Literature DB >> 21831635

Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1α inhibitors.

Wenwei Huang1, Ruili Huang, Matias S Attene-Ramos, Srilatha Sakamuru, Erika E Englund, James Inglese, Christopher P Austin, Menghang Xia.   

Abstract

Quinazolin-4-one 1 was identified as an inhibitor of the HIF-1α transcriptional factor from a high-throughput screen. HIF-1α up-regulation is common in many cancer cells. In this Letter, we describe an efficient one-pot sequential reaction for the synthesis of quinazolin-4-one 1 analogues. The structure-activity relationship (SAR) study led to the 5-fold more potent analogue, 16. Published by Elsevier Ltd.

Entities:  

Mesh：

Substances：

Year:  2011        PMID： 21831635      PMCID： PMC3681418          DOI： 10.1016/j.bmcl.2011.07.043

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  22 in total

Review 1.  Targeting hypoxia and angiogenesis through HIF-1alpha inhibition.

Authors:  Juan A Diaz-Gonzalez; James Russell; Ana Rouzaut; Ignacio Gil-Bazo; Luis Montuenga
Journal:  Cancer Biol Ther       Date:  2005-10-21       Impact factor: 4.742

2.  Melatonin suppresses tumor angiogenesis by inhibiting HIF-1alpha stabilization under hypoxia.

Authors:  Shi-Young Park; Won-Jun Jang; Eui-Yeun Yi; Ji-Yeong Jang; Yunjin Jung; Joo-Won Jeong; Yung-Jin Kim
Journal:  J Pineal Res       Date:  2010-03       Impact factor: 13.007

Review 3.  Hypoxia-inducible factor inhibitors: a survey of recent patented compounds (2004 - 2010).

Authors:  Hyun Seung Ban; Yoshikazu Uto; Hiroyuki Nakamura
Journal:  Expert Opin Ther Pat       Date:  2011-01-06       Impact factor: 6.674

4.  Development of novel inhibitors targeting HIF-1α towards anticancer drug discovery.

Authors:  Nilambari Yewalkar; Vijaykumar Deore; Amol Padgaonkar; Sonal Manohar; Bichismita Sahu; Pramod Kumar; Archana Jalota-Badhwar; Kalpana S Joshi; Somesh Sharma; Sanjay Kumar
Journal:  Bioorg Med Chem Lett       Date:  2010-09-18       Impact factor: 2.823

5.  Ras inhibition in glioblastoma down-regulates hypoxia-inducible factor-1alpha, causing glycolysis shutdown and cell death.

Authors:  Roy Blum; Jasmine Jacob-Hirsch; Ninette Amariglio; Gideon Rechavi; Yoel Kloog
Journal:  Cancer Res       Date:  2005-02-01       Impact factor: 12.701

Review 6.  The biology of cancer: metabolic reprogramming fuels cell growth and proliferation.

Authors:  Ralph J DeBerardinis; Julian J Lum; Georgia Hatzivassiliou; Craig B Thompson
Journal:  Cell Metab       Date:  2008-01       Impact factor: 27.287

7.  RAS-RAF-MEK-dependent oxidative cell death involving voltage-dependent anion channels.

Authors:  Nicholas Yagoda; Moritz von Rechenberg; Elma Zaganjor; Andras J Bauer; Wan Seok Yang; Daniel J Fridman; Adam J Wolpaw; Inese Smukste; John M Peltier; J Jay Boniface; Richard Smith; Stephen L Lessnick; Sudhir Sahasrabudhe; Brent R Stockwell
Journal:  Nature       Date:  2007-06-14       Impact factor: 49.962

Review 8.  Evaluation of HIF-1 inhibitors as anticancer agents.

Authors:  Gregg L Semenza
Journal:  Drug Discov Today       Date:  2007-09-18       Impact factor: 7.851

Review 9.  Biology of HIF-1alpha.

Authors:  A Weidemann; R S Johnson
Journal:  Cell Death Differ       Date:  2008-02-15       Impact factor: 15.828

10.  Ras-dependent induction of HIF-1alpha785 via the Raf/MEK/ERK pathway: a novel mechanism of Ras-mediated tumor promotion.

Authors:  Ji-Hong Lim; Eun-Seo Lee; Ho-Jin You; Jung Weon Lee; Jong-Wan Park; Yang-Sook Chun
Journal:  Oncogene       Date:  2004-12-16       Impact factor: 9.867
View more
  3 in total

1.  Using β-Lactamase and NanoLuc Luciferase Reporter Gene Assays to Identify Inhibitors of the HIF-1 Signaling Pathway.

Authors:  Thai Khuc; Chia-Wen Amy Hsu; Srilatha Sakamuru; Menghang Xia
Journal:  Methods Mol Biol       Date:  2016

2.  Inhibition of the HIF1α-p300 interaction by quinone- and indandione-mediated ejection of structural Zn(II).

Authors:  Madura K P Jayatunga; Sam Thompson; Tawnya C McKee; Mun Chiang Chan; Kelie M Reece; Adam P Hardy; Rok Sekirnik; Peter T Seden; Kristina M Cook; James B McMahon; William D Figg; Christopher J Schofield; Andrew D Hamilton
Journal:  Eur J Med Chem       Date:  2014-06-27       Impact factor: 6.514

3.  Discovery of an algicidal compound from Brevibacterium sp. BS01 and its effect on a harmful algal bloom-causing species, Alexandrium tamarense.

Authors:  Xinli An; Bangzhou Zhang; Huajun Zhang; Yi Li; Wei Zheng; Zhiming Yu; Lijun Fu; Tianling Zheng
Journal:  Front Microbiol       Date:  2015-11-05       Impact factor: 5.640
  3 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.