Hypoxic conditions are usually the common feature of solid tumors resulting from their inefficient microvascular systems due to the rapid tumor growth  [1]. This behavior distinguished solid tumor cells from normal cells causing their resistance to the chemo- and radiotherapy but, on the other hand, also giving new opportunities for selective cancer treatment. In our approaches to the design and synthesis of targeted anticancer prodrugs for tumor site-specific activation we paid our attention to Pt(II) complexes with nitrodiazoles. This class of compounds potentially should exhibit dual mode of action, binding to DNA and undergo the bioreductive activation process.

On presented poster, the synthesis of new platinum complexes with nitropyrazoles and their cytotoxic activity against tumor line cells in aerobic and hypoxic conditions [2] is going to be shown. Revealed activity of tested complexes shows strong cytotoxic activity of new platinum complexes against tumor lines, in a few cases, stronger than reference drug cisplatin.

Research was granted by KBN financial support,  grant nr N N401 052938

References:

1.  Chen Y., Hu L., Design of anticancer prodrugs for reductive activation, Med. Res. Rev., 2009 Jan;29(1), 29-64

2.  Andrzej Regiec, Agnieszka Mastalarz, Henryk Mastalarz, Joanna Wietrzyk, Cis- i trans- związki kompleksowe platyny(II) z 1-metylo-4-nitropirazolem, sposób ich wytwarzania, rozdzielania, izomeryzacji i zastosowanie do wytwarzania leków do terapii przeciwnowotworowej, zgłoszenie patentowe (patent application) nr P.393483, 2010

• Legal notice:
  

  Copyright (c) Pielaszek Research, all rights reserved.
  The above materials, including auxiliary resources, are subject to Publisher's copyright and the Author(s) intellectual rights. Without limiting Author(s) rights under respective Copyright Transfer Agreement, no part of the above documents may be reproduced without the express written permission of Pielaszek Research, the Publisher. Express permission from the Author(s) is required to use the above materials for academic purposes, such as lectures or scientific presentations.
  In every case, proper references including Author(s) name(s) and URL of this webpage: https://science24.com/paper/25500 must be provided.

1. Synthesis of new 5H-indolo[2,3-b]quinoline derivatives with a high selective cytotoxic activity
2. Immunomodulatory activity of new isoxazole derivatives
3. Effect  of  5-amino-3-methyl-4-isoxazolecarboxylic acid hydrazide on primary humoral immune response in mice
4. Immunorestoring activity of isoxazole derivative R-13
5. Administration of isothiocyanate-derived mercapturic acids inhibits solid tumor growth of 4T1 murine mammary carcinoma cells in BALB/c mice
6. Preliminary studies on application of library of artificial receptors for differentiation of metabolites in urine of healthy and cancer mice
7. Starch derivatives as vehicles for drug delivery in anticancer therapy
8. Mercapturic acids as a naturally occurring isothiocyanates prodrug form with site-directed delivery system built-in based on an oxidative environment of the tumor
9. Synthesis and biological activity of novel N,N-cyclic-2,4-dihydroxythiobenzamide derivatives
10. Anticancer activity of vitamin D, genistein and indoloquinoline analogs
11. Synthesis and anticancer activity of acetylenic derivatives of betulin
12. Interaction of endotoxin and polymyxin B in B16 mouse melanoma model of metatstasis
13. Anticancer activity of the conjugates:  modified fibrinogen – methotrexate.
14. New method of obtaining of 2-cyano- 3-alkoxy- 2-butenoates
15. Searchıng for new ısoxazole derıvatıves wıth potentıal ımmunorestorıng actıvıty
16. Vitamin D analogs enhance the activity of imatinib mesylate in human non-small cell lung cancer model
17. Colon cancer treatment with the use of vitamin D analogs and irinotecan 
18. Novel bifunctional synthetic isothiocyanates with high antiproliferative activity
19. Naturally occurring hydroxyalkyl isothiocyanates and isothiocyanatoalkyl benzoates - structure-activity and structure-mechanism of action relationship studies.
20. Synthesis and biological evaluation of new amino acid and dipeptide derivatives of neocryptolepine as anticancer agents. 
21. Antitumor activity of carrier-methotrexate conjugates.
22. CLA derivatives as functional food compounds
23. New acetylenic derivatives of betulin with anticancer activity
24. Catalytic synthesis and antiproliferative activity in vitro of polisubstituted isoxazolopyridine derivatives.
25. Steroid profile of Asplenium cuneifolium
26. Research into transformations of 5-amino-3-methyl- 4-isoxazolecarboxylic acid hydrazide under orthoesters influence
27. Electrochemical studies of Pt (II) complexes with potential bioreductive properties
28. The influence of (24R)-1,24- dihydroxyvitamin D₃ on the anticancer activity of 5-fluorouracil in human colon cancer model
29. Comparison of antiproliferative activity of the natural isothiocyanates and their mercapturic derivatives.
30. Could the calorically restricted ketogenic diet be an     effective alternative or supportive therapy for breast cancer?
31. Analogs of genistein and its possible anti-metastatic properties
32. The influence of novel analogs of vitamin D₃ on the antiproliferative activity of cisplatin or doxorubicin on human promyelocytic leukaemia cell line HL-60 
33. New amino acid and peptide derivatives of 5H-indolo[2,3-b]quinoline and their biological activity.
34. The cytotoxic activity of glycosides of indolo[2,3-b]quinoline derivatives.
35. Disubstituted indolo[2,3-b]quinoline derivatives - the cytotoxic activity in vitro against various human tumor cell lines.
36. Mono substituted 5H- and 6H-indolo[2,3-b]quinoline derivatives and their ability to overcome the barrier of drug resistance.
37. Synthesis and antiproliferative activity in vitro of (4-substituted-2-butynylthio)quinolines
38. New calcipotriol analogs, their toxicity and antitumor activity in vivo in comparison to the affinity with VDR and DBP
39. Two examples of very closely related isoxazoles exhibiting opposite immunological activities
40. Synthesis new 1,2,4-triazoline- and 1,3,4-tiadiazole - isoxazole derivatives with immunomodulatory activities
41. Synthesis and cytostatic activity of new 1-substituted 6H-pyrido[4,3-b]carbazole derivatives
42. The new analogs of genistein decrease mitochondrial membrane potential and activate caspase-3
43. New amino acid derivatives of 6H-indolo[2,3-b]quinolines
44. Influence of Transformation of the Amino Group in Anthracyclines into -N=CH-N< or -N=CH-O- Group on Their Biological Properties
45. PRIMARY CYTOTOXICITY EVALUATION OF NEW HETEROCYCLIC SYSTEMS WITH PYRIDODIAZEPINE.
46. SYNTHESIS AND ANTIPROLIFERATIVE ACTIVITY IN VITRO OF NEW 2-AMINOBENZIMIDAZOLE DERIVATIVES. PART 3. REACTIONS OF 2-ARYLIDENE- AMINOBENZIMIDAZOLE WITH SELECTED 1,3-DIKETONES.
47. CONJUGATED LINOLEIC ACIDS PREPARATIONS AS EFFECTIVE NUTRACEUTICS
48. THE ANTIMETASTATIC EFFECT OF BACTERIOPHAGE T4* ADMINISTRATED IN COMBINED TREATMENT WITH SELECTED CYTOSTATICS IN MICE WITH B16 MELANOMA
49. SYNTHESIS AND ANTIPROLIFERATIVE ACTIVITY OF DIACETYLENIC THIOQUINOLINES
50. SYNTHESIS AND CYTOTOXIC ACTIVITY OF 10-DEACETYL-10-PROPARGILPACLITAXEL
51. THE CYTOTOXIC GLYCOSIDES OF INDOLO[2,3-B]QUINOLINE DERIVATIVES. IN VITRO AND IN VIVO STUDIES
52. MONO SUBSTITUTED 5H-INDOLO[2,3-B]- QUINOLINE DERIVATIVES AND THEIR ABILITY TO OVERCOME THE BARRIER OF DRUG RESISTANCE.
53. DISUBSTITUTED INDOLO[2,3-b]QUINOLINE DERIVATIVES. THE CYTOTOXIC ACTIVITY IN VITRO AGAINST VARIOUS HUMAN TUMOR CELL LINE.
54. ANTITUMOR EFFECT OF CISPLATIN OR FLUOROURACIL IN COMBINED TREATMENT WITH (24R)-1,24-DIHYDROXYVITA- MIN D₃
55. IMMUNOLOGICAL ACTIVITY OF DISUBSTITUTED SEMICARBAZIDE AND THIOSEMICARBAZIDE ISOXAZOLE DERIVATIVES
56. PRELIMINARY STUDIES ON IMMUNOTROPIC ACTIVITY OF THE NEW LEAD STRUCTURES IN THE ISOXAZOLE HETEROCYCLIC SYSTEM
57. FIRST ROUND STUDIES ON LEWIS LUNG CARCINOMA ACTIVITY OF THE NEW LEAD STRUCTURES IN THE ISOXAZOLE HETEROCYCLIC SYSTEM
58. GENISTEIN, ITS NEW ANALOGS AND COMPLEXES - THE ANTIPROLIFERATIVE EFFECTS ON HL-60 LEUKEMIA CELL LINE
59. COMBINATION OF: IMATINIB, PRI-2191 AND CYTOSTATICS - THE ANTIPROLIFERATIVE EFFECTS ON HL-60 LEUKEMIA CELL LINE
60. ANTIPROLIFERATIVE ACTIVITY IN VITRO OF DIASTEREOMERIC ANALOGUES OF VITAMIN D3 AGAINST NORMAL AND CANCER CELL LINES