2,6-Dithienyl-4-furyl pyridines: Synthesis, topoisomerase I and II inhibition, cytotoxicity, structure–activity relationship, and docking study

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSynthesis and biological activity of substance P C-terminal hexapeptide analogues: structure-activity studiesConstantine Poulos, John R. Brown, and Christopher C. JordanCite this: J. Med. Chem. 1986, 29, 7, 1281–1284Publication Date (Print):July 1, 1986Publication History Published online1 May 2002Published inissue 1 July 1986https://pubs.acs.org/doi/10.1021/jm00157a028https://doi.org/10.1021/jm00157a028research-articleACS PublicationsRequest reuse permissionsArticle Views59Altmetric-Citations18LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-Alertsclose Get e-Alerts

Structure–activity relationship

10.1021/jm00157a028

Cite

Citations (23)

Synthesis and biological activity of 2-methyl-20-epi analogues of 1α,25-dihydroxyvitamin D3

Bioorganic & Medicinal Chemistry Letters (1998)

Toshie Fujishima Zhao‐Peng Liu Daishiro Miura Manabu Chokki Seiichi Ishizuka

Epimer

Diastereomer

10.1016/s0960-894x(98)00363-1

Cite

Citations (32)

Synthesis and biological activity of aminophthalazines and aminopyridazines as novel inhibitors of PGE2 production in cells

Bioorganic & Medicinal Chemistry Letters (2012)

Federico Medda Earlphia Sells Hui Hua Chang Justin Dietrich Shashi Chappeta

IC50

Structure–activity relationship

10.1016/j.bmcl.2012.11.030

Cite

Citations (12)

Synthesis of the Biologically Active Natural Product Cyclodepsipeptides Apratoxin A and Its Analogues

Chemical and Pharmaceutical Bulletin (2014)

Takayuki Doi

This paper describes the synthetic studies conducted on a marine natural product, cyclodepsipeptide apratoxin A. Total synthesis of the oxazoline analogue of apratoxin A was achieved. The conversion of oxazoline to thioamide, as well as thioamide formation from a serine-derived compound, were both unsuccessful. However, thiazoline formation from a cysteine-derived compound led to the total synthesis of apratoxin A. An in vivo study on synthetic apratoxin A revealed that it has potent antitumor activity, but with significant toxicity. Solid-phase synthesis of apratoxin A was accomplished using a preformed thiazoline derivative as a coupling unit. This method was used to synthesize several azido-containing analogues as precursors of molecular probes, and these analogues exhibited potent biological activity.

Thiazoline

Thioamide

Oxazoline

Natural product

Depsipeptide

Semisynthesis

Solid-Phase Synthesis

Derivative (finance)

10.1248/cpb.c14-00268

Cite

Citations (18)

The Synthesis of the Insulin Chains and Their Combination to Biologically Active Material

Diabetes (1964)

Panayotis G. Katsoyannis

The synthesis of the A- and B-chains of insulin and their isolation in the S-sulfonate form were accomplished. Combination experiments between the synthetic A- and natural B-chain, the synthetic B- and the natural A-chain, and between the synthetic A- and B-chains generated insulin activity. The yield of the generated activity in all cases was within the range of the activity obtained when similarly treated natural A- and B-chains are combined. This work represents the first chemical synthesis of a naturally Occurring protein and constitutes a case in which the proposed primary structure of a protein has been confirmed ky chemical synthesis.

Side chain

Chemical structure

10.2337/diab.13.4.339

Cite

Citations (61)

Chemotactic Peptide Analogues. Synthesis and Chemotactic Activity of N‐Formyl‐Met‐Leu‐Phe Analogues Containing (S)‐Phenylalaninol Derivatives

Archiv der Pharmazie (1995)

Giampiero Pagani Zecchini Mario Paglialunga Paradisi Ines Torrini Susanna Spisani

The synthesis and the biological activity towards human neutrophils of some N-formyl-Met-Leu-Phe-OMe analogues containing (S)-phenylalaninol (Pheol) or its derivatives in place of the native phenylalanine are reported. While the analogue containing Pheol (4) was found to be devoid of significant biological activity, its esters 3 and 5, although inactive as chemoattractants, are able to strongly stimulate superoxide production and are active with a lower efficacy in the lysozyme release.

Formyl peptide receptor

Peptide Synthesis

Oligopeptide

10.1002/ardp.19953280908

Cite

Citations (5)

Role of the C8 gem-dimethyl group of bryostatin 1 on its unique pattern of biological activity

Bioorganic & Medicinal Chemistry Letters (2012)

Gary E. Keck Yam B. Poudel Arnab Rudra Jeffrey C. Stephens Noémi Kedei

Bryostatin 1

10.1016/j.bmcl.2012.04.073

Cite