Pharmacophoric model building for antitubercular activity of the individual Schiff bases of small combinatorial library

Abdel-Aal, Wesam S.; Hassan, Hoda Y.; Aboul‐Fadl, Tarek; Youssef, Adel F.

doi:10.1016/j.ejmech.2009.12.005

Cited by 24 publications

(10 citation statements)

References 23 publications

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“…Isatins and hydrazides building blocks were obtained either commercially or synthesized along with the designed target Schiff bases according to the reported literatures [26,27,29-31]. Cytotoxicity was done at Stem Cell Therapy Program, King Faisal Specialized Hospital and Research Center, Riyadh-Saudi Arabia.…”

Section: Discussionmentioning

confidence: 99%

“…In continuation to our synthetic work on Schiff bases of isatin with potential biological activity [26-32], the current work describes the antiproliferative activity of Schiff bases of combinatorial mixtures of the isatin derivatives M1-M22 as well as the individual compounds 1-11(A-K) of these combinatorial mixtures. Moreover, Ligand based pharmacophore modeling of these Schiff bases was conducted to evaluate the common features essential for activity and the hypothetical geometries adopted by these ligands in their most active conformers were undertaken.…”

Section: Introductionmentioning

confidence: 99%

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Schiff bases of indoline-2,3-dione (isatin) with potential antiproliferative activity

Aboul‐Fadl

Radwan

Attia

et al. 2012

Chemistry Central Journal

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BackgroundCancer is one of the most dreaded diseases and it is a leading cause of mankind death worldwide. Recent reports documented a remarkable antiproliferative activity of isatin nucleus against various cancer cell lines. The current work describes the antiproliferative activity of Schiff bases of combinatorial mixtures of the isatin derivatives M1-M22 as well as the individual compounds 1-11(A-K) of these combinatorial mixtures.ResultsThe designed combinatorial library composed from eleven hydrazides A-K and eleven isatin derivatives 1-11 has been synthesized to formally generate 22 mixtures, M1-M22 of 121 Schiff bases, and their antiproliferative activity against K562 chronic myelogenous leukemia cells was evaluated. The indexed method of analysis of the prepared library was applied to elucidate the active components in the tested mixtures M1-M22. The predictions from the crossing procedure was validated through evaluation of the antiproliferative activity of individual compounds 1-11(A-K) of the library. Individual compounds 1-11(A-K) were also evaluated against the non-tumorigenic MCF-12A cell line to investigate their selectivity. A pharmacophore model was developed to further optimize the antiproliferative activity among this series of compounds.ConclusionsVariable antiproliferative activity was revealed with the investigated mixtures M1-M22 and the individual compounds 1-11(A-K). Most of the tested mixtures and several individual Schiff bases displayed high potency with IC50 values in the low micromolar range. A considerable selectivity of some individual compounds to the tumorigenic K562 cell line compared with the non-tumorigenic MCF-12A cell line was observed as indicated by their selectivity index (SI).

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Schiff bases of indoline-2,3-dione (isatin) with potential antiproliferative activity

Aboul‐Fadl

Radwan

Attia

et al. 2012

Chemistry Central Journal

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“…in applications in organic electronics and photonics (Perepichka & Perepichka, 2009) and in the medical area. In the latter context, the thiophene nucleus is present in many natural and synthetic products having a wide range of pharmacological activities, such as anti-viral (Chan et al, 2004), anti-cancer (Romagnoli et al, 2011), anti-bacterial (Sivadas et al, 2011;Jain et al, 2012), anti-fungal (Jain et al, 2012;Saeed et al, 2010), anti-inflammatory (Kumar et al, 2004) and anti-microbial and anti-tuberculosis (anti-TB) activities (Abdel-Aal et al, 2010). Our interests in the biological activities and structural chemistry of heterocyclic compounds have led us to investigate thiophene and its derivatives as tuberculostatic agents.…”

Section: Chemical Contextmentioning

confidence: 99%

N′-[(1E)-(5-Nitrofuran-2-yl)methylidene]thiophene-2-carbohydrazide: crystal structure and Hirshfeld surface analysis

et al. 2016

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“…In the last two decades it is estimated that 2500 secondary metabolite compounds from marine biota and symbionts have been isolated and identified, and as many as 353 of them are thought to have potential as new anti-bacterial ingredients. Extracts of secondary metabolites from marine algae contain bioactive compounds which are known to have pharmacological properties such as: antibacterial 1 antimalarials and anti-tuberculosis 2,3,4,5 . So far there has been very little or no research data that explores groups of protein compounds from marine algae and symbiotic bacteria as raw material for anti-bacterial drugs, although there have been many reported antimicrobial agents of protein and peptide compounds from other organisms 6,7,8 .…”

Section: Introductionmentioning

confidence: 99%

Purification and Gene Cloning of a Novel Antibacterial L-Asparaginase of the Endophytic Microsymbiont Algae Sargassum Sp. From Cikoang Island, Indonesian Territory

Karim¹,

Arfah²,

Karim³

et al. 2019

Int. Res. J. Pharm.

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Endophytic bacterial symbiont algae are an environmentally potential source of various bioactive compounds that can be used as raw material for drugs. A new anti-bacterial L-asparaginase (L-ASNase) has been purified from the endophytic bacterial symbiont algae Sargassum sp. by using ammonium sulphate fractionation, followed by dialysis, column chromatography and reversed-phase HPLC, and behaves as a single-band on SDS-PAGE with molecular weight of 39 kDa. Based on amino acids partial sequence, we cloned and sequenced cDNA encoding L-ASNase.The cDNA of L-ASNase gene consists of 843 nucleotides encoding 280 amino acid residues including a putative initiation Met. To obtain it in large amounts, the coding sequence of L-ASNase was cloned into pGEX-2TK vector to yield recombinant plasmid pGEX-2TK-L-ASNase cDNA and expressed as an L-ASNase fusion protein in Escherichia coli BL21 strain. The soluble fusion protein collected from the supernatant of the cell lysate after lysis by ultrasonication was purified by a single-step chromatography on glutathione agarose beads. The purified native L-ASNase protein and recombinant L-ASNase fusion protein was determinated for a novel anti-bacterial activity. Recombinant L-ASNase fusion protein exhibited a similar anti-bacterial activity to the native L-ASNase. The recombinant L-ASNase had stronger anti-bacterial activity toward Staphylococus aureus (G + ) with the diameters of inhibition zone 2.5 times more than that from Vibrio cholerae (G -) with the same protein product. This research might provide a significant supporting for the following research on the anti-bacterial action and mechanism in cellular and molecular level of L-ASNase protein from endophytic bacterial symbiont algae Sargassum sp.

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Pharmacophoric model building for antitubercular activity of the individual Schiff bases of small combinatorial library

Cited by 24 publications

References 23 publications

Schiff bases of indoline-2,3-dione (isatin) with potential antiproliferative activity

Schiff bases of indoline-2,3-dione (isatin) with potential antiproliferative activity

N′-[(1E)-(5-Nitrofuran-2-yl)methylidene]thiophene-2-carbohydrazide: crystal structure and Hirshfeld surface analysis

Purification and Gene Cloning of a Novel Antibacterial L-Asparaginase of the Endophytic Microsymbiont Algae Sargassum Sp. From Cikoang Island, Indonesian Territory

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