Synthesis and cytotoxic activity of 3-O-acyl/3-hydrazine /2-bromo/20,29-dibromo betulinic acid derivatives

Bioorganic & Medicinal Chemistry Letters
Rama MukherjeeAnand C Burman

Abstract

A series of 3-O-acyl, 3-hydrazine, 2-bromo, and 20,29-dibromo betulinic acid derivatives (1-27) have been synthesized and screened for in vitro cytotoxic activity on human cancer cell lines MOLT-4, JurkatE6.1, CEM.CM3, BRISTOL8, U937, DU145, PA-1, A549, and L132. A number of compounds have shown ED(50)<1 microg/mL against the cancer cell lines tested and have shown better cytotoxicity than betulinic acid. Compounds 13, 19, 20, 23, and 27 were the best derivatives and were selected as lead molecules for further development. The structure-activity relationship has been described.

References

Jul 10, 1999·International Journal of Cancer. Journal International Du Cancer·S FuldaK M Debatin

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Citations

Sep 14, 2007·Investigational New Drugs·Praveen RajendranAnand C Burman
Jun 3, 2006·Natural Product Reports·Petr DzubakJan Sarek
Nov 23, 2006·Natural Product Reports·Pavel A Krasutsky
Nov 6, 2015·Bioconjugate Chemistry·Miroslav SouralMilan Urban
Jun 10, 2014·Expert Opinion on Therapeutic Patents·René Csuk
Apr 11, 2015·Phytochemistry Reviews : Proceedings of the Phytochemical Society of Europe·Barbara Bednarczyk-Cwynar, Lucjusz Zaprutko
Jun 3, 2015·Medicinal Research Reviews·Dong-Mei ZhangWen-Cai Ye
Mar 5, 2017·Phytomedicine : International Journal of Phytotherapy and Phytopharmacology·Kok Hoong LeongDaisuke Sugiyama
Sep 23, 2014·Angewandte Chemie·Quentin MichaudelPhil S Baran
Jan 10, 2012·Organic & Biomolecular Chemistry·Barbara Bednarczyk-CwynarBogusław Hładoń

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