Novel semisynthetic spin-labeled derivatives of podophyllotoxin with cytotoxic and antioxidative activity.
A series of novel spin-labeled podophyllotoxin derivatives were synthesized by reacting the corresponding N-(1-oxyl-2,2,6,6-tetramethyl-4-piperidinyloxy carbonyl)-amino acids with 4beta-amino-4'-demethylepipodophyllotoxin. The synthesized derivatives 12a-g were evaluated for the partition coefficients, cytotoxicities in vitro against three tumor cell lines (A-549, HL-60, and RPMI-8226) and antioxidative activities in tissues of SD rats by the TBA method. The vast majority of target compounds have shown superior or comparable activities against A-549, HL-60, and RPMI-8226 compared to VP-16, and they have shown more significant antioxidative activities and superior water solubility than VP-16.
Zhang
Jia-Qiang
JQ
State Key Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou 730000, China.
Zhang
Zhi-Wei
ZW
Hui
Ling
L
Chen
Shi-Wu
SW
Tian
Xuan
X
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000975:Antioxidants / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D003603:Cytotoxins / Q000138:chemical synthesis* / Q000494:pharmacology; D019073:HT29 Cells; D006801:Humans; D011034:Podophyllotoxin / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D013113:Spin Labels / Q000138:chemical synthesis*
D000970:Antineoplastic Agents; D000975:Antioxidants; D003603:Cytotoxins; D013113:Spin Labels; D011034:Podophyllotoxin