Etopside analogs

US5332811A · kind A · utility

Assignee

• The University of North Carolina at Chapel Hill · US

Inventors

• Kuo-Hsiung Lee · Chapel Hill, US
• Xiao-Ming Zhou · Carrboro, US
• Zhe Wang · Xiangtan City, CN
• Jang-Yang Chang · Taipei, TW
• Hong-Xing Chen · New Haven, US
• Yung-Chi Cheng · Woodbridge, US
• Ya-Ching Shen
• Fu-Shen Han · New Haven, US
• Hong Hu · Berkeley Heights, US
• Yi Zhang · Nanjing, CN

Key dates

• Filing date: May 1, 1991
• Grant date: Jul 26, 1994
• Expiry date: May 1, 2011

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D493/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Compounds which are analogs of etoposide and which exhibit anti-tumor activity are disclosed. These compounds having the following structure: ##STR1## wherein R is selected from ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently selected from H, CH.sub.3, C.sub.2 H.sub.5, C.sub.3 H.sub.7, i--C.sub.3 H.sub.7, C.sub.4 H.sub.9, CF.sub.3, OCH.sub.3, OC.sub.2 H.sub.5 , OC.sub.3 H.sub.7, OC.sub.4 H.sub.9, O--i--C.sub.3 H.sub.7, O--i--C.sub.4 H.sub.9, --OCH.sub.2 O--, --OCH.sub.2 CH.sub.2 O--, CH.sub.2 OH, C.sub.2 H.sub.4 OH, CH.sub.2 Cl C.sub.2 H.sub.4 Cl, CH.sub.2 F, C.sub.2 H.sub.4 F, CH.sub.2 OCH.sub.3, COCH.sub.3, COC.sub.2 H.sub.5, CO.sub.2 CH.sub.3, CO.sub.2 C.sub.2 H.sub.5, NO.sub.2, NH.sub.2, NH.sub.2.HCl, NH.sub.2.HAc, NH.sub.2.1/2H.sub.2 SO.sub.4 , NH.sub.2.1/3H.sub.3 PO.sub.4, N(CH.sub.3).sub.2, N(C.sub.2 H.sub.5).sub.2, OH, CN, N.sub.3, SO.sub.2 H, SO.sub.2 NH.sub.2 , SO.sub.2 Cl, phenyl, substituted phenyl, phenoxy, substituted phenoxy, anilinyl, substituted anilinyl, cyclohexyl, piperidine, ##STR3## wherein R.sub.6 is selected from hydrogen, methyl, ethyl, n-propyl, i-propyl, butyl and bridged methylene; PA1 wherein R.sub.7 is selected fr…