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1

Wydzielanie, właściwości i aktywność przeciwnowotworowa polisacharydów ze strzykwy

Duan Kunfeng

Przemysł Chemiczny

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2019

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T. 98, nr 2

200--203

PL

Z surowego polisacharydu uzyskanego ze strzykwy (ogórka morskiego) metodą hydrolizy enzymatycznej wydzielono trzy rafinowane polisacharydy, które zastosowano jako inhibitory w leczeniu raka płuc (linia komórkowa A549), raka żołądka (linia komórkowa SGC-7901), raka piersi (linia komórkowa MCF-7) oraz raka trzustki (linia komórkowa PANC-1). Rafinacja poprawiła efekt hamowania wzrostu komórek nowotworowych, zwłaszcza przy zastosowaniu polisacharydów o większym stężeniu. Hamowanie było najskuteczniejsze w przypadku komórek raka piersi MCF-7, a najsłabsze dla komórek raka płuc A549.

EN

Three polysaccharides were prepd. by refining the crude polysaccharide of sea cucumber by enzymatic hydrolysis and studied as cancer inhibitors on human lung cancer cells A549, human gastric carcinoma cells SGC-7901, human breast cancer cells MCF-7 and pancreatic cancer cell PANC-1. The refining resulted in increasing the inhibition effects. They increased also with increasing the polysaccharide concn. The inhibition was strongest in respect to MCF-7 cells and weakest for A549 cells.

2

Synthesis, Spectral Characteristics and Antitumor Activity of Tungstosilicic Polyoxometalate Containing 5-Fluorouracil

Feng C. G., Wang S. S., Liu X.

Polish Journal of Chemistry

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2009

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Vol. 83, nr 12

2079-2087

EN

A novel polyoxometalate com pound with 5-fluorouracil C4H4FN2O2H3SiW12O40ź12H2O (FSW) was synthesized and its structure was analyzed using IR spectra, X-ray powder diffraction (XRD), 183W NMR and TG. IR spectra and XRD indicate that FSW has a Keggin structure of heteropolyanion with a ring structure of 5-fluorouracil as expected. It was found by the analysis of the 183W NMR spectra that the W atoms of FSW remain in the same chemical environment. The results of TG show that the compound has two weight-losing steps with certain degree of thermal stability. The present study uses 5-fluorouracil as the positive control group in the cytotoxicity tests of FSW on human renal embryonic cell HEK293 and the antitumor activity tests in cervical cancer cell Hela using the methyl thiazolyl tetrazolium method. The results obtained show that the therapeutic index of the new polyoxometalate compound is 0.75, higher than that of 5-fluoro-uracil.

3

Kombretastatyna A-4 (CA-4) i jej analogi : synteza i aktywność biologiczna

Dzierzbicka K., Kubacka P., Renusz S., Kołodziejczyk A.M.

Wiadomości Chemiczne

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2008

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[Z] 62, 11-12

1037-1064

EN

This article described synthesis and biological activity of combretastatin A-4 (CA-4) and its analogues. Combretastatin A-4 (CA-4), a natural product isolated from the South African bush willow tree Combretum caffrum, binds to the colchicine binding site and inhibits the polymerization of microtubules. CA-4 exhibits potent cytotoxicity against a variety of human cancer cell lines including multidrug-resistant (MDR) cell lines [5-7]. The studies of structure-activity relationship (SAR) of CA-4 1 (Fig. 1) showed that 3,4,5-trimethoxy substitution on the A ring and the 4'-methoxy group on the B ring and the cis-olefin configuration are crucial for potent cytotoxicity, while the 3'-hydroxy group is optional [5-7]. A many of CA-4 analogues were synthesized where the double bond have been replaced by introduction of nonheterocyclic groups (e.g. ethers, olefins, ketones, sulfonates, sulfonamides, amide derivatives, amine, cyclopentanes) or heterocyclic groups containing five-membered rings (e.g. pyrazoles, thiazoles, triazoles, tetrazoles, oxazoles, furans, dioxolanes, thiophenes) and indoles [5, 7, 41, 56] (Fig. 9-12). Up to now, many CA-4 analogues and their biological activity have been extensively studied and three derivatives are currently in clinical trials: a water-soluble disodium phosphate derivative of CA-4 (CA-4P) 11c (Fig. 3); Oxi-4503, a water-soluble combretastatin A-1 (CA-1diP) 4a (Fig. 1); and AC7700 59e (Scheme 7) an aminocombretastatin prodrug developed in Japan in 1998 [5-10, 34].

4

Kompleksy platyny (IV) jako potencjalne związki przeciwnowotworowe

Ciołkowski M., Budzisz E.

Wiadomości Chemiczne

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2007

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[Z] 61, 1-2

43-60

EN

Cisplatin is an important anticancer drug. Unfortunately it does not bring satisfactory effects in all types of tumor. Other problems are its toxicity and intrinsic or acquired resistance of tumor cells. That is why new drugs based on this molecule are being searched. One of the promising group of chemical compounds are neutral platinum(IV) complexes. They are more inert than platinum(II) complexes. In consequence their reactivity in bloodstream is weaker and more molecules can reach their target. Many studies were done to establish the relation among the structure, lipophilicity, reduction potential and cytotoxicity of those complexes. It is believed that platinum(IV) complexes must be reduced to platinum(II) complexes to obtain cytotoxicity. The speed of reduction depends on the nature of axial ligands. The complexes with chloride ligands are reduced the most quickly and complexes with hydroxide ligands are reduced the most slowly. In vitro cytotoxic activity of those complexes was shown to depend on their reduction potential. However suggestions exist that this result can be misleading for their in vivo activity, as platinum(IV) complexes are pro-drugs and might be inactive before reaching cancer cells. In a study of group of platinum(IV) complexes, derivatives of cisplatin and dichloroethylenediamineplatinum(II), a tendency for an increase of cytotoxic activity when lipophilicity increased was observed. However in a study of tetrakis(carboxylato)(1,2-diaminocyclohexane)platinum(IV) complexes, different cytotoxic activity of complexes possessing similar lipophilicity was observed. Hence lipophilicity of complex is important but it is not the only factor that determines complex activity. In other studies complexes of general structure cis, trans, cis-[PtNH3(RNH2)Cl2(OCOR')2] were examined. The research showed an increased activity of compounds with longer carbon chains of carboxylate axial ligands. It was also revealed that complexes with alicyclic amine ligands were more cytotoxic than those with aliphatic or aromatic amine ligands. Hall et al. revealed that platinum(IV) complexes, derivatives of cisplatin and dichloroethylenediamineplatinum(II), are active against DLD-1 colon cancer cell line in hypoxic environment. An examination of trans-dichlorodihydroxo(dimethylamine)(isopropylamine)platinum(IV) revealed its greater cytotoxic activity against A2780, CH1 and 41M human ovarian cancer cell lines, in vitro. Moreover this complex was shown to be active against A2780cisR, CH1cisR and 41McisR human ovarian cell lines which are resistant to cisplatin. Two platinum(IV) complexes: iproplatin (cis, trans, cis-dichlorodihydroxobis(isopropylamine)platinum(IV)) and tetraplatin (tetrachloro(cyclohexane-1,2-diamine)platinum(IV)) have had entered clinical trials. However iproplatin occurred to be less active than cisplatin and tetraplatin turned out to be neurotoxic. Presently two other complexes seem to be very promising: satraplatin (bis(acetato)amminedichlorocyclohexylamineplatinum(IV)) and adamplatin (bis(acetato)(1-adamantylamine)amminedichloroplatinum(IV)). Both have entered clinical trials. There are some "nonstandard" approaches to investigating platinum complexes. For example platinum(IV) complexes with radioactive iodine isotope or with enzyme inhibitor were examined. Studies mentioned above present different approaches to searching for anticancer drugs among platinum(IV) complexes. Despite all encountered difficulties during researching platinum(IV) complexes, this group of compounds still seems to be potential source of new anticancer drugs.

5

Synthesis of (3-Amino-7-chloro-8-methyl-1,1-dioxo-4H-1,5,2-benzo[f]dithiazepin-4-ylidene)acetic Acid De rivatives as Potential Antitumor Agents

Brzozowski Z., Sączewski F., Sławiński J.

Polish Journal of Chemistry

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2007

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Vol. 81, nr 12

2133-2142

EN

Several 3-amino-7-chloro-8-methyl-1,1-dioxo-4H-1,5,2- benzo[f]dithiazepin- 4-yli - dene)acetic acid derivatives (2, 4-15) have been syn the sized. The in vi tro antitumor activity of the compounds 8, 10-12 and 14-15 have been evaluated in the US National Cancer Institute. Screening data indicated that compounds 10, 11 and 14 exhibited high activity against 1-28 human tumor cell lines (GI50 < 0.01 to 3.0 mM). [3-(Benzo-2,1,3-thiadiazol-4-ylamino)-7-chloro-8-methyl-1,1-dioxo-4H-1,5,2-benzo[f]dithiazepin-4--ylidene]acetic acid 11 is the prominent one due to remark able activity and selectivity toward CNS cancer SF-295 cell line of (GI50 < 0.01 mM; TGI = 0.05 mM) and BT-549 cell line of breast cancer (GI50 < 0.01 mM; TGI = 0.09 mM).

6

Synthesis, and In Vitro Antitumor Activity of a New Series of 4-Chloro-2-mercapto-5-methylbenzenesulfonamide Derivatives

Sławiński J., Brzozowski Z.

Polish Journal of Chemistry

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2007

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Vol. 81, nr 8

1433-1440

EN

The synthesis of S-(5-chloro-4-methyl-2-sulfamoylphenyl) N-(phenylsulfonyl)benzothiohydrazonates 4a–k is described. The compounds 4b–f and 4j–k were screened at the US National Cancer Institute for their in vitro activities against a panel of 53–57 human tumor cell lines and relationship between structure and antitumor activity is discussed. The compound 4b was inactive, whereas the remaining compounds exhibited fairly high or reasonable activity (GI50 = 8.12–24.9 miM) against one or more human tumor cell lines.

7

Inhibitory mikrotubul w terapii przeciwnowotworowej

Dzierzbicka K., Kołodziejczyk A.M.

Wiadomości Chemiczne

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2006

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[Z] 60, 5-6

345-364

EN

Microtubule targeting drugs being in the late preclinical or early clinical development are described in this article. New semisynthetic paclitaxel analogues, natural compounds of diverse structure such as epothilones, combretastatins, colchino-ids or dolastatins and synthetic compounds of low molecular weight such as heterocombretastatins, sulfonamides, phenstatins, indoles and quinolones belong to this category of anticancer medicines. Microtubules are hollow tubes consisting of L- and B-tubulin heterodimer proteins that polymerize parallelly to a cylindrical axis. The targeting of microtubules is an important mechanism in cancer chemotherapy for such drugs as the vinca alkaloids (vincristine (1), vin-blastine (la)), podophilotoxin, their semisynthetic analogues and taxanes (paclitaxel (2), docetaxel (3)) known of their great usefulness in the anticancer therapy. These agents may stabilize microtubules, as the taxanes do, or destabilize them, as it is in the case of the vinca alkaloids. Today, more than 30 compounds targeting tubulin, either stabilizing or destabilizing microtubule dynamics, are in late preclinical or early clinical development. Despite of more than 30 years after the discovery of paclitaxel microtubule inhibitors they are still of the topic of interest of all over the world. In the end of 1990 and up to 2005 year survey articles on the microtubule inhibitors were published .We expect now that the paper which presents last results study may be useful.

8

Transition Metal Manganese(II), Nickel(II), Copper(II) and Zinc(II) Complexes of a New Schiff Base Ligand: Synthesis, Characterization and Antitumor Activity Studies

Yang T., Qin W.

Polish Journal of Chemistry

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2006

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Vol. 80, nr 10

1657-1662

EN

Four transition metals complexes ([Mn(L)2] (complex 1), [Ni(L)20.5H2O] (complex 2), [Cu(L)24H2O] (complex 3) and [Zn(L)20.5H2O] (complex 4)), which contain a new Schiff base ligand (HL) derived from 2,4-dihydroxylacetophenone with triaminotriethylamine, have been synthesized and subsequently characterized by element analysis, 1HNMRand mass spectra. Their properties have been investigated by IR, UV and TG-DTA techniques. Tentative structures for the complexes have been proposed based on the experimental results. The antitumor activity against HL-60 human leukemia cells of free ligand (L) and its Mn(II), Ni(II), Cu(II) complexes were also studied by MTT method. The Ni(II) complex shows the best antitumor activity properties among these complexes.

9

Synthesis, Spectral Properties and Antitumor Activity of Some Transition Metal Complexes with a Schiff Base Ligand

Tai X., Yin X., Tan M.

Polish Journal of Chemistry

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2003

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Vol. 77 / nr 4

411-414

EN

Four complexes of transition metals, namely: [Mn(L)2] (complex 1), [Ni(L)2ź0.5H2O] (complex 2), [Cu(L)2ź4H2O] (complex 3) and [Zn(L)2ź0.5H2O] (complex 4), (L = Schiff base derived from trimethylol amino methane and salicylic aldehyde), have been synthesized. The complexes were characterized by elemental analysis, IR, 1H NMR, UV and TG-DTA spectra. Tentative structures for the complexes have been proposed. The antitumor activity against HL-60 human leukemia cells of free ligand and its Mn, Ni, Cu complexes were studied by MTT method.