a result of repeated therapies. A 55-year-old male patient with HCC underwent right lobectomy of the liver and cholecystectomy in September 2006. He received wedge resection for lung metastasis twice (July 2009, January 2011) and Gamma Knife stereotactic radiosurgery for brain metastasis (April 2011). Over the last 3 years, he has developed metastasis in subcutaneous tissues, muscle, and bone with pain. He has undergone 7 courses of radiotherapies for subcutaneous tissues, muscle, and bone metastasis and been prescribed sorafenib and he is still capable of all self-care.

흑색종 세포증식 저해효능의 새로운 Benzaminoquinoline 유도체의 합성 (Synthesis of New Benzaminoquinoline Derivatives with Antiproliferative Activity against Melanoma Cell Line)

  • 유경호;남봉수
    • 한국응용과학기술학회지
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    • 제26권3호
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    • pp.297-305
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    • 2009
  • Melanoma is the most serious type of skin cancer as a malignant tumor of melanocytes. In this work, the syntheses of a novel series of benzaminoquinoline derivatives 1a-c and their antiproliferative activities against A375 human melanoma cell line were described. All the compounds ($IC_{50}=0.78-1.02{\mu}M$) showed superior antiproliferative activities to Sorafenib ($IC_{50}=5.58{\mu}M$) as a reference compound. These results suggested that benzaminoquinoline derivatives have potentials as a therapeutic agent for the treatment for melanoma.

Synthesis and Antiproliferative Activity of New Aminoisoquinolinylurea Derivatives against Melanoma Cell Line

  • Cho, Hye Jung;El-Gamal, Mohammed I.;Oh, Chang-Hyun;Lee, So Ha;Kim, Garam;Hong, Jun Hee;Choi, Hong Seok;Yoo, Kyung Ho
    • Bulletin of the Korean Chemical Society
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    • 제33권11호
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    • pp.3635-3639
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    • 2012
  • A series of new diarylureas possessing aminoisoquinoline scaffold was synthesized, and their in vitro antiproliferative activity against A375P human melanoma cell line was tested. Compounds 1d, 1l, 1n, 1p, 1q, and 1t showed superior potency against A375P to Sorafenib. The highest potency was shown by compound 1p possessing 3,5-bis(trifluoromethyl)phenyl terminal ring with $IC_{50}$ value of $0.41{\mu}M$.

Synthesis of New Pyrimidinylaminobenzene Derivatives and Their Antiproliferative Activities against Melanoma Cell Line

  • Kim, Hee Jin;Oh, Chang-Hyun;Yoo, Kyung Ho
    • Bulletin of the Korean Chemical Society
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    • 제34권8호
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    • pp.2311-2316
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    • 2013
  • A series of new diarylamide and diarylurea derivatives possessing pyrimidinylaminobenzene scaffold was synthesized. Their in vitro antiproliferative activities were tested against A375P human melanoma cell line. Among them, compounds 1a-c, k and 2b-d, f, g, j, l showed superior potencies against A375P human melanoma cell line to Sorafenib. In particular, compound 2f possessing 3-fluoro-5-trifluoromethyl moiety exhibited the highest potency with $IC_{50}$ value in nanomolar scale.

예후가 좋지 않은 갑상선암에 대한 최신 치료 방침 (Recent Improvements in the Treatment of High-Risk Thyroid Cancer)

  • 이은경
    • 대한두경부종양학회지
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    • 제38권1호
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    • pp.1-9
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    • 2022
  • Thyroid cancer is one of the slow-growing tumors with excellent oncological outcomes. However, a small set of patients with unexpectedly severe outcomes are usually ignored. Anaplastic thyroid cancer (ATC) remains one of the most aggressive and lethal solid tumors. Recently, dabrafenib and trametinib combination therapy or neoadjuvant BRAF induction therapy has shown promising results. In addition, a combination of targeted drugs, immunotherapy, surgery, and radiation therapy can improve overall survival in ATC patients. Another disease for which there is no breakthrough treatment is radioactive iodine-refractory differentiated thyroid cancer (DTC). To date, multikinase inhibitors (sorafenib, lenvatinib) targeting the growth factor signaling pathway have been developed and approved as anticancer agents for patients with advanced DTC. This review includes results from multikinase inhibitors to the emergence of new target molecules, including rearrangements during transformation (RET) and tropomyosin receptor kinase (TRK).

Synthesis and Antiproliferative Activity of Pyridinylcarbonylpyrimidines Against Melanoma Cell Line

  • Ahn, Hye-Mi;Lee, Jun-A;Kim, Hwan;Oh, Chang-Hyun;Lee, So-Ha;Sim, Tae-Bo;Hah, Jung-Mi;Kim, Dong-Jin;Yoo, Kyung-Ho
    • Bulletin of the Korean Chemical Society
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    • 제32권4호
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    • pp.1209-1214
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    • 2011
  • The synthesis of the series of pyrimidinylamines 1a-d and pyrimidinylureas 1e-u bearing a novel pyridinylcarbonylpyrimidine scaffold and their antiproliferative activities against A375 human melanoma cell line were described. Among them, three compounds 1e, 1h, and 1o showed superior antiproliferative activities to Sorafenib ($IC_{50}=5.5{\mu}M$) as a reference compound. In our series, urea compound 1o having 4-chloro-3-trifluoromethyl moiety on the benzene nucleus exhibited very good antiproliferative activity with $IC_{50}$ value of $1.4{\mu}M$.

Clinicopathological Characteristics of Hepatocellular Carcinoma in Turkey

  • Dogan, Erkan;Yalcin, Suayib;Koca, Dogan;Olmez, Aydemir
    • Asian Pacific Journal of Cancer Prevention
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    • 제13권6호
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    • pp.2985-2990
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    • 2012
  • Background: Hepatocellular carcinoma (HCC), the main malignant tumor of the liver, is very common and highly lethal. The aim of this study was to determine its clinicopathologic characteristics and risk factors in Turkey. Materials and methods: In this study, patients who were diagnosed as suffering from HCC in the period between August 2004 and December 2011 were evaluated retrospectively. Results: A total of 98 patients were included, with a median age 61 (range: 16 to 82). Seventy nine (80.6%) were male 59 (60.2%) were infected with hepatitis B virus (HBV) and 15 (15.3%) with HCV, another 15 (15.3%) being alcohol abusers. Seventy two (73.5%) were at advanced stage and 54 (55.1%) had elevated serum alpha-fetoprotein (AFP). Surgery, chemoembolization, systemic chemotherapy and application of the tyrosine kinase inhibitor sorafenib were the major treatment options. Conclusions: According to our findings HCC is mostly diagnosed in advanced stage and age, being five times more common in males than females. Main risk factors of HCC are HBV infection, HCV infection and alcohol abuse. Elevation in AFP may facilitate early diagnosis of HCC in high risk groups.

Complete cure of advanced hepatocellular carcinoma with right adrenal gland metastasis and portal vein thrombosis by multiple applications of an interdisciplinary therapy: Case report with 8-year follow up

  • Jung, Hojung;Kim, Byung Ik;Cho, Yong Kyun;Jeon, Woo Kyu;Kim, Hong Joo;Hong, Hyun Pyo
    • 대한간학회지
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    • 제24권4호
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    • pp.424-429
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    • 2018
  • Hepatocellular carcinoma (HCC) is the sixth most common cause of death worldwide and the main cause of primary liver cancer. The principle problem of HCC is the poor prognosis, since advanced HCC reportedly has a median survival of only 9 months. The standard therapies are sorafenib and regorafenib, but the outcomes remain unclear. We report a 60-year-old man with advanced HCC with right adrenal gland metastasis and portal vein tumor thrombosis, who showed a complete response to multiple applications of an interdisciplinary therapy.