Author
Louis A. Watanabe
Bio: Louis A. Watanabe is an academic researcher from Kyushu Institute of Technology. The author has contributed to research in topics: Amino acid & Hydroxamic acid. The author has an hindex of 4, co-authored 9 publications receiving 112 citations.
Papers
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TL;DR: An efficient and convenient synthesis of both enantiomers of pipecolic acid has been developed using the intramolecular cyclization of 2-amino-6-bromohexanoic acid under mild conditions.
Abstract: An efficient and convenient synthesis of both enantiomers of pipecolic acid has been developed using the intramolecular cyclization of 2-amino-6-bromohexanoic acid under mild conditions.
36 citations
TL;DR: Cyclic tetrapeptide retrohydroxamic acids were prepared as histone deacetylase (HDAC) inhibitors and evaluated the inhibitory activity and found that they have potential as anticancer drugs.
35 citations
TL;DR: In this article, the authors synthesize functionalized amino acids with 4-6 methylene spacers from α-carbon to the nitrogen atom of fulleropyrolidine and corresponding multifullerene peptides.
23 citations
TL;DR: In this article, the synthesis of non-natural amino acids with side chain lengths varying from 4 to 10 methylene units has been studied and shown to be useful intermediates for functionalization.
22 citations
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TL;DR: With the advent of numerous drugs that target specific enzymes involved in the epigenetic regulation of gene expression, the utilization of epigenetic targets is emerging as an effective and valuable approach to chemotherapy as well as chemoprevention of cancer.
Abstract: The initiation and progression of cancer is controlled by both genetic and epigenetic events. Unlike genetic alterations, which are almost impossible to reverse, epigenetic aberrations are potentially reversible, allowing the malignant cell population to revert to a more normal state. With the advent of numerous drugs that target specific enzymes involved in the epigenetic regulation of gene expression, the utilization of epigenetic targets is emerging as an effective and valuable approach to chemotherapy as well as chemoprevention of cancer.
1,155 citations
TL;DR: This review discusses the approaches proposed by several research groups working on the synthesis of HDAC inhibitors, based on modelling studies and the way these findings were used to obtain new HDAC inhibitor with possible isoform selectivity.
312 citations
TL;DR: The state of the art of this emerging field is presented and illustrated with some of the most representative examples of fullerenes for drug delivery in the biological and the biomedical domains.
Abstract: The fullerene family, and especially C(60), has delighted the scientific community during the last 25 years with perspective applications in a wide variety of fields, including the biological and the biomedical domains. Several biomedical uses have been explored using water-soluble C(60)-derivatives. However, the employment of fullerenes for drug delivery is still at an early stage of development. The design and synthesis of multifunctionalized and multimodal C(60) systems able to cross the cell membranes and efficiently deliver active molecules is an attracting challenge that involves multidisciplinary strategies. Promising results have emerged in the last years, bringing fullerenes again to the front of interest. Herein, the state of the art of this emerging field is presented and illustrated with some of the most representative examples.
249 citations
TL;DR: In this article, X-ray crystallographic data from 25 hydroxamato and 17 hydroximato mononuclear non-oxo-containing complexes with bidentate O, O 'coordination from monohydroxamic acids was analyzed.
235 citations
TL;DR: A series of benzene sulfonamides containing triazole-O-glycoside tails for evaluation as carbonic anhydrase (CA) inhibitors may prove interesting lead candidates to target tumor-associated CA isozymes, wherein the CA domain is located extracellularly.
Abstract: We report the synthesis of a series of benzene sulfonamides containing triazole-O-glycoside tails for evaluation as carbonic anhydrase (CA) inhibitors. These glycoconjugates were synthesized by the 1,3-dipolar cycloaddition reaction of 4-azidobenzenesulfonamide with O-propynyl glycosides. Compounds were assessed for their ability to inhibit the enzymatic activity of the physiologically dominant isozymes hCA I and II and the tumor-associated isozyme hCA IX (h = human). Against hCA I these compounds were either micromolar or low-nanomolar inhibitors, while against hCA II and IX inhibition in the range of 6.8-53 and 9.7-107 nM, respectively, was observed. The most potent inhibitor against hCA IX was the galactose derivative 8 (Ki = 9.7 nM); this is so far the most potent glycoconjugate inhibitor reported for the tumor-associated hCA IX. These carbohydrate-tethered sulfonamides may prove interesting lead candidates to target tumor-associated CA isozymes, wherein the CA domain is located extracellularly.
176 citations