Anti-influenza activity of monoterpene-containing substituted coumarins

Khomenko, T. M.; Zarubaev, Vladimir V.; Orshanskaya, Iana R.; Kadyrova, Renata A.; Sannikova, Victoria A.; Корчагина, Д. В.; Волчо, К. П.; Salakhutdinov, N. F.

doi:10.1016/j.bmcl.2017.04.091

Cited by 37 publications

(15 citation statements)

References 29 publications

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“…In recent work they have used different electronic properties along with the topo-chemical analysis for modeling. In the present work we have used data from the work of Khomenko et al [13] This clearly indicates that this is best model for estimating predicting clogP values of the compounds in the present study, the small residue value and R 2 pred confirms the above statement.…”

Section: Resultssupporting

confidence: 82%

Anti-Influenza Activity of Monoterpene-Containing Substituted Coumarins Using Physicochemical Parameters

Kumar¹,

Kumari²

2018

Organic Chem Curr Res

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A Quantative-Structure-Activity Relationship (QSAR) study is performed on monoterpene-containing substituted coumarins, A number of highly descriptive and predictive QSAR models for these compounds were obtained by Using physicochemical parameters using stepwise-multiple linear regressions methods. Model validation is performed by incorporating training and test sets approach and calculating R2 which is equal to 0.9943 and also Regression analysis data has indicated that activity can be best modeled in multi-parametric regression.

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Section: Resultssupporting

confidence: 82%

Anti-Influenza Activity of Monoterpene-Containing Substituted Coumarins Using Physicochemical Parameters

Kumar¹,

Kumari²

2018

Organic Chem Curr Res

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“…Natural and synthetic coumarins (2H-chromen-2-one) demonstrate diverse biological activities, and are often considered as a privileged scaffold [1][2][3][4][5][6]. In particular, a large number of coumarin derivatives with high antitumor activity have been found in recent years [7][8][9][10][11][12][13][14][15][16][17][18].…”

Section: Introductionmentioning

confidence: 99%

Promising New Inhibitors of Tyrosyl-DNA Phosphodiesterase I (Tdp 1) Combining 4-Arylcoumarin and Monoterpenoid Moieties as Components of Complex Antitumor Therapy

Khomenko

Zakharenko

Chepanova

et al. 2019

IJMS

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Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is an important DNA repair enzyme in humans, and a current and promising inhibition target for the development of new chemosensitizing agents due to its ability to remove DNA damage caused by topoisomerase 1 (Top1) poisons such as topotecan and irinotecan. Herein, we report our work on the synthesis and characterization of new Tdp1 inhibitors that combine the arylcoumarin (neoflavonoid) and monoterpenoid moieties. Our results showed that they are potent Tdp1 inhibitors with IC50 values in the submicromolar range. In vivo experiments with mice revealed that compound 3ba (IC50 0.62 µM) induced a significant increase in the antitumor effect of topotecan on the Krebs-2 ascites tumor model. Our results further strengthen the argument that Tdp1 is a druggable target with the potential to be developed into a clinically-potent adjunct therapy in conjunction with Top1 poisons.

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“…[21] This compounds also demonstrate inhibition activity against influenza virus A/California/07/09 (H1 N1)pdm09. [22] The chemical modification of natural bioregulator analogs is one of the most promising methods for the synthesis of new biologically active compounds. A series of terpenophenols was previously synthesized and its structure-activity relationship was evaluated.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Biological Evaluation of Novel Coumarins withtert‐Butyl and Terpene Substituents

Попова

Шевченко

Chukicheva

et al. 2019

Chemistry & Biodiversity

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Coumarins with terpene and tert‐butyl substituents were synthesized via Pechmann condensation reaction. New derivatives were investigated in different model system for the exhibition of antioxidant, radical scavenging and membrane‐protective activities. It has been found that 4‐methylcoumarin derivatives with monoterpene moieties exhibit high antioxidant activities. The most active and promising for further investigations is 5‐hydroxy‐6,8‐diisobornyl‐4‐methylcoumarin, containing two isobornyl substituents on the benzopyran ring.

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Anti-influenza activity of monoterpene-containing substituted coumarins

Cited by 37 publications

References 29 publications

Anti-Influenza Activity of Monoterpene-Containing Substituted Coumarins Using Physicochemical Parameters

Anti-Influenza Activity of Monoterpene-Containing Substituted Coumarins Using Physicochemical Parameters

Promising New Inhibitors of Tyrosyl-DNA Phosphodiesterase I (Tdp 1) Combining 4-Arylcoumarin and Monoterpenoid Moieties as Components of Complex Antitumor Therapy

Synthesis and Biological Evaluation of Novel Coumarins withtert‐Butyl and Terpene Substituents

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