- HUMAN TOPOISOMERASE II-TARGETING ORGANOPLATINUM COMPOUNDS
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Some organoplatinum compounds have been synthesized. These organoplatinum compounds are designed to be human Topoisomerase II-targeting drugs.
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Page/Page column 0041-0042; 0101
(2020/03/15)
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- ORGANOPLATINUM COMPOUNDS AND PHARMACEUTICAL COMPOSITION THEREOF AND METHOD OF PREPARING CRYSTAL OF hTop2
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Some organoplatinum compounds have been synthesized. These organoplatinum compounds are designed to be human Topoisomerase II-targeting drugs.
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Paragraph 0023-0025; 0081-0082
(2020/10/21)
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- The Catalytically Lignan-Activation-Based Approach for the Synthesis of (epi)-Podophyllotoxin Derivatives
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Under the effect of a catalytic amount of Au(I) complex, 4-O-(2-cyclopropylethynyl)benzoyl-(epi)-podophyllotoxins, easily prepared via dehydrative condensation between (epi)-podophyllotoxin and ortho-cyclopropylethynylbenzoic acid, could efficiently coupl
- Wan, Jun-Hao,Hu, Yang,Liu, Hui,Tu, Yuan-Hong,He, Zhong-Yi,Sun, Jian-Song
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p. 5652 - 5662
(2017/06/07)
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- Preparation method of etoposide, teniposide and analogs of etoposide and teniposide
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The invention discloses a preparation method of etoposide, teniposide and analogs of etoposide and teniposide. The preparation method includes the following steps of 1, selective protection of 4'domethylpodophyllotoxin4'hydroxy; 2, introduction of 4 hydroxy hydroxyl; 3, removal of a protecting group. The method is mild in reaction condition and environmentally friendly, and the yield and purity of the products are high.
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Paragraph 0100; 0101; 0102
(2017/01/02)
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- Synthesis and cytotoxic activity on human cancer cells of carbamate derivatives of 4β-(1,2,3-triazol-1-yl)podophyllotoxin
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Carbamate derivatives of 4β-(1,2,3-triazol-1-yl)podophyllotoxin were synthesized by means of click chemistry, and their cytotoxicities against human cancer cell lines HL-60, A-549, HeLa, and HCT-8 were evaluated. Some compounds were more potent than the anticancer drug etoposide. 4′-O-Demethyl- 4β-[(4-hydroxymethyl)-1,2,3-triazol-1-yl]-4-deoxypodophyllotoxin cyclopentyl carbamate, the most potent compound, induced cell cycle arrest in the G2/M phase accompanied by apoptosis in A-549 cells. Furthermore, this compound inhibited the formation of microtubules in A-549 cells and caused the inhibition of DNA topoisomerase-II.
- Liu, Jian-Fei,Sang, Chun-Yan,Xu, Xiao-Hui,Zhang, Lin-Lin,Yang, Xuan,Hui, Lin,Zhang, Jin-Bang,Chen, Shi-Wu
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p. 621 - 628
(2013/07/27)
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- Synthesis and evaluation of the apoptosis inducing and CT DNA interaction properties of a series of 4β-carbamoyl 4′-O- demethylepipodophyllotoxins
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A series of carbamate derivatives of 4′-demethylepipodophyllotoxin have been synthesized, and their cytotoxicities against several human cancer cell lines, including HeLa, A549, HCT-8, and HL-60 cells, evaluated. Some of these compounds exhibited higher levels of cytotoxicity than the anticancer drug etoposide. 4β-4′-Demethylepipodophyllotoxin 1-(4-nitrophenyl) piperazinyl carbamate (19) was found to be the most potent compound of those synthesized in the current study, and induced cell cycle arrest in the G2/M phase in HeLa cells, which was accompanied by apoptosis. Furthermore, this compound activated the expression of Bax, p53 and caspase-3 in HeLa cells, leading to changes in the conformation of calf thymus DNA from the B-form to a more compact C-form.
- Sang, Chun-Yan,Liu, Jian-Fei,Qin, Wen-Wen,Zhao, Jie,Hui, Lin,Jin, Yong-Xin,Chen, Shi-Wu
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- Anti-AIDS agents. Part 61: Anti-HIV activity of new podophyllotoxin derivatives
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A series of novel podophyllotoxin derivatives containing structural modifications at C-4 (7-14), C-4′ (16-17), and the methylenedioxy A-ring (23-28) was synthesized and tested for inhibition of HIV replication. Four of these compounds (25-28) were previou
- Zhu, Xiao-Kang,Guan, Jian,Xiao, Zhiyan,Cosentino, L. Mark,Lee, Kuo-Hsiung
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p. 4267 - 4273
(2007/10/03)
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- Synthesis and antitumor activity of new glycosides of epipodophyllotoxin, analogues of etoposide, and NK 611
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A series of 3-amino- and 3-alkylamino-2-deoxy-β-D-ribo- and β-D- arabino-glycosides of 4'-demethylepipodophyllotoxin have been synthesized by means of an improved trimethylsilyl-iodide procedure for the podophyllotoxin- 4'-demethylepipodophyllotoxin conversion, an efficient and high yielding synthesis of silyl glycoside donors of 3-azido-2,3-dideoxy-β-D-ribo-and β- D-arabino-hexopyranosides and stereoselective glycosylations. In vitro evaluation of cytotoxic effects against murine L1210 leukemia critically demonstrates the essential role played by a 4,6-acetal for biological activity. Among the most cytotoxic compounds, 3-amino-2,3-dideoxy-and 3-N,N- (dimethylamino)-2,3-dideoxy etoposide analogues, 17 and 27-29 are at least as potent as etoposide on the in vivo P388 (iv/ip) murine leukemia models. However, surprisingly enough, none of these compounds inhibits the human DNA topoisomerases I or II or binds to tubulin to prevent its polymerization and microtubule assembly. Therefore, their mechanism of action remains to be cleared up.
- Daley, Laurent,Guminski, Yves,Demerseman, Pierre,Kruczynski, Anna,Etiévant, Chantal,Imbert, Thierry,Hill, Bridget T.,Monneret, Claude
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p. 4475 - 4485
(2007/10/03)
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- Novel D-ring analogues of podophyllotoxin as potent anti-cancer agents
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Several D-ring modified analogues of podophyllotoxin were prepared viz semi-synthesis starting from naturally occuring podophyllotoxin and determined their in vitro anti-cancer activity. Most of the analogues have shown good activity towards human cancer cell lines.
- Subrahmanyam, Duvvuri,Renuka,Rao, C.V. Laxmana,Sagar, P. Sangeeta,Deevi, Dhanvanthri S.,Babu, J. Moses,Vyas
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p. 1391 - 1396
(2007/10/03)
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- Stereo and chemoselective enzymatic reduction of azido functionality: Synthesis of 4-β-Aminopodophyllotoxin congeners by Baker's yeast
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4β-Aminopodophyllotoxin congeners have been synthesized by the stereoselective biocatalytic reduction of the 4-azidopodophyllotoxins employing baker's yeast in excellent yields under mild conditions.
- Kamal, Ahmed,Laxminarayana,Gayatri, N. Lakshmi
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p. 6871 - 6874
(2007/10/03)
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