Atsushi Akao

Cytotoxicity and actin-depolymerizing activity of aplyronine A, a potent antitumor macrolide of marine origin, and its analogs

Abstract Artificial analogs of aplyronine A ( 1 ), a potent antitumor macrolide, were synthesized and structure–activity (cytotoxicity and actin-depolymerizing activity) relationships were investigated; the side-chain in 1 was found to play a key role in both biological activities.

Cytotoxicity and actin depolymerizing activity of aplyronine A, a potent antitumor macrolide of marine origin, and the natural and artificial analogs

Abstract The artificial analogs of aplyronine A ( 1 ), a potent cytotoxic and antitumor macrolide, were synthesized and the structure-activity (cytotoxicity and actin depolymerizing activity) studies were performed; the side chain portion in 1 was found to play a key role in both biological activities.

Practical synthesis of a potent indolocarbazole-based, DNA topoisomerase inhibitor

Abstract DNA topoisomerase I inhibitors are currently under investigation as cancer chemotherapy agents of which indolocarbazole glycoside ( 1 ) has been identified as a promising candidate. A practical, scalable synthesis of 1 that limits the isolation of cytotoxic compounds to only that of the final product is described. The convergent process features a novel phase transfer-promoted glycosylation of aglycone core ( 4 ); subsequent hydrolysis provides anhydride ( 8 ). The hydrazine fragment ( 3 ), which is coupled with 8 , is synthesized via a modification of existing procedures. The coupled product ( 2 ) is subsequently hydrogenated to provide 1 in excellent purity via direct crystallization (>99.3 A%).