Synthesis and structure-activity relationship of coumarins as potent Mcl-1 inhibitors for cancer treatment

Xia, Yangliu; Wang, Jingjing; Li, Shi-Yang; Liu, Yong; Gonzalez, Frank J.; Wang, Ping; Ge, Guang-Bo

doi:10.1016/j.bmc.2020.115851

Cited by 18 publications

(12 citation statements)

References 40 publications

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“…In human, UGT superfamily is classified into four major families: UGT1, 2, 3 and 8, of which the UGT1 and 2 families being most important for glucuronidation reactions. The substrate spectra of human UGT enzymes (particularly UGT1A members) are highly overlapped to each other 5 , 92 , 93 , 94 , 95 . Accumulating evidence indicates that UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9, UGT2B7, UGT2B10, and UGT2B15 play crucial roles in hepatic glucuronidation of xenobiotics, whereas intestinal UGT1A10 plays a pivotal role in pre-systemic clearance.…”

Section: Optical Substrates For Phase II Drug Metabolizing Enzymesmentioning

confidence: 99%

Optical substrates for drug-metabolizing enzymes: Recent advances and future perspectives

Jin

et al. 2022

Acta Pharmaceutica Sinica B

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Section: Optical Substrates For Phase II Drug Metabolizing Enzymesmentioning

confidence: 99%

Optical substrates for drug-metabolizing enzymes: Recent advances and future perspectives

Jin

et al. 2022

Acta Pharmaceutica Sinica B

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“…Coumarin‐based compounds have attracted much attention by organic/medicinal chemists and drug design scientists as a consequence of their diverse pharmacological and biological properties such as antimicrobial, 15–17 anticancer, 18–20 anti‐inflammatory, 21 antidepressant, 22 antioxidant, 23 antituberculosis, 24,25 anti‐Alzheimer, 26,27 antinociceptive, 28 anti‐edematogenic, 28 antileishmanial, 29 antiviral, 30,31 analgesic, 32 anti‐pyretic, 32,33 antimalarial, 34,35 antithrombotic, 36 antitumor, 37–39 antiretroviral, 40 anti‐coagulation, 41 antiasthmatic, 42 anti‐influenza 43 and antihyperlipidemic 44 . Moreover, some of the coumarin derivatives have been demonstrated to be potent selective human carbonic anhydrase (CA), 45 Mcl‐1, 46 SARS‐CoV‐2, 47 MAO‐B, 48 inhibition of xanthine oxidase, 49 inhibition of lipoxygenase, 50 topoisomerase IV 51 and, also DNA gyrase inhibitor 52 . Also, coumarin were widely used as additives in food, agrochemicals, perfumes, pharmaceuticals and cosmetics, 53 and also used in the preparations of insecticides, optical brightening agents, dispersed fluorescent and tunable laser dye 54 …”

Section: What Is Known and Objectivementioning

confidence: 99%

Synthetic and natural coumarins as potent anticonvulsant agents: A review with structure–activity relationship

Keri

Budagumpi

Somappa

2022

Clinical Pharmacy Therapeu

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What is known and objective:The main objective of this review is to highlight the most relevant studies since 1990 (to date) in the area of medicinal chemistry aspects to provide a panoramic view to the biologists/medicinal chemists working in this area and would assist them in their efforts to design, synthesize and extract (from natural source) coumarin-based anticonvulsant agents. Also, the structure-activity relationship (SAR) studies are also discussed for further rational design of this kind of derivatives. It is hoped that this review will be helpful for new thoughts in the quest for rational designs of more active and less toxic coumarin-based antiepileptic agents.

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“…The synthesis of compounds 7a-c and 8a-c (Fig. 2) were carried out according to the method we have published previously [19][20]. The target compounds were characterized by 1 H-nuclear magnetic resonance ( 1 H NMR), carbon nuclear magnetic resonance ( 13 C NMR) and high resolution mass spectroscopy (HRMS).…”

Section: Synthesismentioning

confidence: 99%

Design, synthesis and biological evaluation of esculetin derivatives as potential anti-HBV agents

Zhao

et al. 2022

Preprint

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A series of esculetin derivatives have been synthesized for the aim of exploring their anti-hepatitis B virus (anti-HBV) activity. In vitro anti-HBV activity was performed against HepG2.2.15 cells by using Elisa kit and cytotoxicity was determined by 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazolium bromide (MTT) assay with lamivudine as the positive control. The results demonstrated that several compounds showed moderate anti-HBV activity, while introduction of morpholine groups could significantly inhibit the expression of hepatitis B e antigen (HBeAg) and introduction of 2-methylimidazole group could significantly inhibit the expression of Hepatitis B surface antigen (HBsAg). Among all tested compounds, compound 4a demonstrated the best anti-HBeAg activity (IC50 = 15.8 ± 4.2 µM), while compound 6d demonstrated the best anti-HBsAg activity (IC50 = 21.4 ± 2.8 µM). Compounds 6b and 6c showed moderate anti-HBV activity and HBsAg inhibition. Compounds 4b showed moderate anti-HBV activity and inhibitory effect on HBeAg. In addition, compounds 4a, 4c, 4d, 6b, 6c and 6d showed improved metabolic stability. This study provides useful guidance for the discovery of anti-hbv drugs, which merits further investigation.

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Synthesis and structure-activity relationship of coumarins as potent Mcl-1 inhibitors for cancer treatment

Cited by 18 publications

References 40 publications

Optical substrates for drug-metabolizing enzymes: Recent advances and future perspectives

Optical substrates for drug-metabolizing enzymes: Recent advances and future perspectives

Synthetic and natural coumarins as potent anticonvulsant agents: A review with structure–activity relationship

Design, synthesis and biological evaluation of esculetin derivatives as potential anti-HBV agents

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