Synthesis and antitumor activity of tetrandrine derivatives.
Tetrandrine possesses antitumor activity, however, only a few studies on its structure modification were reported. To improve the antitumor activity of tetrandrine, 20 new tetrandrine derivatives were designed and synthesized by Sonogashira and Suzuki reactions. Their antitumor activities were evaluated against three tumor cell lines including A549, HepG2, and BGC-823 by methyl thiazolyl tetrazolium assay with taxol as a positive control. The results showed that compounds 2c and 2g were highly potent against BGC-823 cell line, and compounds 1i and 1k showed particular activity against HepG2 cells. These results demonstrated that compounds 1i, 1k, 2c, and 2g were promising leads for further investigation.
a State Key Laboratory of New Drug & Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry , Shanghai , 200040 , China.
Chun-Zhen
CZ
Wu
Long
L
Lai
Xiao
X
Hu
Rong-Rong
RR
Lei
Yi-Fang
YF
Yang
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D044182:Benzylisoquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D056945:Hep G2 Cells; D006801:Humans; D015394:Molecular Structure; D019906:Nuclear Magnetic Resonance, Biomolecular; D018517:Plant Roots / Q000737:chemistry; D031607:Stephania / Q000737:chemistry; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D044182:Benzylisoquinolines; C009438:tetrandrine