Abstract:
A phenanthrene lactam derivative having the anticancer activity is provided to prevent and treat cancer and disease with excellent anticancer activity. A phenanthrene lactam derivative having chemical formula 1 is produced by reaction of the compound of chemical formula 2 and the compound of chemical formula 3 in a solution. R1, R2, R3, R4, R5, R6 and R7R is hydrogen, halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy or aryloxy. R4 and R5, R5 and R6, or R6 and R7 forms dioxol. R8 is the hydrogen or the C1-6 alkyl. The composite for preventing caner and pharmaceutical treatment comprises the phenanthrene lactam derivative of chemical formula 1 or pharmaceutically allowable salt.
Abstract:
Provided is a method for preparing an optically active alkyl 3-hydroxy butanoate derivative from a racemic beta-lactone derivative by using a specific lipase biocatalyst. A method for preparing an alkyl 3- hydroxy butanoate derivative with high optical activity comprises the following steps of reacting a beta-lactone derivative represented by the formula 1 to ROH to obtain a compound, represented by the formula 1, as a (S)-type optical activator and a compound, represented by the formula 3, as a (R)-type optical activator in the presence of a Candida Antarctica-derived lipase, Pseudomonas cepacia-derived lipase, Rhizomucor miehei-derived lipase, Burkholderia cepacia-derived amino PS lipase, amino lipase PS-CI, amino lipase PS-CII, amino lipase PS-DI, or a lipase-OF catalyst.
Abstract:
A pharmaceutical composition containing the triazole derivative having antifungal activity is provided to improve the antifungal activity against the various kinds of pathogens and reduce the toxicity as compared to the conventional antifungal agent, so that it is useful as the infection treatment agent of fungi. The pharmaceutical composition contains the triazole derivative having antifungal activity represented by the chemical formula(1) or the pharmaceutically acceptable salt, hydrate, solvate or isomer thereof, wherein n is 1 or 2; A indicates the direct coupling, C=O or CH2; and R is 5- to 10-membered monocyclic or bicyclic heteroaryl group containing 1 to 4 ring hetero atom independently selected from N, O and S.
Abstract:
본 발명은 p53 종양 억제단백질(tumor suppressor)과 제1 형광단백질의 융합단백질 및 제2 형광단백질을 발현하는 형질전환 세포주, 및 이를 이용하여 p53 종양 억제단백질의 활성에 관여하는 물질을 검색하는 방법에 관한 것으로, 구체적으로 5'에서 3' 방향으로 143번째 아미노산인 발린이 알라닌으로 치환된 비활성 p53 종양 억제단백질 돌연변이 유전자; 상기 유전자에 융합된 제1 형광단백질 유전자; IRES(internal ribosome entry site) 리보솜 결합 염기서열; 및 제2 형광단백질 유전자를 포함하고, 이들의 발현이 하나의 프로모터에 의해 조절되는 재조합 발현벡터; 상기 발현벡터가 안정적으로 도입된 형질전환 세포주; 및 상기 형질전환 세포주를 이용하여 p53 종양 억제단백질의 활성을 증가시키거나 억제하는 물질을 검색하는 방법에 관한 것이다. 본 발명에 따른 재조합 발현벡터 및 형질전환 세포주는 p53 종양 억제단백질의 활성과 관련된 물질을 검색하기 위한 바이오센서로서 항암제, 항암치료 보조제 및 퇴행성 질환 관련 치료제를 스크리닝하는데 유용하게 사용될 수 있다.
Abstract:
본 발명은 신규한 헤테로고리 화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 NAE(NEDD8-Activating Enzyme) 또는 SAE(Sumo Activating Enzyme) 관련 질환의 예방 또는 치료용 약학적 조성물에 관한 것으로, 본 발명에 따른 헤테로고리 화합물은 NAE(NEDD8-Activating Enzyme) 또는 SAE(Sumo Activating Enzyme)를 나노몰 단위의 농도로 우수하게 저해할 수 있어, 이를 유효성분으로 함유하는 NAE(NEDD8-Activating Enzyme) 또는 SAE(Sumo Activating Enzyme) 관련 질환 예를 들어, 암의 예방 또는 치료용 약학적 조성물로 유용하게 사용될 수 있다.
Abstract:
PURPOSE: An isoindolinone derivative and pharmaceutical composition containing the same are provided to enhance expression of alkaline phosphatase. CONSTITUTION: An insoindolinone derivative is denoted by chemical formula 1. A method for preparing the isoindolinone derivative comprises a step of amide-coupling phenylene diamine with a compound of chemical formula 8 to obtain an isoindolinone of chemical formula 2. In case of that one or more substituent R1-R4 in chemical formula 8 are halogen, the method further comprises a step of Suzuki-coupling boronic acid compound of chemical formula 17(RB(OH)_2) under the presence of palladium catalyst. A pharmaceutical composition for preventing or treating bone diseases contains the isoindolinone derivative of chemical formula 1 or pharmaceutically acceptable salt as an active ingredient.
Abstract:
A benzothiazole derivatives is provided to prevent the generation of drug resistance bacteria and improve the sterilization effect to plant late blight. A benzothiazole derivative is denoted by the chemical formula 1. In the chemical formula 1, X is H or C1-4 alkoxyl. The structure of Y is selected among structure formulas a, b, c, d, e, and f. The left side of Y is connected to N, the right side is connected to Z. R2 is H or C1-4 alkyl. Z is phenyl; phenyl which is substituted with one selected among halogen atom, cyano, methyl, nitro, phenyl, phenoxy, trifluoromethyl and hydroxyl, and isoxazole which is substituted with phenyl, chlorophenyl, or dichlorophenyl.