Simple indole alkaloids and those with a nonrearranged monoterpenoid unit (1999)

Hibino, Satoshi; Choshi, Tominari

doi:10.1039/b004055j

Cited by 218 publications

(39 citation statements)

References 82 publications

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“…The addition of alcohols had an interesting effect, MeOH inhibits the reaction, while when iPrOH or tBuOH were added the enantiomeric ratio decreased slightly. Finally, when Ti(OiPr) 4 was used as an additive, the corresponding tertiary alcohol 2a was obtained with very low enantioselectivity (entry 10). Therefore, we decided as optimized reaction conditions the ones presented in entry 6, Table 2.…”

Section: Resultsmentioning

confidence: 99%

“…This scaffold is present in a large variety of natural and synthetic compounds that exhibit pharmaceutical properties [1][2][3][4][5][6][7][8]. Structure-activity relationship studies have shown that the biological activities of these compounds are significantly affected both by the configuration of the C3 and its substitution pattern [9][10][11].…”

Section: Introductionmentioning

confidence: 99%

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Catalytic Enantioselective Addition of Me2Zn to Isatins

et al. 2017

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Catalytic Enantioselective Addition of Me2Zn to Isatins

et al. 2017

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“…Bis(indolyl)methanes (BIMs) are one of the most important groups of indole derivatives that are found in cruciferous plants and marine sources [2]. These compounds have shown different pharmaceutical activities such as anticancer [3], antihyperglycemic, antiviral, and antimicrobial [4], and antioxidant [5] properties. They are also known as a promoter of estrogen metabolism [6] and induce apoptosis in human cancer cells [7].…”

Section: Introductionmentioning

confidence: 99%

A domino electro-oxidative synthesis of 3,3′-bis(indolyl)methane nanoparticles

Nikoofar

Ghanbari

2015

Monatsh Chem

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An effective route for electro-oxidative synthesis of 3,3 0 -bis(indolyl)methane nanoparticles has been described via a domino multi-component reaction between various alcohols and indole derivatives in an undivided cell under constant potential conditions in CH 3 CN at room temperature. The mechanistic aspect of this electro-oxidative condensation has also been studied by UV-Vis spectra and cyclic voltammograms. The nanostructure of the products has been confirmed by scanning electron microscopy. Graphical abstract N H N -OH O --2e + ,-2H -+1e N H N H Carbon anode Carbon cathod

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“…Among them, the nitrogenous heterocyclic 4-(3H)-quinazolinones and substituted quinazolines represent a very important class of drugs with several biological properties, such as anticancer [11], diuretic [12], anti-inflammatory [13], anti-convulsant [14] and anti-hypertensive [15] activities.…”

Section: Quinazolinesmentioning

confidence: 99%

In <i>Silico</i> Pharmacokinetics Studies for Quinazolines Proposed as EGFR Inhibitors

Fernandes¹,

Pereira²,

Marinho³

et al. 2015

OJMC

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In silico pharmacokinetics studies can aid the search for molecules with potential ability to be drug candidates. In this paper, a number of quinazoline candidates for epidermal growth factor receptor inhibitors-EGFR, important targets for the treatment of cancer, are computationally analyzed. The literature described that 69 quinazoline molecules were synthesized and the respective half maximum inhibitory concentrations (IC50) were obtained. A bilinear parabolic model was built to investigate the druglikeness by correlating the corresponding lipophilicities, which can be represented by the ideal Log P, with the optimal biological activity in terms of pIC50 values. Structural characteristics leading to improved pharmacokinetics parameters were then analyzed. Compound 56 exhibited the lowest IC50 and, therefore, it had the highest ability to inhibit the EGFR. In the present work, the most potent inhibitor 56 is not calculated to be the most promising drug candidate, since it's out of the parabolic model obtained due to a Log P above 5, which is not within the expected optimum range. Finally, this work is an example of computational prediction that an experimentally, highly active EGFR inhibitor can be unsuccessful as drug candidate because of pitfalls in pharmacokinetics parameters.

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Simple indole alkaloids and those with a nonrearranged monoterpenoid unit (1999)

Cited by 218 publications

References 82 publications

Catalytic Enantioselective Addition of Me2Zn to Isatins

Catalytic Enantioselective Addition of Me2Zn to Isatins

A domino electro-oxidative synthesis of 3,3′-bis(indolyl)methane nanoparticles

In <i>Silico</i> Pharmacokinetics Studies for Quinazolines Proposed as EGFR Inhibitors

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Simple indole alkaloids and those with a nonrearranged monoterpenoid unit (1999)

Cited by 218 publications

References 82 publications

Catalytic Enantioselective Addition of Me2Zn to Isatins

Catalytic Enantioselective Addition of Me2Zn to Isatins

A domino electro-oxidative synthesis of 3,3′-bis(indolyl)methane nanoparticles

In &lt;i&gt;Silico&lt;/i&gt; Pharmacokinetics Studies for Quinazolines Proposed as EGFR Inhibitors

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In <i>Silico</i> Pharmacokinetics Studies for Quinazolines Proposed as EGFR Inhibitors