Synthesis, antimicrobial, anticancer evaluation and QSAR studies of 6-methyl-4-[1-(2-substituted-phenylamino-acetyl)-1H-indol-3-yl]-2-oxo/thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid ethyl esters

Sharma, Sohan Lal; Kumar, Pradeep; Narasimhan, Balasubramanian; Ramasamy, Kalavathy; Mani, Vasudevan; Mishra, Rakesh K.; Majeed, Abu Bakar Abdul

doi:10.1016/j.ejmech.2011.11.028

Cited by 55 publications

(21 citation statements)

References 28 publications

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“…On the other hand electron-releasing groups located on the phenylamino moiety increased the anticancer activity against the MCF-7 cancer cell line. Also, the existence of an oxo moiety at the C-2 position of the tetrahydropyrimidine ring improved the anticancer activity against both tested cell lines, although a thioxo moiety did not significantly improve the anticancer activity (146).…”

Section: Anticancer Activitymentioning

confidence: 89%

Hantzsch-Type Dihydropyridines and Biginelli-Type Tetra-hydropyrimidines: A Review of their Chemotherapeutic Activities

Sepehri¹,

Sánchez²,

Fassihi³

2015

J Pharm Pharm Sci

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Years after the first report on 1,4-dihydropyridines (1,4-DHPs) and 1,2,3,4-tetrahydropyrimidines (1,2,3,4-THPMs) appeared, they are revisited as plausible therapeutic agents. This is mainly due to the convenient methods that exist for their synthesis and the diverse pharmacologic properties that these scaffolds present. 1,4-Dihydropyridines and 1,2,3,4-tetrahydropyrimidines are usually regarded as analogous in several aspects. They are both prepared in multi-component reactions using very similar starting materials and synthesis protocols. This leads to common structural features between 1,4-DHPs and 1,2,3,4-THPMs, as well several related biological effects. For example, they share many pharmacological features such as analgesic, anti-tumor, antioxidant, anti-inflammatory, antitubercular, antibacterial, cardiovascular and adrenoceptor blocking activities. Numerous reviews have been devoted to the chemistry and cardiovascular effects of these compounds. However, the lack of a comprehensive literature overview on the chemotherapeutic ability of these scaffolds is behind the present attempt to provide a detailed survey of 1,4-DHPs and 1,2,3,4-THPMs and their structural features as chemotherapeutic agents.This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

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Section: Anticancer Activitymentioning

confidence: 89%

Hantzsch-Type Dihydropyridines and Biginelli-Type Tetra-hydropyrimidines: A Review of their Chemotherapeutic Activities

Sepehri¹,

Sánchez²,

Fassihi³

2015

J Pharm Pharm Sci

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“…However, very recently the interest has been increased in the development of multi-target QSAR (mt-QSAR) models (Sigroha et al 2012;Sharma et al 2012;Kumar et al 2010). In opposition to ot-QSAR, the mt-QSAR model is a single equation that considers the nature of molecular descriptors which are common and essential for describing the antibacterial and antifungal activities.…”

Section: -32 O Coclmentioning

confidence: 99%

“…In opposition to ot-QSAR, the mt-QSAR model is a single equation that considers the nature of molecular descriptors which are common and essential for describing the antibacterial and antifungal activities. Based on the facts mentioned above and in continuation of our research in the field of mt-QSAR (Sigroha et al 2012;Sharma et al 2012;Kumar et al 2010), we have attempted to develop three different types of mt-QSAR models viz. mt-QSAR model for describing antibacterial activity of synthesized compounds against S. aureus, B. subtilis and E. coli, mt-QSAR model for describing antifungal activity of synthesized compounds against C. albicans and A. niger as well a common mt-QSAR model for describing the antimicrobial (overall antibacterial and antifungal) activity of isatin derivatives against all the above mentioned microorganisms.…”

Section: -32 O Coclmentioning

confidence: 99%

Synthesis, antimicrobial, anticancer, antiviral evaluation and QSAR studies of 4-(1-aryl-2-oxo-1,2-dihydro-indol-3-ylideneamino)-N-substituted benzene sulfonamides

Kumar

Ramasamy

Mani

et al. 2014

Arabian Journal of Chemistry

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A series of 4-(1-aryl-2-oxo-1,2-dihydro-indol-3-ylideneamino)-N-substituted benzenesulfonamide derivatives (1-32) was synthesized and evaluated for its in vitro antimicrobial, antiviral and cytotoxic activities. Antimicrobial results indicated that compounds (11) and (18) were found to be the most effective ones. In general, the synthesized compounds were bacteriostatic and fungistatic in their action. The cytotoxic screening results indicated that the compounds were less active than the standard drug 5-fluorouracil (5-FU). None of the compounds inhibited viral replication at subtoxic concentrations. In general, the presence of a pyrimidine ring with electron releasing groups and an ortho-and para-substituted benzoyl moiety favored antimicrobial activities. The results of

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“…The presence of the carboxamide moiety at positions 2 and 3 has led to the activity of these compounds tend to inhibit various enzymes and proteins. Many studies have been done in this regard, and various properties such as anticancer [6], antimalarial [7], anti-inflammatory [8], anti-diabetic [9][10][11], antimicrobial [12], antitubercular [13], antibacterial [14] and cytotoxic [7] have been reported, for indole derivatives.…”

Section: Introductionmentioning

confidence: 99%

Synthetic strategies, SAR studies, and computer modeling of indole 2 and 3-carboxamides as the strong enzyme inhibitors: a review

Chehardoli

Bahmani

2020

Mol Divers

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Indole derivatives have been the focus of many researchers in the study of pharmaceutical compounds for many years. Researchers have investigated the effect of carboxamide moiety at positions 2 and 3, giving unique inhibitory properties to these compounds. The presence of carboxamide moiety in indole derivatives causes hydrogen bonds with a variety of enzymes and proteins, which in many cases, inhibits their activity. In this review, synthetic strategies of indole 2 and 3-carboxamide derivatives, the type, and mode of interaction of these derivatives against HLGP, HIV-1, renin enzyme, and structure-activity studies of these compounds were investigated. It is hoped that indole scaffolds will be tested in the future for maximum activity in pharmacological compounds.

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Synthesis, antimicrobial, anticancer evaluation and QSAR studies of 6-methyl-4-[1-(2-substituted-phenylamino-acetyl)-1H-indol-3-yl]-2-oxo/thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid ethyl esters

Cited by 55 publications

References 28 publications

Hantzsch-Type Dihydropyridines and Biginelli-Type Tetra-hydropyrimidines: A Review of their Chemotherapeutic Activities

Hantzsch-Type Dihydropyridines and Biginelli-Type Tetra-hydropyrimidines: A Review of their Chemotherapeutic Activities

Synthesis, antimicrobial, anticancer, antiviral evaluation and QSAR studies of 4-(1-aryl-2-oxo-1,2-dihydro-indol-3-ylideneamino)-N-substituted benzene sulfonamides

Synthetic strategies, SAR studies, and computer modeling of indole 2 and 3-carboxamides as the strong enzyme inhibitors: a review

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