Identification and differentiation of bear bile used in medicinal products in Taiwan

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Title:	Identification and differentiation of bear bile used in medicinal products in Taiwan
Authors:	Lin, DL;Chang, HC;Chang, CP;Chen, CY
Contributors:	中國醫藥大學;TAIPEI MED COLL,GRAD INST PHARMACEUT SCI,TAIPEI,TAIWAN;CHINA MED COLL,TAICHUNG,TAIWAN
Date:	1997
Issue Date:	2010-09-24 13:38:58 (UTC+8)
Publisher:	AMER SOC TESTING MATERIALS
Abstract:	As part of our continuing search for potential anticancer drug candidates:in the 2-aryl-1,8-naphthyridin-4(1H)-one series, we have synthesized two series of 3'-substituted 2-phenyl-1,8-naphthyridin-4(1H)-ones and 2-naphthyl-1,8-naphthyridin-4(1H)-ones. All compounds showed significant cytotoxic effects (log GI(50) < -4.0; log molar drug concentration required to cause 50% growth inhibition) against a variety of human tumor cell lines of the National Cancer Institute's in vitro screen, including cells derived from solid tumors such as non-small cell lung, colon, central nervous system, melanoma, ovarian, prostate, and breast cancers. All 3'-substituted compounds demonstrated strong cytotoxic effects in almost all tumor cell lines. Introduction of an aromatic ring at the 2'- and 3'-positions also generated compounds with potent antitumor activity. Incorporation of an aromatic ring at the 3'- and 4'-positions produced compounds with reduced activity. Interestingly, introduction of a halogen at the 3'-position yielded compounds with different selectivity. for the tumor cell lines tested. All 3'-halogenated compounds (29-36) and compounds 38 and 42-44 were potent inhibitors of tubulin polymerization with activities nearly comparable to those of the potent antimitotic natural products colchicine, podophyllotoxin, and combretastatin A-4. Active agents also inhibited the binding of [H-3]colchicine to tubulin.
Relation:	JOURNAL OF FORENSIC SCIENCES 42(5):817-823
Appears in Collections:	[China Medical University] Journal articles

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