Two new conjugates of murrayafoline A with zerumbone and artemisinin 3, 11 were prepared by N-alkylation, in which, compound 3 was synthesized from two consecutive Nalkylation reactions. Their cytotoxicity was evaluated on four human cancer cell lines Hep-G2, LU, RD and Fl. The result showed that both compounds exhibited no activity against the tested cell lines. | Journal of Science and Technology 54 (2C) (2016) 502-508 SYNTHESIS AND CYTOTOXIC ACTIVITY EVALUATION OF NOVEL DERIVATIVES OF MURRAYAFOLINE A Le Duc Anh1, *, Nguyen Thi Hai Ly2, Truong Ngoc Hung3, Nguyen Thi Nga3, Nguyen Manh Cuon 3, Le Mai Huong3, Lê Phong3, Luu Van Chinh3, * 1 2 Chemistry-Materials Institute, Institute of Military Science and Technology 17 Hoang Sam, Cau Giay, Hanoi Tran Phu Gifted High School, 12 Tran Phu, Luong Khánh Thien, Ngo Quyen, Hai Phong 3 Institute of Natural Products Chemistry, VAST, 18 Hoang Quoc Viet, Cau Giay, Hanoi * Email: chinhluuvan@ Received: 20 May 2016; Accepted for publication: 29 October 2016 ABSTRACT Two new conjugates of murrayafoline A with zerumbone and artemisinin 3, 11 were prepared by N-alkylation, in which, compound 3 was synthesized from two consecutive Nalkylation reactions. Their cytotoxicity was evaluated on four human cancer cell lines Hep-G2, LU, RD and Fl. The result showed that both compounds exhibited no activity against the tested cell lines. Keywords: murrayafoline A, N-alkylation, cytotoxicity, sesquiterpene, conjugate. 1. INTRODUCTION A number of natural carbazole alkaloids were recognized to exhibit potential biological activities such as antimicrobial [1, 2], anti-HIV [3], anticancer [4, 5, 6] activities. Among them, several compounds were used as drugs for treatment of cancer [7]. Especially, murrayafoline A, a well-known carbazole alkaloid is promising cytotoxic carbazole in the roots of G. stenocarpa in Vietnam. This carbazole was reported to show significant growth suppression of the human leukemia cell line HL-60 due to apoptosis mediated by the activation of the caspase-9/caspase-3 pathway [7] and prevent heart diseases [8]. Recently, some of the N-substituted derivatives were synthesized and evaluated the anti-inflamamtory activity [9]. However, no reports on the synthesis and biological evaluation of conjugates between murrayfoline A and other bioactive compounds are available.
