Literature DB >> 17614274

Synthesis, in vitro and in vivo cytotoxicity of 6,7-diaryl-2,3,8,8a-tetrahydroindolizin-5(1H)-ones.

F Scott Kimball1, Ashok Rao Tunoori, Samuel F Victory, Dinah Dutta, Jonathan M White, Richard H Himes, Gunda I Georg.   

Abstract

A 6,7-diaryl-2,3,8,8a-tetrahydroindolizin-5(1H)-one library was constructed and tested against the colon cancer cell line HCT-116 as an initial screen for cytotoxic properties. Of this library, the parent compound, in which the southern aromatic ring remains unsubstituted, and the northern aromatic ring carries a 4-methoxy group, exhibited the most potent cytotoxicity with an IC50 value of 0.39 microM and displayed promising activity in vivo in the NCI's mouse hollow fiber assay.

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Year:  2007        PMID： 17614274      PMCID： PMC2065880          DOI： 10.1016/j.bmcl.2007.05.103

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


  8 in total

1.  Cytotoxic alkaloids from Tylophora indica.

Authors:  M Ali; S H Ansari; M R Grever
Journal:  Pharmazie       Date:  2001-02       Impact factor: 1.267

2.  New Synthetic Route to 2-Pyridones and Its Application toward the Synthesis of (+/-)-Ipalbidine.

Authors:  Scott M. Sheehan; Albert Padwa
Journal:  J Org Chem       Date:  1997-02-07       Impact factor: 4.354

3.  Novel 6,7-diphenyl-2,3,8,8a-tetrahydro-1H-indolizin-5-one analogues as cytotoxic agents.

Authors:  Vedula M Sharma; K V Adi Seshu; C Vamsee Krishna; P Prasanna; V Chandra Sekhar; A Venkateswarlu; Sriram Rajagopal; R Ajaykumar; Dhanvanthri S Deevi; N V S Rao Mamidi; R Rajagopalan
Journal:  Bioorg Med Chem Lett       Date:  2003-05-19       Impact factor: 2.823

4.  A manual method for applying the Hansch approach to drug design.

Authors:  J G Topliss
Journal:  J Med Chem       Date:  1977-04       Impact factor: 7.446

5.  Display and analysis of patterns of differential activity of drugs against human tumor cell lines: development of mean graph and COMPARE algorithm.

Authors:  K D Paull; R H Shoemaker; L Hodes; A Monks; D A Scudiero; L Rubinstein; J Plowman; M R Boyd
Journal:  J Natl Cancer Inst       Date:  1989-07-19       Impact factor: 13.506

6.  Synthesis and anti-tubulin activity of a 3'-(4-azidophenyl)-3'-dephenylpaclitaxel photoaffinity probe.

Authors:  Jared T Spletstoser; Patrick T Flaherty; Richard H Himes; Gunda I Georg
Journal:  J Med Chem       Date:  2004-12-16       Impact factor: 7.446

7.  Enantiopure N-Acyldihydropyridones as Synthetic Intermediates: Asymmetric Synthesis of (-)-Septicine and (-)-Tylophorine.

Authors:  Daniel L. Comins; Xinghai Chen; Lawrence A. Morgan
Journal:  J Org Chem       Date:  1997-10-17       Impact factor: 4.354

8.  In vivo cultivation of tumor cells in hollow fibers.

Authors:  M G Hollingshead; M C Alley; R F Camalier; B J Abbott; J G Mayo; L Malspeis; M R Grever
Journal:  Life Sci       Date:  1995       Impact factor: 5.037
  8 in total
  6 in total

1.  Total Syntheses and Cytotoxicity of (R)- and (S)-Boehmeriasin A.

Authors:  Matthew W Leighty; Gunda I Georg
Journal:  ACS Med Chem Lett       Date:  2011-04-14       Impact factor: 4.345

2.  Phenanthroindolizidines and Phenanthroquinolizidines: Promising Alkaloids for Anti-Cancer Therapy.

Authors:  Sherry R Chemler
Journal:  Curr Bioact Compd       Date:  2009-03-01

3.  Enantiospecific synthesis and cytotoxicity of 7-(4-methoxyphenyl)-6-phenyl-2,3,8,8a-tetrahydroindolizin-5(1H)-one enantiomers.

Authors:  F Scott Kimball; Brandon J Turunen; Keith C Ellis; Richard H Himes; Gunda I Georg
Journal:  Bioorg Med Chem       Date:  2008-03-04       Impact factor: 3.641

4.  Structural analogs of tylophora alkaloids may not be functional analogs.

Authors:  Wenli Gao; Annie Pei-Chun Chen; Chung-Hang Leung; Elizabeth A Gullen; Alois Fürstner; Qian Shi; Linyi Wei; Kuo-Hsiung Lee; Yung-Chi Cheng
Journal:  Bioorg Med Chem Lett       Date:  2007-11-21       Impact factor: 2.823

5.  Synthesis and evaluation of heteroaromatic 6,7-diaryl-2,3,8,8a-tetrahydroindolizin-5(1H)-ones for cytotoxicity against the HCT-116 colon cancer cell line.

Authors:  F Scott Kimball; Richard H Himes; Gunda I Georg
Journal:  Bioorg Med Chem Lett       Date:  2008-04-25       Impact factor: 2.823

6.  Metal-free [3 + 2 + 1]/[2 + 2 + 1] biscyclization: stereospecific construction with concomitant functionalization of indolizin-5(1H)-one.

Authors:  Tuan-Jie Li; Zhong-Qiu Liu; Hong-Mei Yin; Chang-Sheng Yao; Bo Jiang; Xiang-Shan Wang; Shu-Jiang Tu; Xiu-Ling Li; Guigen Li
Journal:  J Org Chem       Date:  2013-11-07       Impact factor: 4.354
  6 in total

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