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Combinatorial Chemistry & High Throughput Screening


ISSN (Print): 1386-2073
ISSN (Online): 1875-5402

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

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

Volume 18, Issue 10, 2015

Page: [960 - 974] Pages: 15

DOI: 10.2174/1386207318666150915113549

Price: $65


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.

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