Literature DB >> 12729640

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

Vedula M Sharma1, 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.   

Abstract

A series of 6,7-diphenyl-2,3,8,8a-tetrahydro-1H-indolizin-5-one analogues were synthesized and evaluated for cytotoxic activity against eight human cancer cell lines. Compounds 18, 21, 28, 29, 30 and 31 showed cytotoxic activity with GI(50) values in the range of 2.1-8.1 microM concentration. Among these, compounds 21 and 28 exhibited good pharmacokinetic properties. These compounds were further evaluated for their in vivo efficacy in modified hollow fibre assay (HFA).

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Year:  2003        PMID： 12729640     DOI： 10.1016/s0960-894x(03)00263-4

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


  5 in total

1.  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

2.  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

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

Authors:  F Scott Kimball; Ashok Rao Tunoori; Samuel F Victory; Dinah Dutta; Jonathan M White; Richard H Himes; Gunda I Georg
Journal:  Bioorg Med Chem Lett       Date:  2007-06-13       Impact factor: 2.823

4.  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

5.  Photoswitchable anticancer activity via trans-cis isomerization of a combretastatin A-4 analog.

Authors:  Jonathon E Sheldon; M Michael Dcona; Charles E Lyons; John C Hackett; Matthew C T Hartman
Journal:  Org Biomol Chem       Date:  2015-10-27       Impact factor: 3.876
  5 in total

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