Search Results - "Iso, Kentaro"
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Unified, Efficient, and Scalable Synthesis of Halichondrins: Zirconium/Nickel‐Mediated One‐Pot Ketone Synthesis as the Final Coupling Reaction
Published in Angewandte Chemie International Edition (28-08-2017)“…Unified, efficient, and scalable syntheses of the halichondrin natural products are reported. A newly developed Zr/Ni‐mediated one‐pot ketone synthesis was…”
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2
Delivery of a BET protein degrader via a CEACAM6-targeted antibody–drug conjugate inhibits tumour growth in pancreatic cancer models
Published in Nature communications (11-03-2024)“…Pancreatic ductal adenocarcinoma (PDAC) has the worst prognosis of all cancers. To improve PDAC therapy, we establish screening systems based on organoid and…”
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3
A Concise Synthesis of the Pentacyclic Framework of Cortistatins
Published in Organic letters (21-08-2008)“…An efficient synthesis of the pentacyclic framework of cortistatins has been developed. The key strategy comprises assembly of the A- and the CD-ring fragments…”
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4
A landmark in drug discovery based on complex natural product synthesis
Published in Scientific reports (17-06-2019)“…Despite their outstanding antitumour activity in mice, the limited supply from the natural sources has prevented drug discovery/development based on intact…”
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5
Efficient and stereoselective installation of isoquinoline: formal total synthesis of cortistatin A
Published in Tetrahedron letters (01-07-2009)“…The highly stereoselective attachment of isoquinoline onto the steroidal framework of cortistatin A has been achieved. Our strategy features a Ce-mediated…”
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Synthesis of the Bicyclo[7.3.0]dodecadiyne Core of the Maduropeptin Chromophore
Published in Chemistry, an Asian journal (01-02-2008)“…Maduropeptin, an extremely potent antitumor agent, consists of a 1:1 complex of a carrier protein and a chromophore. We report herein a general and efficient…”
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A Facile Synthesis of 1,2-Dihydroisoquinolines by Three-Component Reaction
Published in Heterocycles (01-01-2007)Get full text
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8
Total Synthesis of Cortistatins A and J
Published in Journal of organic chemistry (15-04-2011)“…This paper describes the details of our synthetic studies on the marine steroidal alkaloids cortistatins A and J. The key features of our strategy include (i)…”
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9
Targeted protein degradation via intramolecular bivalent glues
Published in Nature (London) (07-03-2024)“…Targeted protein degradation is a pharmacological modality that is based on the induced proximity of an E3 ubiquitin ligase and a target protein to promote…”
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10
Stereocontrolled Synthesis of Left Halves of Halichondrins
Published in Journal of organic chemistry (01-09-2017)“…A stereocontrolled synthesis of the left halves of halichondrins was reported. An intramolecular oxy-Michael reaction under basic conditions was used to…”
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11
E7386, a Selective Inhibitor of the Interaction between β-Catenin and CBP, Exerts Antitumor Activity in Tumor Models with Activated Canonical Wnt Signaling
Published in Cancer research (Chicago, Ill.) (15-02-2021)“…The Wnt/β-catenin signaling pathway plays crucial roles in embryonic development and the development of multiple types of cancer, and its aberrant activation…”
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12
Unified Synthesis of Right Halves of Halichondrins A–C
Published in Journal of organic chemistry (01-09-2017)“…The right halves of halichondrins A–C were synthesized by coupling the common C20–C37 building block 9 with the C1–C19 building blocks 10a–c, respectively…”
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13
Ten-Gram-Scale Total Synthesis of the Anticancer Drug Candidate E7130 to Supply Clinical Trials
Published in Organic letters (12-04-2024)“…E7130 is a novel drug candidate with an exceedingly complex chemical structure of the halichondrin class, discovered by a total synthesis approach through…”
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What Does It Take to Develop Structurally Complex Molecules by Total Synthesis? Rapid Process Development and GMP Manufacturing of E7130 Drug Substance for First-in-Human Clinical Study
Published in Organic process research & development (21-06-2024)“…Process development of E7130 Drug Substance, which is a novel anticancer drug candidate, is described. To accomplish rapid delivery of such a large and…”
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15
An Environmentally Friendly Synthetic Method of 1,2-Dihydroisoquinoline Frameworks via Three-Component Reaction with o-Alkynylbenzaldehydes, Primary Amines, and Pronucleophiles
Published in Organic letters (31-08-2006)“…Three-component reactions with ortho-alkynylbenzaldehydes, primary amines, and pronucleophiles (Nu-H), such as CHCl3, proceeded to give 1,2-dihydroisoquinoline…”
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Abstract 4179: E7130 derived from total synthesis of halichondrin as a novel tumor-microenvironment ameliorator
Published in Cancer research (Chicago, Ill.) (15-08-2020)“…Abstract Background and objectives: Natural products have been a rich source of inspiration for drug discovery as demonstrated by the fact that over one-third…”
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Abstract 4183: Mechanism of action analysis of anti-CAF activity of E7130, a novel tumor-microenvironment ameliorator
Published in Cancer research (Chicago, Ill.) (15-08-2020)“…Abstract Background and objectives: Despite the outstanding antitumor activity of halichondrins in mice, the limited supply from the natural sources has…”
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18
Unified, Efficient, and Scalable Synthesis of Halichondrins: Zirconium/Nickel‐Mediated One‐Pot Ketone Synthesis as the Final Coupling Reaction
Published in Angewandte Chemie (28-08-2017)“…Unified, efficient, and scalable syntheses of the halichondrin natural products are reported. A newly developed Zr/Ni‐mediated one‐pot ketone synthesis was…”
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Journal Article -
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Abstract 5177: E7386 : First-in-class orally active CBP/beta-catenin modulator as an anticancer agent
Published in Cancer research (Chicago, Ill.) (01-07-2017)“…Abstract Carcinogenesis is often accelerated by the aberrant activation of components molecules of Wnt signaling pathway, especially, APC and beta-catenin are…”
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