117604-05-4

Upstream product

• 6559-91-7 4'-demethylepipodophyllotoxin 
• 16477-16-0 4'-O-demethyl-4β-bromo-4-desoxypodophyllotoxin 
• 518-28-5 podofilox 
• 746639-24-7 4β-iodo-4-O-demethylpodophyllotoxin 
• 220995-81-3 4-bromo-4'-demethyl-epipodophyllotoxin 
• 40505-27-9 4-demethylpodophyllotoxin 

Downstream Products

• 1092371-33-9 5-(4-hydroxy-3,5-dimethoxy-phenyl)-9-{4-[(3-nitro-phenylamino)-methyl]-[1,2,3]triazol-1-yl}-5,8,8a,9-tetrahydro-5aH-furo[3',4':6,7]naphtho[2,3-d][1,3]dioxol-6-one 
• 1092371-29-3 5-(4-hydroxy-3,5-dimethoxy-phenyl)-9-[4-(o-tolylamino-methyl)-[1,2,3]triazol-1-yl]-5,8,8a,9-tetrahydro-5aH-furo[3',4':6,7]naphtho[2,3-d][1,3]dioxol-6-one 
• 1020538-11-7 4β-[4-(α-D-glucopyranosyloxymethyl)-1,2,3-triazol-1-yl]-4-deoxy-4'-demethylpodophyllotoxin 
• 1316852-86-4 C₄₁H₃₆N₂O₁₁ 
• 1316852-87-5 C₃₈H₃₀ClFN₂O₉ 
• 1469495-51-9 4-N-(theophylline-7-acetic)amino-4'-demethylepipodophyllotoxin 
• 1469495-50-8 4-N-(5-methylpyrazine-2-carboxylic)amino-4'-demethylepipodophyllotoxin 
• 1469495-49-5 4-N-(2-pyrazinecarboxylic)amino-4'-demethylepipodophyllotoxin 
• 1388218-50-5 C₂₄H₂₃N₃O₈ 
• 1388218-52-7 C₂₄H₂₅N₃O₈S 
• 1388218-51-6 C₂₂H₁₉NO₇S 
• 1310548-39-0 4'-O-demethyl-4β-[(4-butyl)-1,2,3-triazol-1-yl]-4-desoxypodophyllotoxin 
• 675199-75-4 4'-O-demethyl-4β-[(4-hydroxymethyl)-1,2,3-triazol-1-yl]-4-desoxypodophyllotoxin 
• 1310548-44-7 4'-O-demethyl-4β-[(4-decyl)-1,2,3-triazol-1-yl]-4-desoxypodophyllotoxin 

Relevant academic research and scientific papers

Synthesis and Biological evaluation of novel 4β-[(5-substituted)-1,2,3,4-tetrazolyl] podophyllotoxins as anticancer compounds

A series of novel 4β-[(5-substituted)-1,2,3,4-tetrazolyl] podophyllotoxin derivatives were synthesized by employing azide-nitrile click chemistry approach. All the derivatives were evaluated for their cytotoxicity against a panel of four human cancer cell lines and their IC50 values were found to be in the range of 2.4-29.06 μM. The cytotoxicity exhibited by the majority of test compounds were found to comparable and often more effective than doxorubicin and all compounds exhibited higher cytotoxicity on A-549 cell lines. Cell cycle analysis showed that the novel 4β-[(5-substituted)-1,2,3,4-tetrazolyl] podophyllotoxins resulted in cell cycle arrest at G2/M phase and were also found to be the potent inhibitors of tubulin polymerization in vitro.

Synthesis, antitumor activity, and molecular docking of (?)-epigallocatechin-3-gallate-4β-triazolopodophyllotoxin conjugates

Two new (?)-epigallocatechin-3-gallate-4β-triazolopodophyllotoxin conjugates (7 and 8) were synthesized and evaluated for biological activity. Compound 8 showed highly potent anticancer activity against A-549 cell line with IC50 of 2.16 ± 1.02

Synthesis and antitumor activity of camptothecin- 4β-triazolopodophyllotoxin conjugates

Two new compounds (9 and 10) having a camptothecin (CPT) analog conjugated to the 4β-azido-4-deoxypodophyllotixin analog by untilizing the copper-catalyzed azide-alkyne cycloadditon (CuAAC) reaction, and were evaluated for their cytotoxicity against a panel of five human cancer cell lines (HL-60, SMMC-7721, A-549, MCF-7 and SW480) using the MTT (3-(4,5-dimethyl-thiahiazo-2-yl)-2,5-diphenyltetrazolium bromide) assay. Two novel conjugates shown weak cytotoxicity, compound 10 showed highly potent against HL-60 cell line tested, with IC50 value 17.69 ± 0.19 μM. This compound suggested its potential as anticancer agents for further development. (Figure presented.).

Synthesis and Biological Activity of Ferrocenyl and Ruthenocenyl Analogues of Etoposide: Discovery of a Novel Dual Inhibitor of Topoisomerase II Activity and Tubulin Polymerization

Two series of the ferrocenyl and ruthenocenyl analogues of etoposide bearing 1,2,3-triazolyl or aminoalkyl linker were synthesized and evaluated for their cytotoxic properties, influence on the cell cycle, ability to induce tubulin polymerization, and inhibition of topoisomerase II activity. We found that the replacement of the etoposide carbohydrate moiety with a metallocenyl group led to organometallic conjugates exhibiting differentiated antiproliferative activity. Biological studies demonstrated that two ferrocenylalkylamino conjugates were notably more active than etoposide, with submicromolar or low-micromolar IC50 values towards SW620, etoposide-resistant SW620E, and methotrexate-resistant SW620M cancer cell lines. Moreover, the simplest ferrocenylmethylamino conjugate exerted dual inhibitory action against tubulin polymerization and topoisomerase II activity while other studied compounds affected only topoisomerase II activity.

Synthesis and Cytotoxicity of Heterocyclic Amine Derivatives of Podophyllotoxin

A series of amine podophyllotoxin derivatives was designed and synthesized by aldehydes reacting with 4β-amino-desoxypodophyllotoxin or 4′-demethyldesoxypodophyllotoxin. The MTT assay was used to test the cytotoxic activity of 11 target compounds on HeLa

ORGANOPLATINUM COMPOUNDS AND PHARMACEUTICAL COMPOSITION THEREOF AND METHOD OF PREPARING CRYSTAL OF hTop2

Some organoplatinum compounds have been synthesized. These organoplatinum compounds are designed to be human Topoisomerase II-targeting drugs.

HUMAN TOPOISOMERASE II-TARGETING ORGANOPLATINUM COMPOUNDS

Some organoplatinum compounds have been synthesized. These organoplatinum compounds are designed to be human Topoisomerase II-targeting drugs.

Novel conjugates of podophyllotoxin and coumarin: Synthesis, cytotoxicities, cell cycle arrest, binding CT DNA and inhibition of Topo IIβ

A series of conjugates of podophyllotoxin and coumarin were prepared using the click reaction, and their cytotoxicities against A549, HepG2, HeLa, and LoVo cells were evaluated. Among them, compound 14e exhibited the strongest cytotoxicities against these cancer cells with IC50 values of 4.9–17.5 μM. Furthermore, 14e disrupted microtubules and induced cell cycle arrest at G1 phase by regulating P21 and Cyclin D1 in LoVo cells. In addition, 14e bond CT DNA and selectively inhibited Topo IIβ over Topo IIα. Molecular docking model showed that 14e appeared to form stable hydrogen bonds with several DNA bases and residue Gln778. Taken together, these conjugates have the potential to be developed as anti-tumor drugs.

Podophyllotoxin compound containing 1,2,4-triazone structure, and application thereof

The invention discloses a podophyllotoxin compound containing a 1,2,4-triazone structure, and an application thereof. The compound has a structure represented by general formula (I). Podophyllotoxin derivatives containing 1,2,4-triazone, represented by th

A podophyllotoxin with norcantharidin of joining together and its preparation and use (by machine translation)

The invention discloses a novel podophyllotoxin and norcantharidin of joining together, and this method for preparing compound and use thereof. The compounds of this invention is to go to a imide base carboxylic acid 4 β - amino -4 ' - to a epipodophyllot