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몇 가지 전이금속, Ni(II) 및 Zn(II) 3,6-bis(2'-pyridyl)pyridazine 착 화합물들의 세포 독성효과
권병목,이정옥,최상운,성낙도 충남대학교 형질전환복제돼지연구센터 2007 논문집 Vol. No.10
A series of cytotoxic activities (ED_(50)) in vitro against six human cancers (lung cancer, uterine cancer, skin cancer, brain cancer, colon cancer and adenocarcinoma) and their seventeen cell lines of 3,6-bis(2'-pyridyl)pyridazine, 1, 3,6-bis-(6'-methyl-2'-pyridyl)pyridazine, 2 and their transition metal, Ni(II), Cu(II) and Zn(II) complexes, 3~6 were measured. Particularly, the results revealed that the cytotoxic activities against the brain cancer cell line (SNB-19) and the colon cancer cell line (SW62) of bis-[3,6-bis-(6'-methyl-2'-pyridyl)pyridazine-k^(2)N^(2),N^(3)]chlorocopper(II)perchlorate, 4 were shown to be higher than that of the first generation anticancer agent, Cis-platin. 6종의 인체 암(폐암, 피부암, 결장암, 자궁암, 선암 및 뇌암)과 그의 17가지 세포주들에 대한 리간드 화합물 3,6-bis(2'pyridyl)pyridazine(1)과 3,6-bis(6'-methyl-2'-pyridyl)pyridazine(2) 그리고 그들의 전이금속(Ni(II), Cu(II) 및 Zn(II)) 착 화합물들 (3~6)의 세포독성을 각각 측정하였다. 그 결과, 특히 Cu(II) 착화합물, bis-[3,6-bis-(6'-methyl-2'-pyridyl)pyridazine-k^(2)N^(2),N^(3)]chlorocopper(II)perchlorate (4)는 뇌암(SNB-19)과 결장암(SW-62) 세포주에 대하여 제1세대 항암제인 Cis-platin보다 높은 세포독성을 나타내었다.
Micromonospora sp. SA-246 균주가 생산하는 Isochromanequinone계 항생물질
여운형,윤봉식,황경숙,이정옥,유승헌 충남대학교 생물공학연구소 1997 생물공학연구지 Vol.5 No.-
저영양성 미생물을 선택적으로 분리, 배양하여 새로운 생리활성물질을 탐색하던 중 SA-246 균주가 강한 항균활성 및 암세포주에 대한 세포독성을 나타내는 것을 발견하였다. SA-246 균주의 동정을 위하여 배양적, 형태적, 생리적 특성을 ISP 방법에 따라 조사한 결과 Micromonospora 屬에 속하는 것으로 동정하였으며 따라서 Micromonospora sp. SA-246으로 명명하였다. 배양액으로 부터 용매추출, silica gel column chromatography, preparative TLC, HPLC 등에 의하여 활성물질을 분리, 정제하였으며 UV 흡수, mass, NMR spectrum의 분석 결과 본 활성물질을 crisamicin A로 동정하였다. 화합물 SA-246은 그람 양성 세균에 항균활성을, 폐암세포주(A549), 난포암세포주(SK-OV-3), 피부암세포주(SK-MEL-2), 신경암세포주(XF498), 대장암세포주(HCT15)에 세포독성을 나타내었다. In the course of screening for new bioactive compounds from oligotrophs in soil, a microorganism, designated as SA-246 and now identified as Micromonospora sp., has been shown to produce a strong anitbacterial compound. The active compound was purified from broth filtrate by ethylacetate extraction, silica gel column chromatography, preparative TLC and HPLC, and was identified as crisamicin A based on mass and NMR spectral data. The compound SA-246 exhibited not only strong anitbacterial activity against Gram-positive bacteria but also cytotoxicity against cancer cell lines such as A549 (lung), SK-OV-3 (ovarian), SK-MEL-2 (melanoma), XF498 (central nervous system) and HCT15 (colon).
Micromonospora sp. SA-246 균주가 생산하는 Isochromanequinone계 항생물질
여운형,윤봉식,황경숙,이정욱,유승헌 한국미생물생명공학회 ( 구 한국산업미생물학회 ) 1996 한국미생물·생명공학회지 Vol.24 No.3
저영양성 미생물을 선택적으로 분리, 배양하여 새로운 생리활성물질을 탐색하던 중 SA-246 균주가 강한 항균활성 및 암세포주에 대한 세포독성을 나타내는 것을 발견하였다. SA-246 균주의 동정을 위하여 배양적, 형태적, 생리적 특성을 ISP 방법에 따라 조사한 결과 Micromonospora 層에 속하는 것으로 동정하였으며 따라서 Micromonospora sp. SA-246으로 명명하였다. 배양액으로부터 용매추출, silica gel column chromatography, preparative TLC, HPLC등에 의하여 활성물질을 분리, 정제하였으며 UV 흡수, mass, NMR spectrum의 분석 결과 본 활성물질을 crisamicin A로 동정하였다. 화합물 SA-246은 그람 양성 세균에 항균활성을, 폐암세포주(A549), 난소암세포주(SK-OV-3), 피부암세포주(SK-MEL-2), 신경암세포주(XF498), 대장암세포주(HCT15)에 세포독성을 나타내었다. In the course of screening for new bioactive compounds from oligotrophs in soil, a microorganism, designated as SA-246 and now identified as Micromonospora sp., has been shown to produce a strong antibacterial compound. The active compound was purified form broth filtrate by ethylacetate extraction, silica gel column chromatography, preparative TLC and HPLC, and was identified as crisamicin A based on mass and NMR spectral data. The compound SA-246 exhibited not only strong antibacterial activity against Gram-positive bacteria but also cytotoicity against cancer cell lines such as A549 (lung), SK-OV-3 (ovarian), SK-MEL-2 (melanoma), XF498 (central nervous system) and HCT15 (colon).
Lee, Chong-Ock,Choi, Eung-Chil,Kim, Byong-Kak The Pharmaceutical Society of Korea 1981 Archives of Pharmacal Research Vol.4 No.2
The carpophores of a mushroom, Naematoloma fasciculare (Fr.) Karst, were extracted with 0.2 N NaOH and the extract was dialyzed through visking tube. It was found to contain an antitumor activity against sarcoma 180 implanted in mice. The components of this aqueous extract were found to be a polysaccharide and a protein by color reactions including Anthrone and Lowery-Folin tests. The hydrolysis of the polysaccharide with 3% HCL-Me-OH and trimethylsily lation of the hydrolysate yielded five monosaccharides, i. e. glucose, frutose, mannose, galactose and xylose, which were detected and analyzed by GLC. After hydrolysis of the protein with 6N HCl, 15 amino acids, including aspartic acid and glutamic acid, were detected and analyzed by an auto amino acid analyzer.
Lee, Hyeon Ji,Latif, Muhammad,Choe, Hyeonjeong,Ali, Imran,Lee, Heung Kyoung,Yang, Eun Hye,Yun, Jeong In,Chae, Chong Hak,Jung, Jae-Kyung,Kim, Hyoung Rae,Lee, Chong Ock,Park, Chi Hoon,Lee, Kwangho 대한약학회 2014 Archives of Pharmacal Research Vol.37 No.9
Syntheses of various bis-ortho-alkoxy-parapiperazineanilino-pyrimidines and -triazines of KRCA-0008 analogs are described and their structure-activity-relationship to anaplastic lymphoma kinase (ALK) is discussed. 5-trifluoromethyl-2,4-pyrimidine analog (2) seems to be most potent in both biochemical and cellular assay in this study, however it shows inferior mice xenograft activity to Crizotinib presumably due to its sub-optimal PK parameters. 4,6-disubstituted pyrimidine and 2,4-disubstituted triazine derivatives of KRCA-0008 are less potent or inactive to ALK wt., and this observation is explained with their molecular modeling compared to KRCA-0008.
Lee, Hyun-Jung,Kim, Jin-Sung,Suh, Myung-Eun,Park, Hyen Joo,Lee, Sang Kook,Rhee, Hee-Kyung,Kim, Hwa Jung,Seo, Eun-Kyung,Kim, Choonmi,Lee, Chong-Ock,Choo Park, Hea-Young 이화여자대학교 약학연구소 2008 藥學硏究論文集 Vol.- No.18
The substituted pyridazino[4,5-b]phenazine-5,12-diones and tri/tetra-azabenzo[a]fluorene-5,6-diones were synthesized from 6,7-dichloroph-thalazine-5,8-dione and 6,7-dichloroquinoline-5,8-dione, respectively. The cytotoxic activities of the prepared compounds were evaluated by an SRB (Sulforhodamine B) assay against the following human cancer cell lines: A549 (lung), SK-0V-3 (ovarian), SK-MEL-2 (melanoma), XF 498 (CNS), and HCT 15 (colon). Almost all synthesized pyridazino[4,5-b]phenazine-5,12-diones (7a-j) presented higher cytotoxicity than that of doxorubicin (IC_(50) = 0.097-0.225 μM) against the cancer cell lines, In particular, the cytotoxicity of compounds 7f (R₁=Et) and 7h (R₁, R₂ = Me) against all human cancer cell lines examined was about 10 times higher than that of doxorubicin. However, the cytotoxicities of several synthesized azabenzo[a]fluorene-5,6-diones (12a, 12c, 12d, 12e, and 12g) against the cancer cell lines in vitro were comparable to those of doxorubicin.
한국산 고등 균류의 성분 및 배양에 관한 연구(제55보) : Lyophyllum decastes의 항암 성분 및 배양
이정옥(Chong Ock Lee),김형수(Hyung Soo Kim),최응칠(Eung Chil Choi),김병각(Byong Kak Kim) 한국생약학회 1986 생약학회지 Vol.17 No.1
To find antitumor components of Lyophyllum decastes, the mycelia of L. decastes were cultured in artificial media and a new antitumor component which showed potent antitumor activity against sarcoma 180 implanted in mice, was isolated and named Lyophyllan A. Lyophyllan A was composed of a polysaccharide moiety (86%) and a protein moiety (2%). The polysaccharide moiety was found to be a heteroglycan which consisted of glucose (48.1%), rnannose (30.8%), galactose, xylose and fucose. The protein moiety contained 18 amino acids. Cultural characteristics of L. decastes were investigated by shake culture method. The best result was obtained when L. decastes was cultured in medium glucose 50 g, peptone 10 g, corn steep liquor 30㎖, KH₂PO₄ 0.87 g, MgSO₄·7H₂O 0.5 g, CaCl₂ 0.3 g, FeSO₄·7H₂O 10 ㎎, MnC1₂·4H₂O 7 ㎎, ZnSO₄·7H₂O 4 ㎎ and CuSO₄·5H₂O 1㎎ per one liter at 26℃, 180 rpm, for 9 days.
Mathi, Gangadhar Rao,Kang, Chung Hyo,Lee, Heung Kyoung,Achary, Raghavendra,Lee, Ha-Yeon,Lee, Joo-Youn,Ha, Jae Du,Ahn, Sunjoo,Park, Chi Hoon,Lee, Chong Ock,Hwang, Jong Yeon,Yun, Chang-Soo,Jung, Hee Jun Elsevier 2017 European journal of medicinal chemistry Vol.126 No.-
<P><B>Abstract</B></P> <P>The piperidine fragment in ceritinib was replaced with diverse aliphatic amines to improve inherent resistance issues of ceritinib. While most of the prepared compounds exhibit as similar in vitro activities as ceritinib, compound <B>10</B> shows encouraging activities against wild-type ALK as well as crizotinib-resistant mutants including extremely resistant G1202R mutant with an IC<SUB>50</SUB> of 1.8 nM. Furthermore, pharmacokinetic profiles of <B>10</B> is apparently better than that of ceritinib. In murine xenograft studies, compound <B>10</B> turns out to be as active as ceritinib, suggesting that further optimization of <B>10</B> may lead to clinical candidates overcoming ALK mutant issues.</P> <P><B>Highlights</B></P> <P> <UL> <LI> The terminal piperidine in ceritinib was replaced with diverse alkyl amines. </LI> <LI> Most of the analogs were as active as crizotinib against ALK wild-type and L1196M mutant. </LI> <LI> Compound <B>10</B> has excellent ALK mutant activities including extremely resistant G1202R. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Cytotoxic Triterpenes from Crataegus pinnatifida
Min, Byung-Sun,Kim, Young-Ho,Lee, Sang-Myung,Jung, Hyun-Ju,Lee, Jun-Sung,Na, Min-Kyun,:lee, Chong-Ock,Lee, Jong-Pil,Bae, Ki-Hwan The Pharmaceutical Society of Korea 2000 Archives of Pharmacal Research Vol.23 No.2
Bioassay-guided fractionation of Crataegus pinnatifida (Rosaceae) gave two cytotoxic ursane-type triterpenes which were identified as uvaol (1) and ursolic acid (2) by physicochemical and spectroscopic methods. 3-Oxo-ursolic acid (3) was synthesized from ursolic acid (2) by Jones method. The cytotoxic activities of these compounds were tested against murine L1210 and human cancer cell lines (A549, SK-OV-3, SK-MEL-2, XF498, and HCT15) in vitro. Compounds 1 and 2 showed moderate cytotoxicities against L1210, whereas they showed weak activities against human cancer cell lines. However compound 3 exhibited potent cytotoxic activities both in murine and in human cancer cell lines.