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

Bioorg Med Chem Lett. 2003 May 19;13(10):1679-82. doi: 10.1016/s0960-894x(03)00263-4.

Vedula M Sharma ¹, 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

Affiliations

Affiliation

1 Discovery Chemistry, Dr. Reddy's Laboratories, Discovery Research, Miyapur, Hyderabad, 500 050, India. [email protected]

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

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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