The analogues of 1,25-dihydroxyvitamin D₃ with reversed configuration at C-1 or C-24 and E or Z geometry of double bond at C-22 in the side-chain or at C-5 in the triene system were examined for their antiproliferative activity in vitro against a spectrum of various human and mouse cancer cell lines.

Calcitriol and tacalcitol (used as a control compounds) as well as analogues coded PRI-2201, PRI-2202 and PRI-2205 revealed strong antiproliferative activity against human HL-60 leukaemia cells, breast MCF-7 and T47D cancer cells, squamous SCC-25 cancer cells and mouse WEHI-3 leukaemia cell line. Interestingly, new analogs, as well as the control tacalcitol were more active against HL-60/MX2 (subline resistant to mitoxantrone) than calcitriol.

The novel analogues similarly to calcitriol appeared to be less active against A549, FaDu, K562, CCRF/CEM, 16/C, MDA-MB-231, ASPC-1, LNCaP (inhibition of proliferation lower than 50%) and not active against other tested human cancer cell lines (antiproliferative activity lower than 20%).

The mechanism of the observed in vitro antiproliferative effect of calcitriol, tacalcitol and PRI-2201 may be related to their effect on the cell differentiation (the accumulation of cells in G0/G1 phase). The appearance of antigen CD14 and CD11b expression after exposure of HL-60 cells to calcitriol or tacalcitol and PRI-2201 confirmed their cell differentiating effect. Analogues PRI-2202 and PRI-2205 were less potent in induction of G0/G1 phase accumulation, rather increases percent of apoptotic cells.

• 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/6461 must be provided.

1. The comparison of the stability indicating  two HPLC methods and their application for the determination of bosentan in coated tablets 
2. Synthesis of new 5H-indolo[2,3-b]quinoline derivatives with a high selective cytotoxic activity
3. Elaboration of travoprost eye drops formulation.
4. What modern crystallography can add to pharmaceutical research?
5. Administration of isothiocyanate-derived mercapturic acids inhibits solid tumor growth of 4T1 murine mammary carcinoma cells in BALB/c mice
6. Antiproliferative and cytotoxic effect of vitamin D₃ and its derivatives on the selected cells with a higher proliferative potential
7. Preliminary studies on application of library of artificial receptors for differentiation of metabolites in urine of healthy and cancer mice
8. Starch derivatives as vehicles for drug delivery in anticancer therapy
9. Mercapturic acids as a naturally occurring isothiocyanates prodrug form with site-directed delivery system built-in based on an oxidative environment of the tumor
10. Synthesis and biological activity of novel N,N-cyclic-2,4-dihydroxythiobenzamide derivatives
11. Anticancer activity of vitamin D, genistein and indoloquinoline analogs
12. Pharmaceutical  technologies  – why do they have to be innovative
13. A novel convergent synthesis of the prostaglandin F_2α analogues
14. Synthesis and anticancer activity of acetylenic derivatives of betulin
15. Comparative permeation studies of tacalcitol through the human skin from brand product versus generic product
16. HPLC method for determination of the enantiomeric purity of a new ω chain aldehyde synthon used in the synthesis of travoprost
17. Interaction of endotoxin and polymyxin B in B16 mouse melanoma model of metatstasis
18. Anticancer activity of the conjugates:  modified fibrinogen – methotrexate.
19. Synthesis and cytotoxic activity of new Pt (II) complexes with nitropyrazoles in aerobic and hypoxic conditions
20. Vitamin D analogs enhance the activity of imatinib mesylate in human non-small cell lung cancer model
21. Colon cancer treatment with the use of vitamin D analogs and irinotecan 
22. Novel bifunctional synthetic isothiocyanates with high antiproliferative activity
23. Naturally occurring hydroxyalkyl isothiocyanates and isothiocyanatoalkyl benzoates - structure-activity and structure-mechanism of action relationship studies.
24. Synthesis and biological evaluation of new amino acid and dipeptide derivatives of neocryptolepine as anticancer agents. 
25. Experimental and theoretical charge density studies on a model analogue of vitamin D
26. Synthetic Technologies of Pharmaceutical Substances
27. Antitumor activity of carrier-methotrexate conjugates.
28. CLA derivatives as functional food compounds
29. New acetylenic derivatives of betulin with anticancer activity
30. Catalytic synthesis and antiproliferative activity in vitro of polisubstituted isoxazolopyridine derivatives.
31. Steroid profile of Asplenium cuneifolium
32. The influence of (24R)-1,24- dihydroxyvitamin D₃ on the anticancer activity of 5-fluorouracil in human colon cancer model
33. Comparison of antiproliferative activity of the natural isothiocyanates and their mercapturic derivatives.
34. Could the calorically restricted ketogenic diet be an     effective alternative or supportive therapy for breast cancer?
35. The use of the hyphenated LC-MS/MS technique for the characterisation of impurity profile of Quetiapine during drug development
36. A novel synthesis of 19-nor analogs of vitamin D
37. Analogs of genistein and its possible anti-metastatic properties
38. The influence of novel analogs of vitamin D₃ on the antiproliferative activity of cisplatin or doxorubicin on human promyelocytic leukaemia cell line HL-60 
39. New amino acid and peptide derivatives of 5H-indolo[2,3-b]quinoline and their biological activity.
40. The cytotoxic activity of glycosides of indolo[2,3-b]quinoline derivatives.
41. Disubstituted indolo[2,3-b]quinoline derivatives - the cytotoxic activity in vitro against various human tumor cell lines.
42. Mono substituted 5H- and 6H-indolo[2,3-b]quinoline derivatives and their ability to overcome the barrier of drug resistance.
43. Isolation, structural elucidation and characterization of impurities in latanoprost
44. New rosiglitazone salts
45. Synthesis and antiproliferative activity in vitro of (4-substituted-2-butynylthio)quinolines
46. New calcipotriol analogs, their toxicity and antitumor activity in vivo in comparison to the affinity with VDR and DBP
47. Synthesis and cytostatic activity of new 1-substituted 6H-pyrido[4,3-b]carbazole derivatives
48. High-yielded method of synthesis of voriconazole.
49. The new analogs of genistein decrease mitochondrial membrane potential and activate caspase-3
50. New amino acid derivatives of 6H-indolo[2,3-b]quinolines
51. Polimorphism of Active Pharmaceutical Ingredients
52. Influence of Transformation of the Amino Group in Anthracyclines into -N=CH-N< or -N=CH-O- Group on Their Biological Properties
53. PRIMARY CYTOTOXICITY EVALUATION OF NEW HETEROCYCLIC SYSTEMS WITH PYRIDODIAZEPINE.
54. SYNTHESIS AND ANTIPROLIFERATIVE ACTIVITY IN VITRO OF NEW 2-AMINOBENZIMIDAZOLE DERIVATIVES. PART 3. REACTIONS OF 2-ARYLIDENE- AMINOBENZIMIDAZOLE WITH SELECTED 1,3-DIKETONES.
55. CONJUGATED LINOLEIC ACIDS PREPARATIONS AS EFFECTIVE NUTRACEUTICS
56. THE ANTIMETASTATIC EFFECT OF BACTERIOPHAGE T4* ADMINISTRATED IN COMBINED TREATMENT WITH SELECTED CYTOSTATICS IN MICE WITH B16 MELANOMA
57. SYNTHESIS AND ANTIPROLIFERATIVE ACTIVITY OF DIACETYLENIC THIOQUINOLINES
58. SYNTHESIS AND CYTOTOXIC ACTIVITY OF 10-DEACETYL-10-PROPARGILPACLITAXEL
59. THE CYTOTOXIC GLYCOSIDES OF INDOLO[2,3-B]QUINOLINE DERIVATIVES. IN VITRO AND IN VIVO STUDIES
60. MONO SUBSTITUTED 5H-INDOLO[2,3-B]- QUINOLINE DERIVATIVES AND THEIR ABILITY TO OVERCOME THE BARRIER OF DRUG RESISTANCE.
61. DISUBSTITUTED INDOLO[2,3-b]QUINOLINE DERIVATIVES. THE CYTOTOXIC ACTIVITY IN VITRO AGAINST VARIOUS HUMAN TUMOR CELL LINE.
62. ANTITUMOR EFFECT OF CISPLATIN OR FLUOROURACIL IN COMBINED TREATMENT WITH (24R)-1,24-DIHYDROXYVITA- MIN D₃
63. SYNTHESIS AND CYTOTOXIC ACTIVITY OF NEW 1-SUBSTITUTED PYRIDO[4,3-b]CARBA- ZOLE DERIVATIVES
64. FIRST ROUND STUDIES ON LEWIS LUNG CARCINOMA ACTIVITY OF THE NEW LEAD STRUCTURES IN THE ISOXAZOLE HETEROCYCLIC SYSTEM
65. CONJUGATES OF METHOTREXATE AND DEXTRANS IN MOUSE LEUKEMIA MODEL WITH MULTIPLE DOSE SCHEDULE
66. GENISTEIN, ITS NEW ANALOGS AND COMPLEXES - THE ANTIPROLIFERATIVE EFFECTS ON HL-60 LEUKEMIA CELL LINE
67. COMBINATION OF: IMATINIB, PRI-2191 AND CYTOSTATICS - THE ANTIPROLIFERATIVE EFFECTS ON HL-60 LEUKEMIA CELL LINE