Abstract:
본 발명은, 친수성인 폴리에틸렌글리콜과 스페이서(spacer) 그룹으로 라이신, 라이신을 포함하는 올리고펩타이드, 아미노에탄올, 아미노프로판올, 아미노부탄올, 아미노펜탄올 및 아미노헥산올로 이루어진 군으로부터 선택된 1종을 도입한 양이온성 선형 폴리포스파젠 화합물, 상기 화합물에 소수성 약물을 화학적으로 결합시킨 폴리포스파젠-약물 컨쥬게이트 화합물 및 이의 제조방법에 관한 것으로, 본 발명의 화합물은 암 조직 선택성이 탁월하고 독성이 아주 낮아 항암제로 실용화 가능성이 높은 신물질이다.
Abstract:
본 발명은, 친수성인 폴리에틸렌글리콜과 스페이서(spacer) 그룹으로 라이신, 라이신을 포함하는 올리고펩타이드, 아미노에탄올, 아미노프로판올, 아미노부탄올, 아미노펜탄올 및 아미노헥산올로 이루어진 군으로부터 선택된 1종을 도입한 양이온성 선형 폴리포스파젠 화합물, 상기 화합물에 소수성 약물을 화학적으로 결합시킨 폴리포스파젠-약물 컨쥬게이트 화합물 및 이의 제조방법에 관한 것으로, 본 발명의 화합물은 암 조직 선택성이 탁월하고 독성이 아주 낮아 항암제로 실용화 가능성이 높은 신물질이다.
Abstract:
본발명에따른화합물은매우낮은농도 2 w/w% 미만에서도경력한수화겔을형성할수 있다. 또한, 그로부터제조된수화겔은생분해성및 온도감응성을가지고, 제조가간편하며, 단백질을불활성화시키지않고, 약물의다량방출효과없이서방성을나타내므로, 약물, 특히단백질약물의서방성전달을위한약물전달체로서유용하게사용될수 있다.
Abstract:
A cyclotriphosphazene-platinum(II) conjugate is provided to show high selectivity on a cancer tissue and excellent anticancer effect due to excellent permeation-retention property effect on the cancer tissue. A cyclotriphosphazene-platinum(II) conjugate is represented by the formula(1), where n is 7, 12 or 16; m is 0, 1 or 2; x is 1; each y and z is respectively 0 or 1; and each R, R' and R' is respectively selected from the group consisting of (CH3)2CH-, (CH3)2CHCH2-, (C2H5)(CH3)CH- and (C6H5)CH2-; and A and A' are independently an amine monodendate or A and A' may bound to each other to form a chelate type diamine didendate. An anticancer composition comprises the cyclotriphosphazene-platinum(II) conjugate as an effective ingredient. A method for preparing the conjugate comprises the steps of: (a) hydrolyzing a cyclotriphosphazene represented by the formula(3) to prepare an alkali metal salt or an alkali earth metal salt thereof represented by the formula(4); and (b) coupling the compound of the formula(4) to a (diamine) platinum(II) complex represented by the formula(5), where the n, m, x, y, z, R, R', R", A and A' are same as defined above; M is two alkali metal ions selected from the group consisting of potassium ion and sodium ion or Ba^2+; and L is one or two anion ligand(s) selected from the group consisting of sulfuric acid ion and nitric acid ion.
Abstract:
PURPOSE: A dendritic oligopeptide-grafted cyclotriphosphazene is provided to form hydrogel in low concentration and use as a drug carrier for transfer a protein drug. CONSTITUTION: A drug carrier with sustained release to drug contains dendritic oligopeptide-grafted cyclotriphosphazene of the chemical formula 1. The drug carrier is used for delivering protein drug or peptide drug. A method for preparing the dendritic oligopeptide-grafted cyclotriphosphazene comprises a step of reacting cyclotriphosphazene containing chlorine and polyethyleneglycol of the chemical formula 5 with ester of branched tetrapeptide of the chemical formula 6.
Abstract:
PURPOSE: A method for preparing an amphiphilic cyclic phosphazene trimer with biocompatibility is provided to improve physiochemical stability, efficacy, and toxicity of a drug. CONSTITUTION: Am amphiphilc cyclic phosphazene trimer is denoted by chemical formula 1[N=P(MPEG)(oligopeptide ester)]_3. The oligopeptide is C1-6 alkyl ester or C7-C13 aryl alkyl ester of hexapeptide to nanopeptide. The oligopeptide contains hydrophobic amino acids of glycine(Gly), phenyl alanine(phe), leucine(Leu), isoleucine alanine(Ala), alanine(Ala), or valine(Val). The hydrophobic drug is doxetacell or paclitaxel.