Project's information

Project's title Synthesis and exploration for anticancer activity of novel murrayafoline A derivatives
Research hosting institution Institute of Natural Products Chemistry
Project leader’s name Dr. Luu Van Chinh
Project duration 01/01/2015 - 01/01/2016
Project’s budget 600.000.000 VNĐ
Classify Excellent
Goal and objectives of the project

-Prepare 10-15 murrayafoline A derivatives by chemical modification of functional groups –NH-, -CH3 and –OCH3
-Screening for their in vitro anticancer activity in order to select a compound for in vivo evaluation

Main results

-In this project, 35 novel derivatives were successfully synthesized from murrayafoline A in moderate yields. Among which, 20 new derivatives are conjugates of murrayafoline A with 2'-hydroxychalcones, 4'-hydroxychalcones and 2',4'-dihydroxychalcones, 8 derivatives were formed by the connection between murrayafoline A with amines via trimethylene bridge. 4 New amino alcohols with structures are similar to those of β-blockers, 3 derivatives were obtained from the chemical modification of 1-OCH3 group and a conjugate is a Mannich base of murrayafoline A and zerumbone
-The screening for in vitro anticancer activity showed that a number of the synthesized derivatives exhibited activity against human cancer cell lines: Hep-G2, LU, FL, MCF7, Jurkat, P338 and SW480 with IC50 values < 5 µg/mL
-Conjugate 140 of murrayafoline A and zerumbone was evaluated in vivo anticancer activity using the LLC cancer cell (Lewis Lung Carcinoma). The results indicated that the tumor volumn reduced by 38.49% in comparision to that of Doxorubicin (64.77%)

Novelty and actuality and scientific meaningfulness of the results

A number of novel derivatives of murayafoline A with various structures were successfully synthesized and screened for in vitro and in vivo anticancer activities

Products of the project

-35 novel murrayafoline A derivatives
-The results of evaluation for in vitro and in vivo activities

Scientific results:
1. Vuong Van Truong, Tran Duy Nam, Truong Ngoc Hung, Nguyen Thi Nga, Pham Minh Quan, Luu Van Chinh, Sang-Hun Jung (2015); Synthesis and anti-proliferative activity of novel azazerumbone conjugates with chalcones; Bioorganic and Medicinal Chemistry Letters; Vol 25, pp 5181 – 5185, SCI
2. Lê Đức Anh, Trương Ngọc Hùng, Nguyễn Thị Nga, Lê Mai Hương, Lưu Văn Chính, Tổng hợp một số chalcone có chứa nhóm azide, Tạp chí Hóa học, tập 53 (5e1), 157-161, 2015.
3. Lê Đức Anh, Trương Ngọc Hùng, Nguyễn Thị Nga, Lê Mai Hương, Nguyễn Mạnh Cường, Vũ Thị Hà, Lưu Văn Chính, Tổng hợp và đánh giá hoạt tính kháng khuẩn của một số dẫn xuất mới của murrayafoline A, Tạp chí Hóa học, tập 53 (5e1), 162-167, 2015.
4. Le Duc Anh, Truong Ngoc Hung, Nguyen Thi Nga, Le Mai Huong, Tran Thi Hong Ha, Tran Thi Thu Thuy, Nguyen Manh Cuong, Le Thi Thoa, Tran Minh Cong, Nguyen Trong Dan, Luu Van Chinh, Synthesis and biological activity of novel derivatives of murrayafoline A, The Academic conference on natural science for young scientists, master and PhD. student from Acean countries, Proceedings, 223-229, 2015.
5. Le Duc Anh, Nguyen Thi Hai Ly, Truong Ngoc Hung, Nguyen Thi Nga, Nguyen Manh Cuong, Le Mai Huong, Le Phong, Luu Van Chinh, Synthesis and cytotoxic activity evaluation novel derivatives of murrayafoline A. Journal of Science and Technology, 54(2C), 507-514, 2016.