Antitumor agents 269. Non-aromatic ring-A neotanshinlactone analog, TNO, as a new class of potent antitumor agents.
Tetrahydroneotanshinlactone (TNT) and tetrahydronaphthalene-1-ol (TNO) derivatives were designed, synthesized, and evaluated for cytotoxic activity. The TNO derivatives were found to be a promising novel class of in vitro antitumor agents. The cyclohexene ring-A could dramatically affect the antitumor activity and selectivity. Compound 20 showed the highest potency with ED(50) values of 0.7 and 1.7 microM against SK-BR-3 and ZR-75-1 breast cancer cell lines, respectively.
Dong
Yizhou
Y
Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA.
Shi
Qian
Q
Nakagawa-Goto
Kyoko
K
Wu
Pei-Chi
PC
Bastow
Kenneth F
KF
Morris-Natschke
Susan L
SL
Lee
Kuo-Hsiung
KH
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy; D045744:Cell Line, Tumor; D049109:Cell Proliferation; D015195:Drug Design; D019008:Drug Resistance, Neoplasm; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D005663:Furans / Q000494:pharmacology*; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy / Q000473:pathology; D051379:Mice; D008819:Mice, Nude; D015394:Molecular Structure; D011724:Pyridazines; D011753:Pyrones / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D000972:Antineoplastic Agents, Phytogenic; D005663:Furans; D011724:Pyridazines; D011753:Pyrones; C494351:neotanshinlactone