Korea Research Institute of Bioscience and Biotechnology

Young-Soo Hong

Jeong-Hyung Lee

Jung Joon Lee

Hang-Sub Kim

Yun Joo Park

Kyeong Seok Lee

Hang Sub Kim

B K Shanthaveerappa

Jung-Joon Lee

Yinlan Jin

Bang-Yeon Hwang

Jin Hwan Kim

Xuejun Jin

Disclosed herein are an HIF-1 inhibitor, a method for the preparation thereof, and a pharmaceutical composition comprising the same as an active ingredient. The HIF-1 inhibitor shows anticancer activity thanks to the inhibition activity against HIF-1, a transcription factor which plays an important role in the growth and metastasis of cancer, but not to general cytotoxicity. Thus, the HIF-inhibitor and a pharmaceutically acceptable salt thereof can be used as a therapeutic for various cancers such as liver cancer; stomach cancer and breast cancer. Also, the compound having inhibition activity against HIF-1 is useful in the treatment of diabetic retinopathy and arthritis, which are aggravated by HIF-1-mediated VEGF expression.

Compounds that inhibit HIF-1 activity, the method for preparation thereof and the pharmaceutical composition containing them as an effective component

The disclosure concerns novel use of diterpene compound as a therapeutic agent of inlfammation, immune disease or cancer. More particularly, the present invention relates to novel use of diterpene compound that include kamebanin, kamebacetal A, kamebakaurin, and exisanin A, which would be effective for the treatment inflammation, immune disease or cancer by inhibiting the production of nitric oxide, prostaglandin, and TNF-through the suppression of NF-B activity.

Use of diterpene compound as a therapeutic agent of inflammation, immune disease or cancer

Disclosed are a novel compound represented by the following chemical formula (1), useful for the prophylaxis and treatment of angiogenic diseases, its production, and a novel microorganism producing the same. Aspergillus sp. Y80118 isolated from soil was found to produce 7,8-dihydro-1,7-dihydroxy-3-hydroxymethyl-xanthenone-8-carboxylic acid methylester which inhibits VEGF-induced proliferation of HUVEC, angiogenesis in CAM assay, and tumor growth. The novel compound can be effectively used for the medical treatment of anigiogenic diseases, including cancers, rheumatoid arthritis, and diabetic retinopathy.

7,8-dihydro-xanthenone-8-carboxylic acid derivative and novel microbe producing the same

The present invention relates to novel isocoumarin derivatves inhibiting angiogenesis, a method for preparation thereof and pharmaceutical compositions comprising the said derivatives as pharmaceutically active ingredients. More particularly, the present invention relates to novel isocoumarin derivatves represented by formula (1), especially 6,8-dihydroxy-4-acetyl-isocoumarin, a method for preparing 6,8-dihydroxy-4-acetyl-isocoumarin from fungi, and pharmaceutical compositions comprising the compounds and/or 6,8-dihydroxy-4-acetyl-isocoumarin as pharmaceutically active ingredients, which would be effective for the treatment of angiogenic diseases such as cancers, rheumatoid arthritis and diabetic retinopathy.

Isocoumarin derivatives inhibiting angiogenesis

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Taejon-si, South Korea

Young-Soo Hong