In vitro and in vivo anticancer activity of 2-deacetoxytaxinine J and synthesis of novel taxoids and their in vitro anticancer activity.

Full Abstract

The taxane diterpneoid 2-deacetoxytaxinine J (2-DAT-J) 1 has been isolated from the bark of Himalayan yew, Taxus baccata L. spp. wallichiana in a reasonably good yield (0.1%) and its anticancer activity against breast cancer cell lines (MCF-7 and MDA-MB-231) and normal human kidney epithelial cell line (HEK-293) has been studied. 2-DAT-J (1) showed significant in vitro activity against breast cancer cell line at a concentration of 20 microM and 10 microM in MCF-7 and MDA-MB-231 respectively. Few novel taxoids were derived (7, 8 and 10-13) from the naturally occurring 2-DAT-J (1) and screened for their anticancer activity. The structure-activity relationship studies indicated that the cinnamoyl group on C-5 and acetyl group on C-10 are essential for the anticancer activity. 2-DAT-J (1) was also tested for its in vivo activity on DMBA-induced mammary tumors in virgin female Sprague Dawley rats at a dose of 10mg/kg body weight orally for 30 days and showed significant regression in mammary tumors as compared to vehicle treated group (p<0.05).

Author information

Author/s: Reddy, K Papi (KP); Bid, Hemant K (HK); Nayak, V Lakshma (VL); Chaudhary, Preeti (P); Chaturvedi, J P (JP); Arya, K R (KR); Konwar, Rituraj (R); Narender, T (T);

Affiliation: Medicinal and Process Chemistry Division, Central Drug Research Institute, Chattrar Manzil, Lucknow 226 001, Uttar Pradesh, India.

Journal and publication information

Publication Type: Journal Article

Journal: European journal of medicinal chemistry (Eur J Med Chem), published in France. (Language: eng)

Reference: 2009-Oct; vol 44 (issue 10) : pp 3947-53

Dates: Created 2009/08/03; Completed 2009/10/14;

PMID: 19446930, status: MEDLINE (last retrieval date: 10/14/2009, IMS Date: )

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