Synthesis of new boswellic acid derivatives as potential antiproliferative agents. Issue 13 (2nd July 2020)

• Record Type: Journal Article
• Authors: Shamraiz, Umair; Hussain, Hidayat; Ur Rehman, Najeeb; Al-Shidhani, Sulaiman; Saeed, Aasim; Khan, Husain Yar; Khan, Ajmal; Fischer, Lucie; Csuk, René; Badshah, Amin; Al-Rawahi, Ahmed; Hussain, Javid; Al-Harrasi, Ahmed
• Is Part Of: Natural product research. Volume 34:Issue 13(2020)
• Page Start: 1845
• Page End: 1852
• Publication Date: 2020-07-02
• Subjects: Boswellic acid -- AKBA-KBA heterodimers -- cytotoxicity; Natural products -- Periodicals; Natural products -- Research -- Periodicals; Biological Factors -- Periodicals; Biological Products -- Periodicals; 547
• DOI: 10.1080/14786419.2018.1564295
• Languages: English
• ISSNs: 1478-6419

Abstract

Abstract: In the current investigation, a series of heterocyclic derivatives of boswellic acids were prepared along with new monomers of 3- O -acetyl-11-keto-β-boswellic acid (AKBA, 1 ) 11-keto-β-boswellic acid (KBA, 2 ) and several new bis-AKBA and KBA homodimers and AKBA-KBA heterodimers. The effects of these compounds on the proliferation of different human cancer cell lines, viz., FaDu (pharynx carcinoma), A2780 (ovarian carcinoma), HT29 (colon adenocarcinoma), and A375 (malignant melanoma), have been evaluated. Thus, KBA homodimer 21 effectively inhibited the growth of FaDu, A2780, HT29, and A375 cells with EC50 values below 9 μM. In addition, compounds 7, 8, 11, 12, 15, 16, and 17 also exhibited cytotoxic effects for A2780, HT29, and A375 cancer cells. In particular, the pyrazine analog 8 was highly cytotoxic for A375 cancer cells with an EC50 value of 2.1 μM. Graphical Abstract: