N6-Дипептидные производныеN12-рибозил-индоло[2,3-a]карбазола

Горюнова, О. В.; Захарчук, Г. М.; Zhukova, O. S.; Фетисова, Л. В.; Кузьмина, Н. Е.

doi:10.7868/s0132342314010047

Cited by 2 publications

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“…Метильная группа при атоме азота индола [11] или при имидном азоте [10] усиливает в ряде случаев цитотоксическую активность соединения. Следует отметить, что в структурах описанных производных индоло [2,3-а] пирроло [3,4-с] карбазола преобладают низкомолекулярные группы заместителей, а, например, молекулы, содержащие пептидные остатки или аминокислоты, представлены лишь в некоторых публикациях [11][12][13][14].…”

Section: оригинальные статьиunclassified

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

Apryshko¹,

Zhukova²,

Фетисова³

et al. 2017

Rossijskij bioterapevtičeskij žurnal

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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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Section: оригинальные статьиunclassified

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

Apryshko¹,

Zhukova²,

Фетисова³

et al. 2017

Rossijskij bioterapevtičeskij žurnal

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“…В настоящее время за рубежом проходят II-III фазы клинических испытаний N-гликозилированных производных индоло [2,3-а]пироло [3,4-с]карбазола [3], в которых гетероциклическая часть препарата обусловливает его противоопухолевые свойства, а заместители, в том числе углеводный остаток, модулируют растворимость и пути фармакокинетического продвижения лекарства в организме. Добавление в структуру молекулы индоло [2,3-а] пироло [3,4-с]карбазола остатков аминокислот или пептидов [4][5][6] способно значительно видоизменить фармакокинетические свойства таких про изводных индолокарбазолов, что определяется биологической активностью введенных компонентов, участвующих в важнейших процессах энергообмена в клетке. Аминокислотные производные гликозидов индолокарбазола (АПГИК) были синтезированы в лаборатории химического синтеза ФГБУ «НМИЦ онкологии им.…”

Section: Introductionunclassified

Comparative in vivo studying of potential antineoplastic properties among of amino-acid derivative glycosides of the indolocarbazole (detailed report)

Голубева

Горюнова

Яворская

2018

Rossijskij bioterapevtičeskij žurnal

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Introduction.The existence of the active metabolite (amino acid) residue in the of an indolocarbazole molecule changes physical-chemical and pro-medicinal properties of aminoacid derivatives glycosides of indolocarbazole. The computer method has earlier foretold low probability of their cytotoxic activity in vitro that was confirmed in the MTT-test on 5 lines of tumor cells. The same computer method predicted significant probability of antineoplastic activity of aminoacid derivatives glycosides of indolocarbazole in vivo that demands the experimental check. Purpose of the study– assessment of aminoacid derivatives glycosides of indolocarbazole as potential antitumor medications.Materials and methods.The research of antineoplastic activity of aminoacid derivatives glycosides of indolocarbazole was performed on mice tumoral models – cervical cancer СС5. Abdominal injections were made to CBA/Lac mice 5 times a day with 24 h interval. Observation of animals was continued till their death. The antineoplastic effect of medicines was estimated according to tumor growth inhibition, increase in life expectancy of experiental mice in comparison with control animals.Results.The optimum dose for this number of compounds, equal to 100 mg/kg is titrated. The antineoplastic activity of aminoacid derivatives glycosides of indolocarbazole on the model СС5 is estimated.Conclusions.On the basis of the obtained data the expanded research of antineoplastic properties of the selected 5 aminoacid derivatives glycosides of indolocarbazole is supposed to perform in vivo.

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N6-Дипептидные производныеN12-рибозил-индоло[2,3-a]карбазола

Cited by 2 publications

References 0 publications

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

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

Comparative in vivo studying of potential antineoplastic properties among of amino-acid derivative glycosides of the indolocarbazole (detailed report)

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