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Archive for the ‘Hot articles’ Category

HOT: Estrogen dependent breast cancer lead compound

02 Dec 2010

Adam McCluskey and colleagues at The University of Newcastle have developed a library of compounds that can act as anti-cancer agents.

In this paper, they report the discovery of a family of 2-phenylacrylonitriles with excellent growth inhibition of a panel of ten human cancer cell lines.

Read this MedChemComm full paper free to access.

Library synthesis and cytotoxicity of a family of 2-phenylacrylonitriles and discovery of an estrogen dependent breast cancer lead compound
Mark Tarleton, Jayne Gilbert, Mark J. Robertson, Adam McCluskey and Jennette A. Sakoff
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C0MD00147C , Concise Article

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Promising anabolic agent for bone disease

19 Nov 2010

Chan Soo Shin, Seung Bum Park and colleagues at Seul National University in Korea have discovered a novel small-molecule bone anabolic agent with osteogenic effects.

The efficacy of this new benzopyranyl compound has been confirmed and evaluated both in vivo and in vitro.

Find out more about this promising anabolic agent for bone disease on our free to access MedChemComm article.

Discovery of a novel benzopyranyl compound as a potent in vitro and in vivo osteogenic agent

Sangmi Oh, Sun Wook Cho, Jae-Yeon Yang, Hyun Jin Sun, Young Sun Chung, Chan Soo Shin and Seung Bum Park

Med. Chem. Commun., 2010, Advance Article
DOI: 10.1039/C0MD00149J, Concise Article

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HIV-1 fusion inhibitors

14 Sep 2010

Oishi, Fujii and co-workers report on the affinity-based screening technology and sequence-activity relationships for aminoacid optimization in HIV-1 fusion inhibitors directed against enfuvirtide-resistant HIV strains.

Find out more about this affinity selection-mass spectrometry method to explore novel HIV-1 fusion inhibitors. Do you have anything to say? Comment on it!

Affinity selection and sequence-activity relationships of HIV-1 membrane fusion inhibitors directed at the drug-resistant variants
Shinya Oishi, Kentaro Watanabe, Saori Ito, Michinori Tanaka, Hiroki Nishikawa, Hiroaki Ohno, Kazuki Shimane, Kazuki Izumi, Yasuko Sakagami, Eiichi N. Kodama, Masao Matsuoka, Akira Asai and Nobutaka Fujii
Med. Chem. Commun., 2010, Advance Article
DOI: 10.1039/C0MD00091D , Concise Article

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Discovery of a promising anticancer compound

23 Aug 2010

Hengmiao Cheng and colleagues have synthesised a compound through integration of structure based drug design (SBDD) and physical properties based optimization (PPBO) with in vivo and in vitro great efficacy.

Currently, this compound is being evaluated in human clinical trilas for the treatment of cancer.

Read more and comment on it here:

Discovery of the highly potent PI3K/mTOR dual inhibitor PF-04691502 through structure based drug design

Hengmiao Cheng, Shubha Bagrodia, Simon Bailey, Martin Edwards, Jacqui Hoffman, Qiyue Hu, Robert Kania, Daniel R. Knighton, Matthew A. Marx, Sacha Ninkovic, Shaoxian Sun and Eric Zhang

Med. Chem. Commun., 2010, 1, 139-144
DOI: 10.1039/C0MD00072H

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RSC Medicinal Chemistry Blog

Archive for the ‘Hot articles’ Category

HOT: Estrogen dependent breast cancer lead compound

Promising anabolic agent for bone disease

HIV-1 fusion inhibitors

Discovery of a promising anticancer compound

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