Literature DB >> 16722623

Novel chromene-derived selective estrogen receptor modulators useful for alleviating hot flushes and vaginal dryness.

Nareshkumar Jain1, Ramesh M Kanojia, Jiayi Xu, Guo Jian-Zhong, Emmanuel Pacia, Muh-Tsann Lai, Fuyong Du, Amy Musto, George Allan, DoWon Hahn, Scott Lundeen, Zhihua Sui.   

Abstract

A novel SERM (selective estrogen receptor modulators), 1-(R), a chromene-derived bisbenzopyran, was discovered to alleviate hot flushes and effectively increase vaginal fluidity in rats. Moreover, 1-(R) was found to have beneficial effects on plasma cholesterol and bone metabolism while maintaining antiestrogenic activity in the uterus. The biological profile of its enantiomer 1-(S) was also evaluated.

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Year:  2006        PMID: 16722623     DOI: 10.1021/jm060353u

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  5 in total

1.  Diastereoselective synthesis of novel spiro indanone fused pyrano[3,2-c]chromene derivatives following hetero-Diels-Alder reaction and in vitro anticancer studies.

Authors:  Pravati Panda; Sabita Nayak; Susanta Ku Sahoo; Seetaram Mohapatra; Deepika Nayak; Rajalaxmi Pradhan; Chanakya Nath Kundu
Journal:  RSC Adv       Date:  2018-05-08       Impact factor: 4.036

Review 2.  Tamoxifen: catalyst for the change to targeted therapy.

Authors:  V Craig Jordan
Journal:  Eur J Cancer       Date:  2008-01       Impact factor: 9.162

Review 3.  Estrogen receptors alpha (ERα) and beta (ERβ): subtype-selective ligands and clinical potential.

Authors:  Ilaria Paterni; Carlotta Granchi; John A Katzenellenbogen; Filippo Minutolo
Journal:  Steroids       Date:  2014-06-24       Impact factor: 2.668

4.  Introducing novel potent anticancer agents of 1H-benzo[f]chromene scaffolds, targeting c-Src kinase enzyme with MDA-MB-231 cell line anti-invasion effect.

Authors:  Hany E A Ahmed; Mohammed A A El-Nassag; Ahmed H Hassan; Rawda M Okasha; Saleh Ihmaid; Ahmed M Fouda; Tarek H Afifi; Ateyatallah Aljuhani; Ahmed M El-Agrody
Journal:  J Enzyme Inhib Med Chem       Date:  2018-12       Impact factor: 5.051

Review 5.  The discovery and development of selective estrogen receptor modulators (SERMs) for clinical practice.

Authors:  Philipp Y Maximov; Theresa M Lee; V Craig Jordan
Journal:  Curr Clin Pharmacol       Date:  2013-05
  5 in total

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