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Synthesis and In Vitro Cytotoxicity of 3-or 4-Dialkylaminomethyl-1-azaanthraquinones
Lee, Heesoon,Choi, Jae-Young,Lee, Seung-lI,Hong, Seoung-Soo,Cho, Jungsook,Kim, Young-Ho 충남대학교 약학대학 의약품개발연구소 1999 藥學論文集 Vol.15 No.-
Six 3-dialkylaminomethyl-1-azaanthraquinones and five 4-dialkylaminomethyl-1-azaanthraquinones were synthesized and evaluated in vitro cytotoxicity against four human cancer cell lines. The compounds retained much of their cytotoxic activity against the multi-drug-resistant cell line (KB-V-1) as shown by resistance index.
( Chang Hoon Lee ),( Jungsook Cho ),( Kyeong Lee ) 한국응용약물학회 2020 Biomolecules & Therapeutics(구 응용약물학회지) Vol.28 No.2
Changing trends in anticancer research have altered the treatment paradigm to the extent that it is difficult to investigate any anticancer drugs without mentioning immunotherapy. Thus, we are finally contemplating tumour regression using magic bullets known as immunotherapy drugs. This review explores the possible options and pitfalls in tumour regression by first elucidating the features of cancer and the importance of tumour microenvironments. Next, we evaluated the trends of anticancer therapeutics regulating tumour microenvironment. Finally, we introduced the concept of tumour regression and various targets of tumour microenvironment, which can be used in combination with current immunotherapy for tumour regression. In particular, we emphasize the importance of regulating the neurological manifestations of tumour microenvironment (N) in addition to inflammation (I) and hypoxia (H) in cancer.
Synthesis and In vitro Evaluation of 4-Substituted-1-azaanthraquinones
Lee, HeeSoon,Hong, Seoung-=Soo,Choi, Jae-Young,Cho, JungSook,Kim, Young-Ho 충남대학교 약학대학 의약품개발연구소 1998 藥學論文集 Vol.14 No.-
Doxorubicin and daunomycin are the best known members of the anthracycline antibiotics and the most commonly used intercalaing agents in the treatment of cancer(Wakelin and Waring, 1990). Doxorubicin has a broad spectrum of activity, being particularly efficacious against solid tumors. However its clinical usefulness is limited by cardiotoxicity that develop after extended therapy, and the appearance of an acquired resistance (Priebe, 1995; Surato et al 1990). Synthetic analogues, mitoxantrone and ametantrone, resulted from efforts to produce anthracycline analogues that lack cardiac toxicity. Mitoxantrone in particular currently plays an important role in the clinical management of hematological malignancies such as chronic myelogenous leukemia, acute nonlymphoblastic leukemia, and non-Hodgkin's lymphoma, as well as in combination therapy of refractory overian and breast cancers (Wakelin and Waring, 1990). Although mitoxantrone is endowed with an improved tolerability profile compared with doxorubicin and other anthracylines, this drug is not devoid of significant toxic side effects especially those associated with myelosupporession(Gandolf et al., 1995). A number of studies have identified mitoxantrone as an intercalating agent, all indications being that its biological activity is attributable to its DNA-binging properties. DNA intercalation and interference with the DNA-topoisomerase Ⅱ activity resulting in protein associated DNA strand breaks have been proposed as critical events that lead to mitoxantrone-induced cell death(Wakelin and Waring, 1990). The search for new analogues side effects of the anthracycline analogues is of extreme interest and numerous analogues have been reported(Priebe, 1995).