154889-68-6Relevant articles and documents
Antitumor antibiotics: Duocarmycins
Nagamura, Satoru,Saito, Hiromitsu
, p. 1386 - 1405 (2007/10/03)
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The synthesis of [3H]KW-2189, a novel active antitumor antibiotic
Nagamura, Satoru,Kinugawa, Masahiko,Ogasa, Takehiro,Saito, Hiromitsu
, p. 471 - 477 (2007/10/03)
The synthesis of [3H]KW-2189, 2, a novel active antitumor antibiotic, is described. The key intermediate 6 in the synthesis, was synthesized in four steps from duocarmycin B2 (1). Treatment of 6 with [3H]methyl iodide in the presence
Synthesis and antitumor activity of duocarmycin derivatives: Modification of segment A of duocarmycin B2
Nagamura, Satoru,Asai, Akira,Kanda, Yutaka,Kobayashi, Eiji,Gomi, Katsushige,Saito, Hiromitsu
, p. 1723 - 1730 (2007/10/03)
Several A-ring pyrrole derivatives of duocarmycin B2 were synthesized effectively from the 3-hydroxy compounds by utilizing an interesting acid- catalyzed rearrangement, their anticellular activity was preliminarily evaluated by assays of growth inhibition of HeLa S3 cells (in vitro) and antitumor activity against murine sarcoma 180 (in vivo). The 8-O-N,N- dialkylcarbamoyl derivatives of the A-ring pyrrole compound showed remarkably potent in vivo antitumor activity, superior to that of duocarmycin B2. These derivatives were subjected to further biological evaluation. They exhibited potent antitumor activity toward murine solid tumors including M5076 sarcoma, B-16 melanoma and Colon 26 adenocarcinoma. Their most noteworthy feature was their efficacy against various human xenografts including LC-6 (lung), St-4 (stomach), and Co-3 (colon).
