Journal ArticleDOI
Synthesis, Biological Evaluation, and Quantitative Structure−Activity Relationship Analysis of New Schiff Bases of Hydroxysemicarbazide as Potential Antitumor Agents†
Shijun Ren,Rubin Wang,Kenichi Komatsu,Patricia Bonaz-Krause,Yegor Zyrianov,Charles E. McKenna,Csaba Csipke,Zoltán A. Tökés,Eric J. Lien +8 more
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TLDR
Quantitative structure-activity relationship (QSAR) analysis showed that, besides the essential pharmacophore (-NHCONHOH), hydrophobicity, molecular size/polarizability, and the presence of an oxygen-containing group at the ortho position (I) were important determinants for the antitumor activities.Abstract:
Thirty Schiff bases of hydroxysemicarbazide (Ar−CHNNHCONHOH) have been synthesized and tested against L1210 murine leukemia cells. The IC50 values were found to be in a range from 2.7 × 10-6 to 9.4 × 10-4 M. A total of 17 out of the 30 compounds had higher inhibitory activities than hydroxyurea (an anticancer drug currently used for the treatment of melanoma, leukemia, and ovarian cancer) against L1210 cells. Six compounds with IC50 values in micromolar range were 11- to 30-fold more potent than hydroxyurea (IC50 = 8.2 × 10-5 M). The partition coefficient (log P) and ionization constants (pKa) of a model compound [1-(3-trifluoromethylbenzylidene)-4-hydroxysemicarbazide, 1] were measured by the shake-flask method, and the measured log P was used to derive Hansch−Fujita π constant of −CHNNHCONHOH. On the basis of the newly derived π and those of other moieties, the partition coefficients (SlogP) of the other 29 compounds were calculated by the summation of π values. Quantitative structure−activity relations...read more
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Ribonucleotide reductase inhibitors and future drug design.
TL;DR: The discovery of p53R2, a p53-inducible form of the small subunit of RR, raises the interest to develop subunit-specific RR inhibitors for cancer treatment, and compiles recent studies on the structure, function, and regulation of two forms of RR.
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A Series of α-Heterocyclic Carboxaldehyde Thiosemicarbazones Inhibit Topoisomerase IIα Catalytic Activity
He Huang,Qin Chen,Xin Ku,Linghua Meng,Liping Lin,Xiang Wang,Caihua Zhu,Yi Wang,Zhi Chen,Ming Li,Hualiang Jiang,Kaixian Chen,Jian Ding,Hong Liu +13 more
TL;DR: Results about the mechanisms involved in the anticancer activities of thiosemicarbazones will aid in the rational design of novel topoisomerase II-targeted drugs and will provide insights into the discovery and development of novel cancer therapeutics based on the dual activity to chelate iron and to inhibit the catalytic activity of topoisomersase IIalpha.
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A review on applications of chitosan-based Schiff bases.
TL;DR: The biological applications of CSBs including antimicrobial activity, anticancer activity, drug carrier ability, antioxidant activity and tissue engineering capacity are discussed and the applications in other fields such as catalysis, adsorption and sensors are demonstrated.
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An insight into synthetic Schiff bases revealing antiproliferative activities in vitro.
TL;DR: This work has focussed its attention on the collected synthetic simple Schiff bases of aldimine- and ketIMine-types revealing anticancer activities in vitro, that have been described in the scientific literature during the last decade, and on structural variations whose affect the antiproliferative activity in sets of the designed molecules.
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Synthesis and characterization of Co(II), Ni(II), Cu(II) and Zn(II) complexes of tridentate Schiff base derived from vanillin and dl-α-aminobutyric acid
TL;DR: In this paper, the Schiff base derived from vanillin and dl-alpha-aminobutyric acid was synthesized and characterized by elemental analysis, IR, electronic spectra, conductance measurements, magnetic measurements, powder XRD and biological activity.
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TL;DR: The preliminary studies with methotrexate-resistant L1210 cells indicates that cross resistance is increased in the case of moderate-sized, hydrophilic drugs, and suggests that current chemotherapy regimens may be improved by treating resistant cells with antineoplastic agents displaying physicochemical characteristics opposite to that of the original inducing agent.
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Is there tissue penetration after application of topical salicylate formulations
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Inhibition of nucleoside diphosphate reductase by hydroxybenzohydroxamic acid derivatives
Howard L. Elford,Bart van’t Riet +1 more
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Multivariate quantitative structure-pharmacokinetic relationships (QSPKR) analysis of adenosine A1 receptor agonists in rat.
TL;DR: A multivariate 3D QSPKR model is developed that could adequately predict overall pharmacokinetic behavior of adenosine A1 receptor agonists in rat and can also be used for other classes of compounds.
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Phase II trial of didox in advanced breast cancer. Cancer Research Campaign Phase I/II Clinical Trials Committee.
TL;DR: Fourteen patients with advanced breast cancer were treated with the ribonucleotide reductase inhibitor didox 6 g m-2 given by intravenous infusion over 36 h every 3 weeks, and none responded and toxicity was minimal.