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

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).

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Reddy KP,Bid HK,Nayak VL,Chaudhary P,Chaturvedi JP,Arya KR,Konwar R,Narender T

doi

10.1016/j.ejmech.2009.04.022

subject

Has Abstract

pub_date

2009-10-01 00:00:00

pages

3947-53

issue

10

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(09)00221-9

journal_volume

44

pub_type

杂志文章

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