Synthesis and evaluation of a thio analogue of duocarmycin SA.
The design, synthesis, and preliminary evaluation of methyl 1,2,8,8a-tetrahydrocyclopropa[c]thieno[3,2-e]indol-4-one-6-carboxylate (CTI) derivatives are detailed representing a single atom change (N to S) embedded in the duocarmycin SA alkylation subunit.
MacMillan
Karen S
KS
Department of Chemistry and the Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.
Lajiness
James P
JP
Cara
Carlota Lopez
CL
Romagnoli
Romeo
R
Robertson
William M
WM
Hwang
Inkyu
I
Baraldi
Pier Giovanni
PG
Boger
Dale L
DL
D018906:Antineoplastic Agents, Alkylating / Q000138:chemical synthesis / Q000737:chemistry*; D000080890:Duocarmycins; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry*; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry; D013438:Sulfhydryl Compounds / Q000138:chemical synthesis / Q000737:chemistry*; D013876:Thiophenes / Q000138:chemical synthesis / Q000737:chemistry*
D018906:Antineoplastic Agents, Alkylating; D000080890:Duocarmycins; D007211:Indoles; D011758:Pyrroles; D013438:Sulfhydryl Compounds; D013876:Thiophenes; C066098:duocarmycin SA