| Structure Identification: |
| Bioorg Med Chem Lett. 2009 Jun 1;19(11):3036-40. | | Synthesis of aristolactam analogues and evaluation of their antitumor activity.[Pubmed: 19394218] | A series of natural aristolactams and their analogues have been prepared and evaluated for antitumor activity against human cancer cells, including multi-drug resistant cell lines.
METHODS AND RESULTS:
Naturally occurring aristolactams, such as aristolactam BII (cepharanone B), aristolactam BIII, Aristolactam FI (piperolactam A), N-methyl piperolactam A, and sauristolactam showed moderate antitumor activities in selected cell lines.
However, several synthetic aristolactam derivatives exhibited potent antitumor activities against a broad array of cancer cell lines with GI(50) values in the submicromolar range. | | Org Lett. 2008 Aug 21;10(16):3543-6. | | Total synthesis of aristolactams via a one-pot suzuki-miyaura coupling/aldol condensation cascade reaction.[Pubmed: 18642834] |
METHODS AND RESULTS:
A direct one-pot synthesis of phenanthrene lactams, which employs a Suzuki-Miyaura coupling/aldol condensation cascade reaction of isoindolin-1-one with 2-formylphenylboronic acid, has been developed. The approach is used to efficiently produce a number of natural aristolactams, such as aristolactam BII (cepharanone B), aristolactam BIII, Aristolactam FI (piperolactam A), N-methyl piperolactam A, and sauristolactam. |
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