Journal ArticleDOI
3,3-diaryl-1,3-dihydroindol-2-ones as antiproliferatives mediated by translation initiation inhibition.
Amarnath Natarajan,Yun Hua Fan,Han Chen,Yuhong Guo,Julia Iyasere,Frederick Harbinski,W. J. Christ,Huseyin Aktas,Jose A. Halperin +8 more
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TLDR
The diphenyloxindole showed mechanism-specific antiproliferative activity that was comparable to known translation initiation inhibitors such as clotrimazole or troglitazone and identified as a lead compound for Ca2+-depletion-mediated inhibition of translation initiation.Abstract:
A series of substituted 3,3-diphenyl-1,3-dihydro-indol-2-ones was synthesized from the corresponding isatins. The compounds were studied for cell growth inhibition mediated by partial depletion of intracellular Ca2+ stores that leads to phosphorylation of eIF2α. The diphenyloxindole (1) showed mechanism-specific antiproliferative activity that was comparable to known translation initiation inhibitors such as clotrimazole or troglitazone. SAR studies identified m‘-tert-butyl and o-hydroxy substituted diphenyloxindole (25) as a lead compound for Ca2+-depletion-mediated inhibition of translation initiation.read more
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Synthetic methodologies of achiral diarylmethanols, diaryl and triarylmethanes (TRAMs) and medicinal properties of diaryl and triarylmethanes-an overview
Sankalan Mondal,Gautam Panda +1 more
TL;DR: In this paper, the authors present a comprehensive review of achiral diarylmethanols, diaryl and triarylmethanes and the molecules derived thereof in the last fifteen years (1995-2013).
Journal ArticleDOI
In vitro cytotoxicity evaluation of some substituted isatin derivatives.
Kara L. Vine,Julie M. Locke,Marie Ranson,Kirsten Benkendorff,Stephen G. Pyne,John B. Bremner +5 more
TL;DR: Results indicate that di- and tri-substituted isatins may be useful leads for anticancer drug development in the future.
Journal ArticleDOI
Rhodium-catalyzed addition of arylboronic acids to isatins: an entry to diversity in 3-aryl-3-hydroxyoxindoles.
Patrick Y. Toullec,Richard B. C. Jagt,Johannes G. de Vries,Ben L. Feringa,Adriaan J. Minnaard +4 more
TL;DR: A general method for the catalytic 1,2-addition of aryl and alkenyl boronic acids to isatins is described using a rhodium(I)/triphenylphosphite catalyst and allows the synthesis of a variety of 3-aryl-3-hydroxyoxindole building blocks in high yields.
Journal ArticleDOI
Facile synthesis of 3,3-di(heteroaryl)indolin-2-one derivatives catalyzed by ceric ammonium nitrate (CAN) under ultrasound irradiation
Shun-Yi Wang,Shun-Jun Ji +1 more
TL;DR: Ceric ammonium nitrate efficiently catalyzes the reaction of isatin with indoles under sonic waves to afford symmetric 3,3-di(indolyl)indolin-2-ones in excellent yields.
Journal ArticleDOI
Asymmetric organocatalysis: an enabling technology for medicinal chemistry
TL;DR: A comprehensive overview of the applications of asymmetric organocatalysis in medicinal chemistry can be found in this article, with a focus on the preparation of antiviral, anticancer, neuroprotective, cardiovascular, antibacterial, and antiparasitic agents, as well as several miscellaneous bioactive agents.
References
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Journal ArticleDOI
Structural features in eukaryotic mRNAs that modulate the initiation of translation.
TL;DR: In higher eukaryotes, translation is modulated at the level of initiation by five aspects of mRNA structure: (i) the m7G cap; (ii) the primary sequence or context surrounding the AUG codon; (iii) the position of the Aug codon, i.e. whether or not it s “first”; (iv) secondary structure both upstream and downstream from the AUU; and (v) leader length.
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An analysis of vertebrate mRNA sequences: intimations of translational control.
TL;DR: In this paper, structural features in mRNAs have been found to contribute to the fidelity and efficiency of initiation by eukaryotic ribosomes, and it was suggested that throttling at the level of translation may be a critical component of gene regulation in vertebrates.
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Ras links growth factor signaling to the cell cycle machinery via regulation of cyclin D1 and the Cdk inhibitor p27KIP1.
TL;DR: It is reported here that Ras proteins play a key role in integrating mitogenic signals with cell cycle progression through G1, and regulation of cyclin D1 is a critical target of the Ras signaling cascade.
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Clotrimazole inhibits cell proliferation in vitro and in vivo
TL;DR: Modulation of early ionic mitogenic signals and potent inhibition of cell proliferation both in vitro and in vivo are new and potentially useful clinical effects of CLT.
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Preparation of 3,3-Diaryloxindoles by Superacid-Induced Condensations of Isatins and Aromatics with a Combinatorial Approach
TL;DR: In this article, isatin, benzene, and acid systems of varying strength (composed of CF3SO3H and CF3CO2H) were evaluated for 3,3-Diaryloxidoles.