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Synthesis, Antitumor Activity, and Structure-activity Relationship of Some Benzo[a]pyrano[2,3-c]phenazine Derivatives

[ Vol. 18 , Issue. 10 ]

Author(s):

Jing Gao, Ming Chen, Xue Tong, He Zhu, Hongbin Yan, Daichun Liu, Wanjing Li, Shengyu Qi, Dake Xiao, Yongzhi Wang, Yuanyuan Lu and Feng Jiang   Pages 960 - 974 ( 15 )

Abstract:


A series of benzo[a]pyrano[2,3-c]phenazine derivatives with a wide range of substitutions at ring C of the benzophenazine were designed and synthesized using the one-pot, four-component domino reactions. The targeted compounds were evaluated for their antitumor activities against HCT116, MCF7, HepG2 and A549 cancer cell lines in vitro. The most active compound 6{1,2,1,9} featured the CN and p-dimethylamino phenyl substituents on γ-pyran structure on ring C. Significantly, compound 6{1,2,1,9} was found to have the highest growth inhibitory activity against the HepG2 cell line with IC50 values of 6.71 µM, which was 1.6-fold more potent than positive control anticancer drug Hydroxycamptothecine (HCPT). Furthermore, structure-activity relationship (SAR) studies on the substitutions at ring C were discussed in details.

Keywords:

Antitumor activity, benzo[a]pyrano[2, 3-c]phenazine, SAR.

Affiliation:

School of Engineering, China Pharmaceutical University, Nanjing, Jiangsu 210009, China.



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