ChemInform Abstract: AMINO ACID AND DIPEPTIDE DERIVATIVES OF DAUNORUBICIN. 2. CELLULAR PHARMACOLOGY AND ANTITUMOR ACTIVITY OF L1210 LEUKEMIC CELLS IN VITRO AND IN VIVO

Background. The addition of active metabolites (in particular, amino acids) to the molecule affects the physicochemical and prodrug properties of derivatives of indolocarbazoles. Using computed chemoinformatics, probability antitumor activity of amino-acid derivatives of glycosides of indolocarbazol (AADGI) is predicted with low probability of their cytotoxic activity in vitro. Based on these data, a study of these compounds in vivo is conducted. Objective: the assessment of AADGI as potential antitumor medications. Materials and methods. Research antitumor activity of AADGI was done using murine tumor models - cervical cancer CC-5. Investigated compounds were injected to mice СВА abdominally 5-times daily with interval of 24 h. Observation of animals were continued till their death. Antitumor effect of compounds was assessed by criteria of tumor growth inhibition and increase in life expectancy of mice comparing to control animals. Results. The optimal dose for these series of compounds was titrated and this dose is 100 mg/kg. Antitumor activity of AADGI was assessed on CC-5. Conclusions. Based on data received we suggest an extended study in vivo of antitumor qualities of selected 5 leader AADGI.

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Synthesis, in vitro and in vivo antitumor activity of symmetrical bis-Schiff base derivatives of isatin

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2013.04.040 ◽

2014 ◽

Vol 74 ◽

pp. 742-750 ◽

Cited By ~ 57

Author(s):

Chengyuan Liang ◽

Juan Xia ◽

Dong Lei ◽

Xiang Li ◽

Qizheng Yao ◽

...

Keyword(s):

Schiff Base ◽

Antitumor Activity ◽

Schiff Base Derivatives ◽

In Vivo Antitumor Activity ◽

Derivatives Of

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Macrophage Antitumor Activity Induced by the Antigenic Lymphoma L5178Y/DTIC Subline

Tumori Journal ◽

10.1177/030089168206800502 ◽

1982 ◽

Vol 68 (5) ◽

pp. 365-371 ◽

Cited By ~ 3

Author(s):

Ornella Marelli ◽

Alberto Mantovani ◽

Paola Franco ◽

Angelo Nicotin

Keyword(s):

Antitumor Activity ◽

Tumor Cell ◽

Tumor Cells ◽

Peritoneal Macrophages ◽

Leukemic Cells ◽

Target Cells ◽

Tumor Target ◽

Growth Inhibitory

Murine leukemic cells, after in vivo treatment with antineoplastic drugs, have been shown to express new antigenic specificities that were not detectable on parental cells and that were heritable after the withdrawal of drug treatment. A study was conducted of macrophage antitumor activity triggered by LY/DTIC cells, a subline of LY murine lymphoma, antigenically altered by the drug DTIC. In vitro non-specific inhibition of tumor cell growth was exhibited by spleen and peritoneal macrophages from mice previously challenged with viable LY/DTIC. Peritoneal macrophages from LY/DTIC immune animals showed moderate, although significant lytic activity against unrelated tumor target cells. Supernatants from mixed lymphocyte-tumor cell cultures, in which LY/DTIC immune lymphocytes and LY/DTIC tumor cells had been cultured, rendered normal macrophages non-specifically growth inhibitory for tumor cells.

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Highly water-soluble derivatives of the anesthetic agent propofol: in vitro and in vivo evaluation of cyclic amino acid esters

European Journal of Pharmaceutical Sciences ◽

10.1016/s0928-0987(03)00161-1 ◽

2003 ◽

Vol 20 (1) ◽

pp. 17-26 ◽

Cited By ~ 24

Author(s):

Cosimo Altomare ◽

Giuseppe Trapani ◽

Andrea Latrofa ◽

Mariangela Serra ◽

Enrico Sanna ◽

...

Keyword(s):

Amino Acid ◽

Water Soluble ◽

Anesthetic Agent ◽

Amino Acid Esters ◽

In Vivo Evaluation ◽

Derivatives Of ◽

Acid Esters

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Antitumor activity of derivatives of neplanocin A in vivo and in vitro.

Journal of Pharmacobio-Dynamics ◽

10.1248/bpb1978.9.202 ◽

1986 ◽

Vol 9 (2) ◽

pp. 202-206 ◽

Cited By ~ 10

Author(s):

AKIO HOSHI ◽

MITSUZI YOSHIDA ◽

MASAAKI IIGO ◽

REIKO TOKUZEN ◽

KIYOFUMI FUKUKAWA ◽

...

Keyword(s):

Antitumor Activity ◽

Neplanocin A ◽

Derivatives Of

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Synthesis and Anti-Hepatocarcinoma Effect of Amino Acid Derivatives of Pyxinol and Ocotillol

Molecules ◽

10.3390/molecules26040780 ◽

2021 ◽

Vol 26 (4) ◽

pp. 780

Author(s):

Ying Zhang ◽

Hui Yu ◽

Shuzheng Fu ◽

Luying Tan ◽

Junli Liu ◽

...

Keyword(s):

Amino Acid ◽

Human Cancer ◽

Ultra Performance Liquid Chromatography ◽

Amino Acid Derivatives ◽

Flight Mass Spectrometry ◽

Liver And Kidney ◽

Derivatives Of ◽

Cancer Activity

Aiming at seeking an effective anti-hepatocarcinoma drug with low toxicity, a total of 24 amino acid derivatives (20 new along with 4 known derivatives) of two active ocotillol-type sapogenins (pyxinol and ocotillol) were synthesized. Both in vitro and in vivo anti-hepatocarcinoma effects of derivatives were evaluated. At first, the HepG2 human cancer cell was employed to evaluate the anti-cancer activity. Most of the derivatives showed obvious enhanced activity compared with pyxinol or ocotillol. Among them, compound 2e displayed the most excellent activity with an IC50 value of 11.26 ± 0.43 µM. Next, H22 hepatoma-bearing mice were used to further evaluate the anti-liver cancer activity of compound 2e. It was revealed that the growth of H22 transplanted tumor was significantly inhibited when treated with compound 2e or compound 2e combined with cyclophosphamide (CTX) (p < 0.05, p < 0.01), and the inhibition rates of tumor growth were 35.32% and 55.30%, respectively. More importantly, compound 2e caused limited damage to liver and kidney in contrast with CTX causing significant toxicity. Finally, the latent mechanism of compound 2e was explored by serum and liver metabolomics based on ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS) technology. A total of 21 potential metabolites involved in 8 pathways were identified. These results suggest that compound 2e is a promising agent for anti-hepato-carcinoma, and that it also could be used in combination with CTX to increase efficiency and to reduce toxicity.

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In silico and in vitro research of potential antineoplastic amino acid derivatives of indolocarbazol glycosides properties

Russian Journal of Biotherapy ◽

10.17650/1726-9784-2017-16-4-46-54 ◽

2017 ◽

Vol 16 (4) ◽

pp. 46-54 ◽

Cited By ~ 2

Author(s):

G. N. Apryshko ◽

O. S. Zhukova ◽

L. V. Fetisova ◽

N. K. Vlasenkova ◽

R. B. Pugacheva ◽

...

Keyword(s):

Amino Acid ◽

Antitumor Activity ◽

Cytotoxic Activity ◽

Cell Lines ◽

Molecular Descriptors ◽

Human Tumor ◽

Amino Acid Derivatives ◽

Computer Methods ◽

Derivatives Of

Objective: to evaluate the prospects of the glycosides of indolocarbazole containing amino acid residues as potential antitumor compounds. Materials and methods. For 32 compounds by structural formulas using the methods of chemoinformatics, a number of molecular descriptors and the probability of manifestation of various types of biological activity were calculated, the cytotoxic activity was evaluated in vitro by methylthiazole tetrazolium (MTT) assay using five human tumor cell lines. Results. For the studied amino acid derivatives of glycosides of indolocarbazole, a high probability of antitumor activity with a low probability of cytotoxic activity in vitro is predicted by computer method. Low cytotoxic activity was confirmed in the MTT test on 5 cell lines. Computer methods were used to predict the mechanisms of possible antitumor activity and to calculate a number of molecular descriptors that are important for the qualification of substances as potential drugs. Conclusion. It is expedient to study the antitumor activity of amino-acid derivatives of glycosides of indolocarbazole in experiments on animals with transplanted tumors.

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